Drug composition antagonistic to both pgd2/txa2 receptors

Abstract

A compound of the formula (I): 1

Description

TECHNICAL FIELD

[0001] This invention relates to a pharmaceutical composition comprising a dual antagonist against thromboxane A2 and prostagrandin D2 receptors and in detail, a compound having a [2.2.1] or [3.1.1.] bicyclo skeleton.

BACKGROUND ART

[0002] As a pharmaceutical composition comprising a dual antagonist against PGD2/TXA2 receptors, a compound of the formula: 2

[0003] wherein RX is optionally substituted single ring or fused heterocyclyl; X is hydrogen or alkyl was described in WO 99/15502. The above mentioned compound has a substituent of the formula: —CH2—CH═CH—CH2—CH2—CH2—COOX wherein X is hydrogen or alkyl, as an a chain and R on an a) chain is a single or fused heterocycl optionally substituted with amino, halogen, hydroxy and the like.

[0004] Further, the other compounds having a [2.2.1] bicyclo skeleton similar to the compounds of the present invention have been described in WO97/00853 and the like. In this publication, it is described that the compounds are useful as prostagrandin D2 (PGD2) antagonists.

[0005] However, in these publications, almost none of compound having other substituents than those represented by the formula: 3

[0006] wherein X1 and X3 are each independently optionally substituted aryl, optionally substituted heteroaryl or optionally substituted non-aromatic heterocyclyl; X2 is a bond, —CH2—, —S—, —SO2— and the like; X4 is —CH2— and the like; m is 0 or 1; p is 0 or 1 as the ω chain, and furthermore, the formula: —CH2—CH═CH—CH2—CH2—CH2—COOR2 wherein R2 is hydrogen or alkyl, as the α chain of bicyclic ring, has been described.

[0007] PGD2 receptor antagonists have a quite different character from that of TXA2 receptor antagonists in the site and mechanism of action and indications thereof.

[0008] On the other hand, a compound having a dual antagonistic activity against both a TXA2 receptor and a PGD2 receptor can be useful as therapeutic agents for various diseases caused by TXA2 or PGD2.

[0009] For example, in the case of bronchial asthma, it is known that TXA2 cause potent tracheal contraction and respiratory anaphylaxis and PGD2 effects infiltration of eosionophils. From these comprehension, TXA2 and PGD2 are thought to be one of causative substances of the pathopoiesis and advance of asthma, thus the dual antagonistic compounds are expected to be more potent agents for treating asthma than ever known antagonists.

[0010] Further, in the case of allergic rhinitis, it is recognized that TXA2 and PGD2 cause the swelling of nasal mucosa through the aggravation of vascular permeability, and PGD2 induces the nasal blockage through the enlargement of vascular volume. Therefore, the dual antagonistic compounds are expected to be more potent agents for treating nasal blockage than ever known antagonists.

[0011] These diseases and condition thereof might be treated by administering both a TXA2 receptor antagonist and a PGD2 receptor antagonist at the same time, for example, in combination therapy or as a mixture thereof. But the administration of two or more agents often causes some problems due to the difference of their metabolic rate. For example, when the antagonists are different from each other in the time to reach a maximum blood concentration or the duration of action, they do not always efficiently exhibit each receptor antagonistic effect at the same time, failing to give a desired additive or synergic effect.

[0012] It has therefore been desired to develop medicines having a dual antagonistic activity against TXA2/PGD2 receptors, which exhibit new excellent therapeutic effects and can be used for many indications.

[0013] On the other hand, it was disclosed that 3-oxa-derivatives were prepared as metabolically stable TXA2/PGH2 receptor antagonists in Bioorganic & Medicinal Chemistry Letters, Vol.2, No.9, pp. 1069-1072, 1992. The active value of the compound was only described but the metabolic stability has not been described in the literature. 4

[0014] wherein, Z is p-fluorophenyl; Rx is benzenesulfonamino and the like.

[0015] Furthermore, it was reported in PROSTAGLANDINS, 1986, 31, 95 that ILOPROST, PGI2 mimetics was stabilized metabolically by converting to the 3-oxa-derivative. But, remaining activity of each compound was only compared under a presence of the metabolic enzyme of a rat and the metabolic stability did not mentioned, since there was a possibility of a production of active metabolites

DISCLOSURE OF INVENTION

[0016] The present inventors have studied intensively to develop a pharmaceutical composition having a dual antagonistic activity against TXA2/PGD2 receptors and found out new compounds and pharmaceutical compositions comprising them.

[0017] The present invention provides:

[0018] (1) a compound of the formula (I): 5

[0019] wherein 6

[0020] A is alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond;

[0021] R is —C(═O)—R1, —CH2—R1, or tetrazolyl;

[0022] R1 is hydroxy, alkyloxy, or optionally substituted amino;

[0023] m is 0 or 1;

[0024] provided that combinations wherein m is 1, A is —CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 (R1 is hydroxy or alkyloxy) and wherein A is —CH2—CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 wherein R1 is hydroxy or alkyloxy are excluded, p is 0 or 1, provided when p=0, X1 is not bonded to X3 via X4;

[0025] X1 and X3 are each independently optionally substituted aryl, optionally substituted heteroaryl or optionally substituted non-aromatic heterocyclyl;

[0026] X2 is a bond, —CH2—, —CH2—CH2—, —C(═O)—, —O—, —S—, —SO—, —SO2—, —NH—, —N(CH3)—, —C(═N—O—CH3)—, —N═N—, —CH═CH—, —(C═O)—NH—, —NH—(C═O)—, —CH2—NH—, —NH—CH2—, —CH2—O—, —O—CH2—, —CH2—, —S—CH2—, —CH2—SO2—, —SO2—CH2—, —SO2—NH—, —NH—SO2—, —C(═CH2)—, —SO2N(Me)—, —CH2NHSO2—, —CH2NH—(C═O)—, —NH—C(═O)—NH or —NH—C(═O)—N(Me)—;

[0027] X4 is —CH2—, —CH2—CH2—, —C(═O)—, —SO—, —SO2—, —(C═O)—NH—, —NH—(C═O)—, —CH2—NH—, —NH—CH2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, —CH2—SO2—, —SO2—CH2—, —SO2—NH— or —NH—SO2—,

[0028] provided that a combination wherein 7

[0029] A is —CH═CH—CH2—CH2—CH2—, R is —COOH, m is 1, p is 0, X1 and X3 are phenyl, and X2 is —N═N—, is excluded

[0030] and provided that when 8

[0031] X1 and X3 are phenyl, X2 is —CH═CH—, —O—, or —S—, m is 0, and p is 0, a compound wherein A is —CH═CH—CH2—CH2—CH2—C(CH3)2— and R is COOH, A is —CH2—C(═O)—CH2—CH2—CH2—CH2— and R is COOH, A is —CH2—CH2—CH2—CH2—CH2— and R is —COOH, or A is —CH═CH—CH2—CH2—CH2— and R is —CH2OH,

[0032] is excluded,

[0033] a prodrug, a pharmaceutically acceptable salt or a solvate thereof,

[0034] (2) A compound as described in (1) wherein A is alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having a unsaturated bond;

[0035] R is —C(═O)—R1, —CH2—R1, or tetrazolyl;

[0036] R1 is hydroxy, alkyloxy, or optionally substituted amino;

[0037] provided compounds wherein A is —CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 (R1 is hydroxy or alkyloxy), or A is —CH2—CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 wherein R1 is hydroxy or alkyloxy are excluded,

[0038] a prodrug, a pharmaceutically acceptable salt or a solvate thereof,

[0039] (3) A compound as described in (1) or (2), wherein A is alkylene intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond,

[0040] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0041] (4) A compound as described in (1) or (2), wherein A is C1 to C4 or C7 to C9 alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond, a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0042] (5) A compound as described in (1) or (2), wherein A is —CH213 CH2—CH2—, —CH2—CH2—CH(F)—, —CH2CH═CH—, —CH2—O—CH2—, —CH2CH═C(F)—, —CH2—CH2—CH2—CH2—, —CH2CH═CH—CH2—, —CH2—CH2—CH═CH—, —CH═CH—CH2—CH2—, —CH2—CH2—O—CH2—, —CH2—CH2—S—CH2—, —CH2—CO—NH—CH2—, —CH2—CH2—CH2—CH2—CH2—, —CH2CH═CH—CH2—CH2—, —CH213 CH2—CH2—CH═CH—, —CH2—CH2—CH2—O—CH2—, —CH2—CH2—CH2—S—CH2—, —CH2—CH2—CO—NH—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—CH(Me)—, —CH2—CH2—CH2—CH2—CH2—C(Me)2—, —CH2—CH2—CH2—CH2—CH2—CH(F)—, —CH2—CH═CH—CH2—CH2—CH(Me)—, —CH2—CH═CH—CH2—CH2—C(Me)2—, —CH2—CH═CH—CH2—CH2—CH(F)—, —CH2—CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—CH2—CH═C(Me)—, —CH2—CH2—CH2—CH2—C(Me)═CH—, —CH2—CH2—CH2—CH2—CH═C(F)—, —CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH═CH—CH2—O—CH2—, —CH2—CH═CH—CH2—S—CH2—, —CH2—CH═C(F)—CH2—O—CH2—, —CH2—CH2—O—CH2—CH═CH—, —CH2—CH2—CH2—CH2—S—CH2—, —CH2—CH2—CH2—CO—NH—CH2—, —CH2—CH2CH═N—O—CH2—, —CH2—CH2—S—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—CH2—, or —CH2—CH═CH—CH2—CH2—CH2—CH2—CH2—,

[0043] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0044] (6) A compound as described in (5), wherein A is —CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH═CH—CH2—O—CH2—, —CH2—CH═CH—CH2—S—CH2—, or —CH2—CH2—CH2—CH2—S—CH2—,

[0045] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0046] (7) A compound as described in (6), wherein A is —CH2—CH2—CH2—CH2—O—CH2—,

[0047] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0048] (8) A compound as described in any one of (1) to (7), wherein X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl,

[0049] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0050] (9) A compound as described in (8), wherein at least one of X1 and X3 is optionally substituted heteroaryl,

[0051] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0052] (10) A compound as described in (9), wherein X1 and X3 are each independently optionally substituted heteroaryl,

[0053] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0054] (11) A compound as described in (9), wherein at least one of X1 and X3 is optionally substituted thienyl or optionally substituted benzothienyl,

[0055] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0056] (12) A compound as described in any one of (1) to (11), wherein X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or —NH—C(═O)—NH—,

[0057] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0058] (13) A compound as described in any one of (1) to (12), wherein m is 0 and p is 0,

[0059] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0060] (14) A compound as described in any one of (1) to (13), wherein R is —C(═O)—R1 and R1 is hydroxy, alkyloxy, or optionally substituted amino,

[0061] a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

[0062] (15) A pharmaceutical composition containing a compound, a prodrug, a pharmaceutically acceptable salt, or a solvate thereof as described in any one of above (1) to (14),

[0063] (16) A pharmaceutical composition having a dual antagonistic activity against PGD2/TXA2 receptors as described in the above (15),

[0064] (17) A pharmaceutical composition as described in the above (15), which is used for treatment of asthma,

[0065] (18) A pharmaceutical composition as described in the above (15), which is used for the treatment of nasal blockage,

[0066] (19) A pharmaceutical composition as described in the above (15), which is used for the treatment of allergic conjunctivitis,

[0067] (20) A pharmaceutical composition as described in the above (15), which is used for the treatment of allergic rhinitis,

[0068] (21) Use of the compound as described in any one of (1) to (14) for the preparation of a pharmaceutical composition for treating asthma, nasal blockage, allergic conjunctivitis or allergic rhinitis,

[0069] (22) A method for treating nasal blockage, allergic conjunctivitis or allergic rhinitis, which comprises administrating a compound as described in any one of (1) to (14),

[0070] (23) A compound of formula: X3—X2—X1—COOH wherein X3 is pyrrolyl optionally substituted with alkyl, alkyloxy or halogen, indolyl optionally substituted with alkyl, alkyloxy or halogen, indolinyl optionally substituted with alkyl, alkyloxy or halogen, or 1,2,3,4-tetrahydroquinolyl optionally substituted with alkyl, alkyloxy or halogen; X2 is —SO2—, —S— or —CH2—; X1 is thienyl, or a salt thereof,

[0071] (24) A compound as described in (23), wherein a substituent of the formula: —X1—X2—X3 is 5-(1-pyrrolylsulfonyl)thiophen-2-yl, 5-[(2-methyl-1-pyrrolyl)sulfonyl]thiophen-2-yl, or 5-[(2,5-dimethyl-1-pyrrolyl)sulfonyl]thiophen-2-yl, or a salt thereof.

BEST MODE FOR CARRYING OUT THE INVENTION

[0072] Special feature of a compound in the present invention is

[0073] (A) a bicyclic ring represented by the Y ring of the above formula (I) is [2.2.1] or [3.1.1] skeleton,

[0074] (B) an ω chain attached to the bicyclic ring, a group represented by the formula: 9

[0075]  of the above formula (I), includes —NH—CO—, and X1 and X3 are each independently optionally substituted aryl, optionally substituted heteroaryl or optionally substituted non-aromatic heterocyclyl;

[0076] (C) X1 bonds to X3 via X2,

[0077] (D) an α chain is represented by the formula: —A—R, wherein A is alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond; R is —C(═O)—R1, —CH2—R1, or tetrazolyl; R1 is hydroxy, alkyloxy, or optionally substituted amino, and the like.

[0078] Provided that a compound wherein A is —CH2—CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 (R1 is hydroxy or alkyloxy), is not included in the present invention, since the compound is metabolically unstable coused by oxidizaton of an α-chain at β-position.

[0079] Therefore, a compound of the present invention has a special feature at A and R and has an improved metabolic property. Further, a compound of the present invention is a dual antagonistic activity against PGD2/TXA2 receptors having the above mentioned features (A) to (D).

[0080] A preferred embodiment is a compound of the formula (I) wherein

[0081] (1) X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl,

[0082] (2) at least one of X1 and X3 is optionally substituted heteroaryl,

[0083] (3) X1 and X3 are each independently optionally substituted heteroaryl,

[0084] (4) at least one of X1 and X3 is optionally substituted thienyl or optionally substituted benzothienyl,

[0085] (5) X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2— or —NH—C(═O)—NH—,

[0086] (6) m is 0 and p is 0,

[0087] (7) R is —C(═O)—R1, wherein R1 is hydroxy, alkyloxy or optionally substituted amino,

[0088] (8) in a case of a combination of any one of (1) to (4) with (5),

[0089] (9) in a case of a combination of any one of (1) to (4) with (6),

[0090] (10) in a case of a combination of any one of (1) to (4) with (7).

[0091] Each term used herein is defined to have meanings below in either case of a single or a joint use with other terms, unless otherwise noted.

[0092] “Alkylene” used herein means a straight chain and branched chain C1 to C9 and refers to methylene, methylmethylene, dimethylmethylene, ethylmethylmethylene, ethylene, trimethylene, tetramethylene, pentamethylene, hexamethylene, heptamethylene, octamethylene, nonamethylene, and the like. The above mentioned alkylene optionally contains a hetero atom (oxygen atom, sulfur, nitrogen atom or the like), optionally has an oxo group (═O), is optionally substituted with halogen (e.g. F, Cl, Br, I, preferable is F) and/or optionally contains one or more unsaturated bond (double bond or triple bond) on the chain at any position. Examples are —CH2—CH2—CH2—, —CH2—CH2—CH(F)—, —CH2—CH═CH—, —CH2—O—CH2—, —CH2—CH═C(F)—, —CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—, —CH2—CH2—CH═CH—, —CH═CH—CH2—CH2—, —CH2—CH2—O2—CH2—, —CH2—CH2—S—CH2—, —CH2—CO—NH—CH2—, —CH2—CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH2—, —CH2—CH2—CH2—CH═CH—, —CH═CH—CH2—CH2—CH2—, —CH2—CH2—CH2—O—CH2—, —CH2—CH2—CH2—S—CH2—, —CH2—CH2—CO—NH—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—CH(Me)—, —CH2—CH2—CH2—CH2—CH2—C(Me)2—, —CH2—CH2—CH2—CH2—CH2—CH(F)—, —CH2—CH═CH—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH2—CH(Me)—, —CH2—CH═CH—CH2—CH2—C(Me)2—, —CH2—CH═CH—CH2—CH2—CH(F)—, —CH2—CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—CH2—CH═C(Me)—, —CH2—CH2—CH2—CH2—C(Me)═CH—, —CH2—CH2—CH2—CH2—CH═C(F)—, —CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH═CH—CH2—O—CH2—, —CH2—CH═CH—CH2—S—CH2—, —CH2—CH═C(F)—CH2—O—CH2—, —CH2—CH2—O—CH2—CH═CH—, —CH2—CH2—CH2—CH2—S—CH2—, —CH2—CH2—CH2—CO—NH—CH2—, —CH2—CH2—CH═N—O—CH2—, —CH2—CH2—S—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH2—CH2—CH2—, —CH2—CH2—O—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH═CH2—, and the like.

[0093] Especially, the following embodiment is preferred for the above mentioned “alkylene”:

[0094] 1) alkylene intervened with a heteroatom, optionally having an oxo group, optionally substituted halogen and/or optionally containing unsaturated bond(s),

[0095] 2) C1 to C4 or C7 to C9 alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted halogen and/or optionally containing unsaturated bond(s),

[0096] 3) —CH2—CH2—CH2—, —CH2—CH2—CH(F)—, —CH2—CH═CH—, —CH2—O—CH2—, —CH2—CH2—CH(F)—, —CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—, —CH2—CH2—CH═CH—, —CH═CH—CH2—CH2—, —CH2—CH2—O2—CH2—, —CH2—CH2—S—CH2—, —CH2—CO—NH—CH2—, —CH2—CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH2—, —CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—O—CH2—, —CH2—CH2—CH2—S—CH2—, —CH2—CH2—CO—NH—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—CH(Me)—, —CH2—CH2—CH2—CH2—CH2—C(Me)2—, —CH2—CH2—CH2—CH2—CH2—CH(F)—, —CH2—CH═CH—CH2—CH2—CH(Me)—, —CH2—CH═CH—CH2—CH2—C(Me)2—, —CH2—CH═CH—CH2—CH2—CH(F)—, —CH2—CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—CH2—CH═C(Me)—, —CH2—CH2—CH2—CH2—C(Me)═CH—, —CH2—CH2—CH2—CH2—CH═C(F)—, —CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH═CH—CH2—O—CH2—, —CH2—CH═CH—CH2—S—CH2—, —CH2—CH═C(F)—CH2—O—CH2—, —CH2—CH2—O—CH2—CH═CH—, —CH2—CH2—CH2—CH2—S—CH2—, —CH2—CH2—CH2—CO—NH—CH2—, —CH2—CH2—CH═N—O—CH2—, —CH2—CH2—S—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—CH2—CH2—, or —CH2CH═CH—CH2—CH2—CH2—CH2—CH2—,

[0097] 4) —CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH═CH—CH2—O—CH2—, —CH2—CH═CH—CH2—O—CH2—, or —CH2—CH2—CH2—CH2—S—CH2—, and

[0098] 5) —CH2—CH2—CH2—CH2—O—CH2—.

[0099] The term “heteroaryl” includes a group which has a bond at any substitutable and which can be converted from a 5- to 7-membered aromatic heterocycle containing one or more oxygen atom, sulfur atom and/or nitrogen atom in the ring, or such an aromatic heterocycle as fused with one or more carbocycle or other aromatic heterocycle. Any one of aromatic heterocycle and aromatic carbocycle may have a bond. “Heteroaryl” may have a bond at a nitrogen atom as well as a carbon atom of aromatic heterocycle or aromatic carbocycle. Examples of “heteroaryl” include pyrrolyl (e.g., 1-pyrrolyl, 2-pyrrolyl, 3-pyrrolyl), pyridyl (e.g., 2-pyridyl, 3-pyridyl, 4-pyridyl), pyrazolyl (e.g., 1-pyrazolyl, 3-pyrazolyl, 4-pyrazolyl), imidazolyl (e.g., 1-imidazolyl, 2-imidazolyl, 4-imidazolyl), pyrimidinyl (e.g., 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl), pyrazinyl (e.g., 2-pyrazinyl), indolyl (e.g., 1-indolyl, 2-indolyl, 3-indolyl, 4-indolyl, 5-indolyl, 6-indolyl, 7-indolyl), carbazolyl (e.g., 1-carbazolyl, 2-carbazolyl, 3-carbazolyl, 4-carbazolyl, 9-carbazolyl), benzimidazolyl (e.g., 1-benzimidazolyl, 2-benzimidazolyl, 4-benzimidazolyl, 5-benzimidazolyl), indazolyl (e.g., 1-indazolyl, 2-indazolyl, 3-indazolyl, 4-indazolyl, 5-indazolyl, 6-indazolyl, 7-indazolyl), quinolyl (e.g., 2-quinolyl, 3-quinolyl, 4-quinolyl, 5-quinolyl, 6-quinolyl, 7-quinolyl, 8-quinolyl), isoquinolyl (e.g., 1-isoquinolyl, 3-isoquinolyl, 4-isoquinolyl, 5-isoquinolyl, 6-isoquinolyl, 7-isoquinolyl, 8-isoquinolyl), furyl (e.g., 2-furyl, 3-furyl), benzofuryl (e.g., 2-benzofuryl, 3-benzofuryl, 4-benzofuryl, 5-benzofuryl, 6-benzofuryl, 7-benzofuryl), thienyl (e.g., 2-thienyl, 3-thienyl), benzothienyl (e.g., benzo[b]thiophen-2-yl, benzo[b]thiopben-3-yl, benzo[b]thiophen-4-yl, benzo[b]thiophen-5-yl, benzo[b]thiophen-6-yl, benzo[b]thiophen-7-yl), dibenzothienyl (e.g., 2-dibenzothienyl, 3-dibenzothienyl), dibenzofuryl (e.g., 2-dibenzofuryl, 3-dibenzofuryl), naphthothienyl (e.g., naphtho[2,3-b]thiophen-2-yl, naphtho[2,3-b]thiophen-3-yl, naphtho[1.2-b]thiophen-2-yl, naphtho[1.2-b]thiophen-3-yl), oxazolyl (e.g., 2-oxazolyl, 4-oxazolyl, 5-oxazolyl), isoxazolyl (e.g., 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl), thiazolyl (e.g., 2-thiazolyl, 4-thiazolyl, 5-thiazolyl), isothiazolyl (e.g., 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl), imidazothiazolyl (e.g., imidazo[2.1-b]thiazol-2-yl, imidazo[2.1-b]thiazol-3-yl), benzoisoxazolyl (e.g., benzo[d]isoxazol-3-yl), benzothiazolyl (e.g., benzo[d]thiazol-2-yl), and the like.

[0100] The term of “aromatic carbocycle or other aromatic heterocycle” which may fuse the above “heteroaryl” includes 5- to 7-membered aromatic cycle which may contains one or more oxygen atom, sulfur atom and/or nitrogen atom in the ring, or such an aromatic ring as fused with one or more other aromatic rings.

[0101] The term of “aryl” includes mono aromatic carbocyclyl (e.g., phenyl) or fused aromatic carbocyclyl (e.g., 1-naphthyl, 2-naphthyl, 1-anthryl, 9-anthryl, 1-phenanthryl, 10-phenanthryl).

[0102] The term of “non-aromatic heterocyclyl” includes a group which has a bond at any substitutable and which can be converted from 3- to 7-membered non-aromatic heterocyclyl which contains one or more oxygen atom, sulfur atom and/or nitrogen atom in the ring, or non-aromatic heterocyclyl which is fused with a carbon ring (e.g. aromatic carbocycle) or other heterocyclyl (e.g. aromatic heterocycle). The substitutable bond may exist not only on the carbon atom but also on the nitrogen atom in the non-aromatic heterocyclyl. Examples are aziridinyl, piperidino, piperidinyl, morphorino, morphorinyl, pyrrolinyl, pyrrolidinyl, imidazolinyl, piperadino, piperadinyl, isooxazolinyl, thiolanyl, tetrahydrofuranyl, dioxanyl, oxathianyl, tetrahydropyranyl, and the like. Preferable is 5- or 6-membered non-aromatic heterocyclyl containing a nitrogen atom. The following groups are exexplified as a group which has a bond at any substitutable and which can be converted from non-aromatic heterocyclyl fused with one or more carbon ring (e.g. aromatic carbocycle) or other heterocyclyl (e.g. aromatic heterocycle): 10

[0103] Furthermore, the substitutable bond may exist at any position of the carbon atom or the nitrogen atom.

[0104] “Aryl” or “heteroaryl” may be fused 4- to 7-membered cycloalkane or 4- to 7-membered non-aromatic heterocycle. Examples of cycloalkane include cyclobutane, cyclopentane, cyclohexane, and cycloheptane. Examples of non-aromatic heterocycle include pyrrolidine, piperazine, oxorane, 1,3-dioxorane, 1,4-dioxane, thiorane, or the like. The above “cycloalkane” and “non-aromatic heterocycle” may be fused with other aromatic carbocycle or aromatic heterocycle. Examples of aryl or heteroaryl fused with 4- to 7-membered cycloalkane or 4- to 7-membered non-aromatic heterocycle are illustrated below. 11

[0105] Examples of the substituent on “optionally substituted aryl”, “optionally substituted heteroaryl” or “optionally substituted non-aromatic heterocyclyl” include a group of the formula: —Z1′—Z2 wherein Z1 is a bond, —O—, —S—, —NH—, —NH—C(═O)—, —NH—C(═O)—O—, —NH—SO2—, —C(═O)—, —O—C(═O)—, —C(═O)—O—, or —SO2—; and Z2 is alkyl, haloalkyl, alkenyl, alkynyl, aryl optionally substituted with alkyl or halogen, heteroaryl optionally substituted with alkyl or halogen, arylalkyl optionally substituted with alkyl or halogen, heteroarylalkyl optionally substituted with alkyl or halogen, carboxy, halogen (F, Cl, Br, I), hydroxyalkyl, hydroxy, nitro, cyano, mercapto, thioformyl, thioacetyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, sulfino, sulfo, sulfamoyl, sulfoamino, optionally substituted amino, optionally substituted aminoalkyl, hydroxyamino, carbamoyl, or hydorazino. One to three substituents may be at any suitable position on the above aryl, heteroaryl, or non-aromatic heterocyclyl.

[0106] “Alkyl” includes a straight or branched C1 to C8 alkyl group or a C3 to C8 cycloalkyl group. Examples are methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, n-hexyl, n-heptyl, n-octyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and the like.

[0107] “Haloalkyl” includes a straight or branched C1 to C8 alkyl or C3 to C8 cycloalkyl group substituted with one or more halogen, for example, chloromethyl, fluoromethyl, trifluoromethyl, 2,2,2-trifluoroethyl, 1,1-difluoroethyl, trichloromethyl, 2,2,2-trichloroethyl, 1,1-dichloroethyl or the like.

[0108] “Alkenyl” includes a straight or branched C2 to C8 alkenyl or C3 to C8 cycloalkenyl group having one or more double bond(s), for example, vinyl, 1-propenyl, 2-propenyl, isopropenyl, 2-cyclobuten-1-yl, 2-cyclopenten-1-yl, 3-cyclopenten-1-yl, 2-cyclohexen-1-yl or the like.

[0109] “Alkynyl” includes a straight or branched C2 to C8 alkynyl having one or more triple bond(s), for example, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl or the like.

[0110] “Halogen” includes fluoro, chloro, bromo, and iodo.

[0111] “Alkyl” used in the term “arylalkyl” or “heteroarylalkyl” have the same meaning of the above “alkyl”, “aryl” used in the term “arylalkyl” have the same meaning of the above “aryl” and “heteroaryl” used in the term “heteroarylalkyl” have the same meaning of the above “heteroaryl”.

[0112] “Hydroxy alkyl” includes the above “alkyl” substituted with one or two hydroxy, for example, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 1,2-dihydroxy-n-propyl or the like.

[0113] Examples of the substituent of “optionally substituted amino” or “optionally substituted amino alkyl” include the above “alkyl”, the above “arylalkyl”, the above “aryl”, the above “heteroaryl”, the above “heteroarylalkyl” hydroxy. Alkylsulfonyl, or the like. They may be mono- or di-substituted with these substituents. When the substituent is alkyl, alkyl may form a ring together with a nitrogen atom of an amino group.

[0114] Example of “optionally substituted amino” includes amino, N,N-dimethylamino, N-ethyl-N-methylamino, N,N-(diethylamino, pyrrolidino, piperidino, N-methyl-N-phenylamino, isopropylamino, diisopropylamine, hydroxyamino, alkylsulfonylamino (e.g., methanesulfonylamino, ethanesulfonylamino, etc.), arylsulfonyl (e.g., benzenesulfonylamino, toluenesulfonylamino, etc.), N-alkyl-N-alkylsulfonylamino (e.g., N-methyl-N-methanesulfonylamino, etc.), halogenated alkylsulfonylamino (e.g., trifluoromethanesulfonylamino, etc.), or the like.

[0115] Examples of “optionally substituted aminoalkyl” include N,N-dimethylaminomethyl, N-ethyl-N-methylaminomethyl, N,N-diethylaminomethyl, pyrrolidinomethyl, piperidinomethyl, N-methyl-N-phenylaminomethyl, isopropylaminomethyl, diisopropylaminomethyl or the like.

[0116] “A pharmaceutical composition having a dual antagonistic activity against PGD2/TXA2 receptors” means a pharmaceutical composition comprising at least one compound of the formula (I) having an antagonistic activity against both a PGD2 receptor and a TXA2 receptor. In addition to a compound of the formula (I), the other active agents (e.g. antiiflammatory agents, antiallergy agents and the like) and pharmaceutically acceptable admixtures (e.g., binding agent, filler and the like) may be included.

[0117] The compound of the present invention has an antagonistic activity against PGD2 receptor and TXA2 receptor and can exhibit antagonistic activities against PGD2 receptor and TXA2 receptor in vivo. For example, even if a compound has both antagonistic activities against receptors in vitro, the compound administered can not always exhibit both of the antagonistic activity in vivo, owing to the preferential binding to the receptor of stronger affinity. Therefore, as a compound of the present invention, preferable is that the compound has antagonistic activities against PGD2 and TXA2 receptors and is 100 times, preferably 50 time and more preferably ca. 10 times in a ratio between affinities against PGD2 and TXA2 receptors. The ratio between affinities against PGD2 and TXA2 receptors can be calculated by the use of IC50 values and the like.

[0118] Furthermore, as a compound of the present invention, preferable is less than 0.1 μM in the binding activity against TXA2 receptor using human platelet membrane (IC50 value) and 0.1 μM in the antagonistic activity against PGD2 receptor using human platelet (IC50 value). In particular, the compound is preferable, in which both of the binding activity against TXA2 receptor using human platelet membrane (IC50 value) and the antagonistic activity against PGD2 receptor using human platelet (IC50 value) are less than 0.1 μM. Furthermore, the compound is preferable, in which their ratio is 100 times, preferably 50 time and more preferably ca. 10 times.

[0119] The present invention includes a method for treating asthma, nasal blockage, allergic conjunctivitis or allergic rhinitis which comprises administering a compound of the formula (I) and use of a compound of the formula (I) for manufacturing a medicine for asthma, nasal blockage allergic conjunctivitis or allergic rhinitis.

[0120] Furthermore, in a compound displayed in formula (I), “α chain” means a group represented by the formula: —A—R1, and “ω chain” means a group represented by the formula: 12

[0121] Preferable is following substituents as the α chain. Furthermore, E and Z mean E-form and Z-form in double bond of each formula, respectively. Each sign in 4A to 9B means an A part of the formula and means the same group in Table 1 to Table 15 in this description.

4A —CH2CH2CH2—R
4B —CH2CH2CH(F)—R
4C 13
4D 14
4E —CH2OCH2—R
5A —CH2CH2CH2CH2—R
5B 15
5C 16
5D 17
5E —CH2CH2OCH2—R
5F —CH2CH2SCH2—R
5G —CH2CONHCH2—R
6A —CH2CH2CH2CH2CH2—R
6B 18
6C 19
6D 20
6E —CH2CH2CH2OCH2—R
6F —CH2CH2CH2SCH2—R
6G —CH2CH2CONHCH2—
7A —CH2CH2CH2CH2CH2CH2—R
7B —CH2CH2CH2CH2CH2CH(Me)—R
7C —CH2CH2CH2CH2CH2C(Me)2—R
7D —CH2CH2CH2CH2CH2CH(F)—
7E 21
7F 22
7G 23
7H 24
7I 25
7J 26
7K 27
7L 28
7M —CH2CH2CH2CH2OCH2—R
7N 29
7O 30
7P 31
7Q 32
7R —CH2CH2CH2CH2SCH2—R
7S —CH2CH2CH2CONHCH2—R
7T —CH2CH2CH═N—OCH2—R2
7U —CH2CH2SCH2CH2CH2—R2
7V 33
8A —CH2CH2CH2CH2CH2CH2CH2—R2
8B 34
8C —CH2CH2CH2CH2CH2OCH2—R2
9A —CH2CH2CH2CH2CH2CH2CH2CH2—R2
9B 35

[0122] R is exemplified by —C(═O)—R1, —CH2—R1, or tetrazolyl and preferable is —C(═O)—R1, wherein, R1 is hydroxy, alkyloxy, or optionally substituted amino. Examples of R are COOH, COOMe, CONH2, CONHSO2Me, CH2OH, CH2OMe, CONHMe, CON(Me)SO2Me, 5-tetrazolyl, CONHSO2Ph, CONHSO2CF3 and the like.

[0123] Furthermore, the combination of A and R includes all of the combination and preferable is a combination described in Table 1 to Table 15.

[0124] As an ω chain, the following embodiments are preferred in the formula: 36

[0125] 1) wherein m is 0 and p is 0,

[0126] 2 ) wherein X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl,

[0127] 3) wherein at least one of X1 and X3 is optionally substituted heteroaryl,

[0128] 4) wherein X1 and X3 are each independently optionally substituted heteroaryl,

[0129] 5) wherein at least one of X1 and X3 is optionally substituted thienyl or optionally substituted benzothienyl,

[0130] 6) wherein X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or NH—C(═O)—NH—.

[0131] Concretely, preferable is a combination described below for the formula: —X1—X2—X3. Furthermore, each sign of 1 to 513 below means a group shown by the formula: —X1—X2—X3 and the compound number both in Table 1 to Table 15 and in Examples of reference in the present invention means the same group.

    —X1—X2—X3
1   37
2   38
3   39
4   40
5   41
6   42
7   43
8   44
9   45
10  46
11  47
12  48
13  49
14  50
15  51
16  52
17  53
18  54
19  55
20  56
21  57
22  58
23  59
24  60
25  61
26  62
27  63
28  64
29  65
30  66
31  67
32  68
33  69
34  70
35  71
36  72
37  73
38  74
39  75
40  76
41  77
42  78
43  79
44  80
45  81
46  82
47  83
48  84
49  85
50  86
51  87
52  88
53  89
54  90
55  91
56  92
57  93
58  94
59  95
60  96
61  97
62  98
63  99
64  100
65  101
66  102
67  103
68  104
69  105
70  106
71  107
72  108
73  109
74  110
75  111
76  112
77  113
78  114
79  115
80  116
81  117
82  118
83  119
84  120
85  121
86  122
87  123
88  124
89  125
90  126
91  127
92  128
93  129
94  130
95  131
96  132
97  133
98  134
99  135
100 136
101 137
102 138
103 139
104 140
105 141
106 142
107 143
108 144
109 145
110 146
111 147
112 148
113 149
114 150
115 151
116 152
117 153
118 154
119 155
120 156
121 157
122 158
123 159
124 160
125 161
126 162
127 163
128 164
129 165
130 166
131 167
132 168
133 169
134 170
135 171
136 172
137 173
138 174
139 175
140 176
141 177
142 178
143 179
144 180
145 181
146 182
147 183
148 184
149 185
150 186
151 187
152 188
153 189
154 190
155 191
156 192
157 193
158 194
159 195
160 196
161 197
162 198
163 199
164 200
165 201
166 202
167 203
168 204
169 205
170 206
171 207
172 208
173 209
174 210
175 211
176 212
177 213
178 214
179 215
180 216
181 217
182 218
183 219
184 220
185 221
186 222
187 223
188 224
189 225
190 226
191 227
192 228
193 229
194 230
195 231
196 232
197 233
198 234
199 235
200 236
201 237
202 238
203 239
204 240
205 241
206 242
207 243
208 244
209 245
210 246
211 247
212 248
213 249
214 250
215 251
216 252
217 253
218 254
219 255
220 256
221 257
222 258
223 259
224 260
225 261
226 262
227 263
228 264
229 265
230 266
231 267
232 268
233 269
234 270
235 271
236 272
237 273
238 274
239 275
240 276
241 277
242 278
243 279
244 280
245 281
246 282
247 283
248 284
249 285
250 286
251 287
252 288
253 289
254 290
255 291
256 292
257 293
258 294
259 295
260 296
261 297
262 298
263 299
264 300
265 301
266 302
267 303
268 304
269 305
270 306
271 307
272 308
273 309
274 310
275 311
276 312
277 313
278 314
279 315
280 316
281 317
282 318
283 319
284 320
285 321
286 322
287 323
288 324
289 325
290 326
291 327
292 328
293 329
294 330
295 331
296 332
297 333
298 334
299 335
300 336
301 337
302 338
303 339
304 340
305 341
306 342
307 343
308 344
309 345
310 346
311 347
312 348
313 349
314 350
315 351
316 352
317 353
318 354
319 355
320 356
321 357
322 358
323 359
324 360
325 361
326 362
327 363
328 364
329 365
330 366
331 367
332 368
333 369
334 370
335 371
336 372
337 373
338 374
339 375
340 376
341 377
342 378
343 379
344 380
345 381
346 382
347 383
348 384
349 385
350 386
351 387
352 388
353 389
354 390
355 391
356 392
357 393
358 394
359 395
360 396
361 397
362 398
363 399
364 400
365 401
366 402
367 403
368 404
369 405
370 406
371 407
372 408
373 409
374 410
375 411
376 412
377 413
378 414
379 415
380 416
381 417
382 418
383 419
384 420
385 421
386 422
387 423
388 424
389 425
390 426
391 427
392 428
393 429
394 430
395 431
396 432
397 433
398 434
399 435
400 436
401 437
402 438
403 439
404 440
405 441
406 442
407 443
408 444
409 445
410 446
411 447
412 448
413 449
414 450
415 451
416 452
417 453
418 454
419 455
420 456
421 457
422 458
423 459
424 460
425 461
426 462
427 463
428 464
429 465
430 466
431 467
432 468
433 469
434 470
435 471
436 472
437 473
438 474
439 475
440 476
441 477
442 478
443 479
444 480
445 481
446 482
447 483
448 484
449 485
450 486
451 487
452 488
453 489
454 490
455 491
456 492
457 493
458 494
459 495
460 496
461 497
462 498
463 499
464 500
465 501
466 502
467 503
468 504
469 505
470 506
471 507
472 508
473 509
474 510
475 511
476 512
477 513
478 514
479 515
480 516
481 517
482 518
483 519
484 520
485 521
486 522
487 523
488 524
489 525
490 526
491 527
492 528
493 529
494 530
495 531
496 532
497 533
498 534
499 535
500 536
501 537
502 538
503 539
504 540
505 541
506 542
507 543
508 544
509 545
510 546
511 547
512 548
513 549

[0132] A compound of the present invention can be any of the following stereo isomers of [2.2.1] and [3.1.1] bicyclic skeleton. 550551

[0133] In these stereo isomers, preferable is a compound having the skeleton of the formula: 552

[0134] The present invention includes all stereo isomers of them and the optional mixtures thereof. Namely, the bond binding to the bicyclic ring is in R configuration or S configuration, and all of the stereo isomers (diastereomer, epimer, enantiomer and the like), racemates, and optional mixture thereof are included in the present invention.

[0135] Moreover, the α chain of the compound of the present invention can be in Z configuration or E configuration, thus a compound having any of the configurations and the mixture thereof are included in the present invention.

[0136] A prodrug of a compound of the formula (I) is a derivative of the compound of the present invention having a group which can be decomposed chemically or metabolically, and such prodrug is converted to a pharmaceutically active compound of the present invention by means of solvolysis or by placing the compound in vivo under a physiological condition. Method for the selection and process of an appropriate prodrug derivative are described in the literature such as Design of Prodrugs, Elsevier, Amsterdam 1985.

[0137] When the compound of the formula (I) has a carboxyl group, an ester derivative prepared by reacting a basal acid compound with a suitable alcohol or an amide derivative prepared by reacting a basal acid compound with a suitable amine is exemplified as a prodrug. A particularly preferred ester derivative as an prodrug is an optionally substituted alkyl ester derivative (e.g., methyl ester, ethyl ester, n-propyl ester, isopropyl ester, n-butyl ester, isobutyl ester, tert-butyl ester, morpholinoethyl ester), an arylalkyl ester derivative (e.g., benzyl ester, phenethyl ester, benzhydryl ester), or the like. A particularly preferred amide derivative as a prodrug is alkyl amide derivative (e.g., N-methyl amide, N-ethyl amide, N-(n-propyl)amide, N-isopropyl amide, N-(n-butyl)amide, N-isobutyl amide, N-(tert-butyl)amide), aryl alkyl amide (e.g., N-benzyl amide, N-phenethyl amide, benzhydryl amide), or the like.

[0138] When the compound of the formula (I) has a hydroxy group, an acyloxy derivative prepared by reacting with a suitable acyl halide (e.g., acid chloride, halogenated acid) or a suitable acid anhydride (e.g., mixed acid anhydride) is exemplified as a prodrug. A particularly preferred acyloxy derivative as a prodrug is a derivative substituted with optionally substituted alkylcarbonyloxy (e.g., —OCOC2H5, —OCO(tert-Bu), —OCOC15H31, —OCOCH2CH2COONa, —OCOCH(NH2)CH3, —OCOCH2N(CH3)2—), optionally substituted arylcarbonyloxy (e.g., —OCO(m-COONa-Ph) or the like.

[0139] When the compound of the formula (I) has an amino group, an amide derivative prepared by reacting with a suitable acid halide or a suitable acid anhydride is exemplified as a prodrug. A particularly preferred amide derivative as a prodrug is a derivative substituted with optionally substituted alkylcarbonyl (e.g., —NHCO(CH2)20CH3, —NHCOCH(NH2)CH3) or the like.

[0140] Examples of a salt of the compound of the formula (I) or its prodrug include alkali metal salts such as lithium salts, sodium salts or potassium salts, alkaline-earth metal salts such as calcium salts, salts with organic bases such as tromethamine, trimethylamine, triethylamine, 2-aminobutane, tert-butylamine, diisopropylethylamine, n-butylmethylamine, cyclohexylamine, dicyclohexylamine, N-isopropylcyclohexylamine, furfurylamine, benzylamine, methylbenzylamine, dibenzylamine, N,N-dimethylbenzylamine, 2-chlorobenzylamine, 4-methoxybenzylamine, 1-naphthylene methylamine, diphenylbenzylamine, triphenylamine, 1-naphthylamine, 1-aminoanthorathene, 2-aminoanthorathene, dehydroabiethylamine, N-methylmorpholine, pyridine), basic amino acid salts such as arginine salts or lysine salts.

[0141] A solvate means a solvate with an organic solvent, a hydrate and the like of the compound of the formula (I), its prodrug or its pharmaceutically acceptable salt, for example, monohydrate, dihydrate or the like.

[0142] General processes for the preparation of the compounds of the formula (I) are illustrated as follows. 553

[0143] A is alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond;

[0144] R is —C(═O)—R1, —CH2—R1, or tetrazolyl;

[0145] R1 is hydroxy, alkyloxy, or optionally substituted amino;

[0146] m is 0 or 1;

[0147] provided that when m is 1, A is —CH═CH—CH2—CH2—CH2— and furthermore R is —C(═O)—R1 wherein R1 is hydroxy or alkyloxy, and provided that when A is —CH2—CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 wherein R1 is hydroxy or alkyloxy, a compound is excluded;

[0148] p is 0 or 1, provided that when p=0, X1 is not bonded to X3 via X4;

[0149] X1 and X3 are each independently optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted non-aromatic heterocyclyl;

[0150] X2 is a bond, —CH2—, —CH2—CH2—, —C(═O)—, —O—, —S—, —SO—, —SO2—, —NH—, —N(CH3)—, —C(═N—O—CH3)—, —N═N—, —CH═CH—, —(C═O)—NH—, —NH—(C═O)—, —CH2—NH—, —NH—CH2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, —CH2—SO2—, —SO2—CH2—, —SO2—NH—, —NH—SO2—, —C(═CH2)—, —SO2N(Me)—, —CH2NHSO2—, —CH2NH—(C═O)—, —NH—C(═O)—NH, or —NH—C(═O)—N(Me)—;

[0151] X4 is —C2—, —CH2—CH2—, —C(═O)—, —SO—, —SO2—, —(C═O)—NH—, —NH—(C═O)—, —CH2—NH—, —NH—CH2—, —CH2—O—, —O—CH2—, —CH2—, —S—CH2—, —CH2—SO2—, —SO2—CH2—, —SO2—NH— or —NH—SO2—.

[0152] As shown in the above process, the compound of the formula (I) can be prepared by reacting a carboxylic acid of the formula (M-2) or its reactive derivative with an amino compound of the formula (M-1).

[0153] The reactive derivatives of carboxylic acid of the formula (M-2) mean the corresponding acid halides (e.g., chloride, bromide, iodide), anhydrides (e.g., mixed anhydride with formic acid or acetic acid), active esters (e.g., N-hydroxysuccinimide ester), and the like, and include acylating agents used for the usual acylation of amino group.

[0154] For example, an acid halide is obtained by reacting the compound (M-2) with a thionyl halide (e.g., thionyl chloride), phosphorous halide (e.g., phosphorous trichloride, phosphorous pentachloride), oxalyl halide (e.g., oxalyl chloride), and the like, in accordance with known methods as described in the literatures.

[0155] The reaction can be conducted under a condition generally used for the acylation of amino group. For example, in the case of condensation with the acid halide, the reaction is carried out in a solvent such as an ether solvent (e.g., diethyl ether, tetrahydrofuran, dioxane), benzene solvent (e.g., benzene, toluene, xylene), halogenated hydrocarbon solvent (e.g., dichloromethane, dichloroethane, chloroform) as well as ethyl acetate, dimethylformamide, dimethyl sulfoxide, acetonitrile, or the like, if necessary, in the presence of a base (e.g., organic base such as triethylamine, pyridine, N,N-dimethylaminopyridine, N-methylmorpholine; inorganic base such as sodium hydroxide, potassium hydroxide, potassium carbonate, or the like) under cooling, at room temperature, or under heating, preferably at a temperature ranging from −20° C. to ice-cooling temperature, or from room temperature to a refluxing temperature of the reaction system, during several min to several hr, preferably for 0.5 hr to 24 hr, more preferably for 1 hr to 12 hr.

[0156] Unless R of a compound represented by the formula (M-1) is a carboxyl group, a free form may be used without converting the carboxy group (M-2) into the reactive derivatives and the reaction may be conducted in the presence of a condensing agent (e.g., dicyclohexylcarbodiimide (DCC), 1-ethyl-3-(3-methylaminopropyl)carbodiimide, N,N′-carbonyldiimidazole, or the like) usually used in the condensation reaction of amine and carboxylic acid.

[0157] When “optionally substituted aryl”, “optionally substituted heteroaryl” or “optionally substituted non-aromatic heterocyclyl” in X1 or X3 of the compound of the formula (M-2) is substituted with a hydroxy group or an amino group, such a compound can be used after protection by acetyl group or the like in accordance with the well known method.

[0158] In the reaction of the other reactive derivatives or free acid (M-2) with the amine (M-1), the reaction conditions are determined according to the property of each reactive derivative or free acid, in accordance with a known method. The reaction product can be purified in accordance with a conventional purification, such as the extraction with a solvent, chromatography, recrystallization, and the like.

[0159] In an object compound of the present invention, various derivatives in which R is —C(═O)—R1, —CH2—R1 or tetrazolyl (R1 is hydroxy, alkyloxy or optionally substituted amino) can be converted from a compound in which R is carboxylic acid. For instance, a derivative of the ester or the amide can be prepared by esterification or amidation, in accordance with the well known method. Furthermore, the ester derivative can be converted by reduction to an alcoholic derivative, which can be derived to an ether derivative by O-alkylation. A compound in which R is 5-tetrazolyl, can be prepared by converting an amide derivative having R; CONH2 to R: CN by dehydration in accordance with the well known method, followed by a reaction with sodium azide (J. Am. Chem. Soc. 1958, 80, 3908) or trimethylsilylazide (J. Org. Chem. 1993, 58, 4139).

[0160] In this process, the starting compound (M-1) wherein R1 is —CH2—CH═CH—CH2—CH2—CH2—COOMe, m is 0, Y is [2.2.1]bicyclic skeleton, 7-(3-amino-bicyclo[2.2.1]hept-2-yl)-5-heptenoic acid methyl ester is described in the Japanese Patent Publication (Kokoku) No. 79060/1993. The other starting compounds can be prepared from the aldehyde derivative (Q is a protecting group such as benzyloxycarbonyl, t-butoxycarbonyl and the like) represented by a general formula (M-1a) or (M-1b) by one or more reaction(s) of a yilide compound under a Wittig reaction condition (Org. Reaction, 1965, 14, 270) in combination with other reactions. In a starting compound, various derivatives wherein R is —C(═O)—R1, —CH2—R1 or tetrazolyl (R1 is hydroxy, alkyloxy or optionally substituted amino) can be converted from a compound wherein R is COOH. 554

[0161] For example, the aldehyde (M-1a) is reacted with (3-carboxypropyl)triphenylphosphonium salt under a well known Wittig reaction condition to give a starting material (M-5D), wherein A is —CH2═CH—CH2—CH2—. The compound M-5D is hydrogenated in the presence of palladium, platinum and the like to give a starting material (M-5A), wherein A is —CH2—CH2—CH2—CH2—. Furthermore, after a Wittig reaction using methoxymethyltriphenyl-phosphonium salt, followed by a hydrolysis with hydrochloric acid, formic acid, acetic acid and the like can furnish an aldehyde (M-1b) with one additional carbon atom and moreover a Wittig reaction with 2-(1,3-dioxoran-2-yl)ethyltriphenylphosphonium salt can give a compound represented by a general formula (M-1c). A Jones oxidation (J. Chem. Soc., 1946, 39) of the compound gives a starting material (M-5B) wherein A is —CH2—CH═CHCH2— in the formula (M-1). And by the above similar method, after an aldehyde (M-1d) was obtained by hydrogenation, followed by hydrolysis of the acetal with acid, either a Wittig reaction with a stable yield such as methyl (triphenylphophoranidene)acetate and the like or a Honer-Emmons reaction with methyl dimethylphosphonoacetate can convert to a starting material (M-7I), wherein A is —CH2—CH2—CH2—CH2—CH═CH—. When the above mentioned reaction is applied to an aldehyde (M-1b), a corresponding starting material (M-4B), wherein A is —CH2CH═CH— is obtained and furthermore a corresponding starting material (M-4A) wherein A is —CH2—CH2—CH2— is obtained by a hydrogenation of the double bond. When a starting material wherein A is —CH2—CH2—CH2—CH2—O—CH2— is required, a compound of the formula (M-4A) wherein R is CH2OH can be reacted with halogenated acetic acid or its ester, ether, or amide and the like in the presence of a base in accordance with known methods as described in the literatures.

[0162] Amidation with a starting carboxylic acid (M-2) can be accomplished after a deprotection of an amino protecting group Q in a way of conversion to α-chain, if necessary.

[0163] When p is 0, the carboxylic acid of the formula (M-2) can be prepared by reacting a carboxylic acid having X1 or its reactive derivative with a compound having X3. A person ordinary skilled in the art can carry out such a reaction by selecting the kinds of reactions and their conditions depending on the kind of X2.

[0164] A compound represented by the formula: X3—X2—X1—COOH wherein X3 is pyrrolyl optionally substituted with alkyl, alkyloxy or halogen, indolyl optionally substituted with alkyl, alkyloxy or halogen, indolinyl optionally substituted with alkyl, alkyloxy or halogen or 1,2,3,4-tetrahydroquinolyl optionally substituted with alkyl, alkyloxy or halogen; X2 is —SO2—, —S— or —CH2—; X1 is thienyl, or the pharmaceutically acceptable salt, or especially a substituent represented by the formula: X1—X2—X3 is 5-[(1-pyrrolyl)sulfonyl]thiophen-2-yl, 5-[(2-methyl-1-pyrrolyl)sulfonyl]thiophen-2-yl or 5-[(2,5-dimethyl-1-pyrrolyl)sulfonyl]thiophen-2-yl, or the pharmaceutically acceptable salt is important as an intermediate. Salt refers to lithium salt, sodium salt, potassium salt, calcium salt, triethylammonium salt, pyridinium salt or the like.

[0165] When p is 0, a group of the formula: —NHCO—X1—X2—X3 of the compound (I) can be introduced by reacting a carboxylic acid of the formula: X3—X2—X1—COOH (M-2) or its reactive derivative with amine (M-1), or by reacting a carboxylic acid having X1 or its reactive derivatives with amine (M-1) and reacting the obtained compound with a compound having X3.

[0166] In case of the introduction of a substituent(s) into the “optionally substituted aryl”, “optionally substituted heteroaryl” or “optionally substituted non-aromatic heterocyclyl”, the change of the functional group can be performed before or after reacting a carboxylic acid or its reactive derivative thereof (M-2) with the amine (M-1).

[0167] In an aromatic part such as aryl, heteroaryl and the like, usual methods of introduction or conversion of the functional group known for an aromatic ring can be applied. For example, the compound having an aromatic heterocycle substituted with a nitro group can be prepared through the nitration of the compound with a nitrating acid. Moreover, the compound having an aromatic heterocycle substituted with an amino group can be prepared through the reduction of the above-obtained compound with tin in the presence of hydrochloride. Moreover, the compound having an aromatic heterocycle substituted with hydroxy group can be prepared through the diazonization of the above-obtained compound and the hydrolysis with alkali. On the other hand, the compound having an aromatic heterocycle substituted with an alkoxy group can be prepared through the reaction of the diazonium derivative with alcohol. The compound having an aromatic heterocycle substituted with halogen can be prepared through Sandmeyer reaction, the reaction of the diazonium derivative with a copper salt (e.g., CuCl2, CuBr2). The compound having an aromatic heterocycle substituted with halogen can be also prepared through the direct reaction of the compound having an aromatic heterocycle with chlorine and the like. Using the above-mentioned methods appropriately, halogen can be introduced into a desired position(s). The group of alkyl, alkenyl or acyl group can be directly introduced into an aromatic heterocycle through Friedel Crafts reaction with alkylating agent, an alkenylating agent, or an acylating agent, respectively, in the presence of anhydrous aluminum chloride and the like.

[0168] The objective compound (I) of the present invention can be converted into a corresponding ester derivative, if desired. For example, the ester derivative can be prepared by esterification of a carboxylic acid in accordance with a known method.

[0169] When using the compound (I) of the present invention in treatment, it can be formulated into ordinary formulations for oral and parenteral administration. A pharmaceutical composition containing the compound (I) of the present invention can be in the form for oral and parenteral administration. Specifically, it can be formulated into formulations for oral administration such as tablets, capsules, granules, powders, syrup, and the like; or those for parenteral administration such as injectable solution or suspension for intravenous, intramuscular, or subcutaneous injection, inhalant, eye drops, nasal drops, suppositories, or percutaneous formulations such as ointment.

[0170] In preparing the formulations, carriers, excipients, solvents, and bases known to one having ordinary skill in the art may be used. In case of tablets, they are prepared by compressing or formulating an active ingredient together with auxiliary components. Examples of usable auxiliary components include pharmaceutically acceptable excipients such as binders (e.g., cornstarch), fillers (e.g., lactose, microcrystalline cellulose), disintegrants (e.g., starch sodium glycolate) or lubricants (e.g., magnesium stearate). Tablets may be coated appropriately. In case of liquid formulations such as syrups, solutions, or suspensions, they may contain suspending agents (e.g., methyl cellulose), emulsifiers (e.g., lecithin), preservatives, and the like. In case of injectable formulations, it may be in the form of solution, suspension, or oily or aqueous emulsion, which may contain suspension-stabilizing agents or dispersing agent, and the like. In case of an inhalant, it is formulated into a liquid formulation applicable to an inhaler. In case of eye drops, it is formulated into a solution or a suspension.

[0171] Especially, in case of a nasal drug for treating nasal blockage, it can be used as a solution or suspension prepared by a conventional formulating method, or administered as a powder formulated using a powdering agent (e.g., hydroxypropyl cellulose, carbopole) into the nasal cavity. Alternatively, it can be used as an aerosol filled into a special container together with a solvent of low boiling point.

[0172] In a case using as an eyewash drug for treating allergic conjunctivitis, it can be used as a solution or suspension of the compound or can be used by solving or suspending the compound before use. A stabilizing agent, solubilizing agent, suspending agent, emulsifier, buffer, preservatives and the like can be included. In a case using as an eyewash drug, aseptic treatment is preferable.

[0173] Pharmaceutical preparation of injection, oral agent, inhalation and the like is preferable for treating asthma.

[0174] Although an appropriate dosage of the compound (I) varies depending on the administration route, age, body weight, sex, or conditions of the patient, and the kind of drug(s) used together, if any, and should be determined by the physician in the end, in the case of oral administration, the daily dosage can generally be between 0.01-100 mg, preferably 0.01-10 mg, more preferably generally be between 0.01-100 mg, preferably 0.01-10 mg, more preferably 0.01-1 mg, per kg body weight. In case of parenteral administration, the daily dosage can generally be between 0.001-100 mg, preferably 0.001-1 mg, more preferably 0.001-0.1 mg, per kg body weight. The daily dosage can be administered in 1-4 divisions.

EXAMPLE

[0175] The following examples are provided to further illustrate the present invention and are not to be construed as limiting the scope.

Example 1

[0176] Preparation of (I-5A-59a), (I-5A-59b) 555

[0177] Potassium t-butoxide (4.32 g, 38.5 mmol) was added to a suspension of (3-carboxypropyl)triphenylphosphonium bromide (9.42 g, 22.0 mmol) in THF (45 ml) with cooling in ice. The mixture was stirred for 1 h and cooled to −10° C. A solution of compound (I) (3.0 g, 11.0 mmol) in THF (15 ml) was added dropwise over 15 min. The mixture was stirred at the temperature for 1 h, diluted with water, washed twice with toluene, acidified (pH=1) with hydrochloric acid and extracted with ethyl acetate. The extracts were washed with water and brine, dried and concentrated. An excess diazomethane solution in ether was added to a solution of the residue in ethyl acetate (20 ml) with cooling in ice. The mixture was concentrated and purified by silica gel chromatography (hexane-ethyl acetate, 85:15) to give a compound (2) (3.32 g; yield 85%).

[0178] Process 2

[0179] 10% Palladium-carbon (0.32 g) was added to a solution of compound (2) (3.22 g, 9.0 mmol) in methanol (30 ml). The mixture was stirred under a hydrogen atmosphere for 17 h, filtered and concentrated to give a compound (3) (2.05 g; yield 100%)

[0180] Process 3

[0181] 5-(2-Thienylthio)thiophene-2-carboxylic acid (233 mg, 0.96 mmol) and 1-hydroxybenzotriazole (10.8 mg, 0.08 mmol) were added to a solution of compound (3) (180 mg, 0.80 mmol) in THF (8 ml) and 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide (149 mg, 0.96 mmol) under cooling in ice. The mixture was stirred at room temperature for 14 h, diluted with ethyl acetate, washed with dilute hydrochloric acid, aq. sodium hydrogencarbonate successively, dried and concentrated. The residue was purified by silica gel chromatography (hexane-ethyl acetate, 5:1) to give a compound (I-5A-59b) (325 mg; yield 90%).

[0182] Process 4

[0183] 1N aq. lithium hydroxide (1.8 ml, 1.8 mmol) was added to a solution of compound (I-5A-59b) (325 mg, 0.72 mmol) in THF (8 ml). The mixture was stirred at room temperature for 14 h, acidified and extracted with ethyl acetate. The extracts were washed with water and brine, successively, dried and concentrated to give a compound (I-5A-59a) (300 mg; yield 96%).

Example 2

[0184] Preparation of Compound (I-7M-1a), (I-7N-1a), (I-7N-1b) 556

[0185] Methyl bis(2,2,2-trifluoroethyl)phosphonoacetate (2.94 ml, 13.92 mmol) and 18-crown-6 (5.52 g, 20.88 mmol) in THF (100 ml) were cooled at −60° C. A solution of potassium bis(trimethylsilyl)amide (0.5 M toluene solution, 27.8 ml, 13.9 mmol) was added. The mixture was stirred for 15 h. A solution of compound (4) (2.0 g, 6.96 mmol) in THF (20 ml) was added dropwise during 15 min. The mixture was stirred at the same temperature for 2 h. The temperature was raised to 0° C. and the mixture was diluted with water and extracted with ethyl acetate. The extracts were washed with water and brine, successively, dried, concentrated and purified by silica gel chromatography (hexane-ethyl acetaqte, 5:1) to give a compound (5) (2.10 g; yield 88%).

[0186] Process 2

[0187] Diisopropylaluminum hydride (1M toluene solution, 13.1 ml, 13.1 mmol) was added dropwise to a solution of compound (5) (1.80 g, 5.24 mmol) in dichloromethane (20 ml)-hexane (20 ml) at −78° C. The mixture was stirred at the temperature for 1 h. Methanol (1 ml) was added. The mixture was warmed to the room temperature. 2N Hydrochloric acid was added. The mixture was extracted with ethyl acetate. The extracts were washed with sodium hydrogencarbonate and brine successively, dried, concentrated and purified by silica gel chromatography (hexane-ethyl acetate, 7:3) to give a compound (6) (5.92 g; yield 96%).

[0188] Process 3

[0189] A mixture of compound (6) (1.58 g, 5.01 mmol), t-butyl bromoacetate (1.05 ml, 6.50 mmol), tetrabutylammonium hydrogensulfate (170 mg, 0.5 mmol) and 50% sodium hydroxide (4 ml) were vigorously stirred at room temperature for 18 h. The phase of toluene was separated, washed with water and brine successively, dried and concentrated. The residue obtained, trifluoroacetic acid (6.38 ml, 83 mmol) and anisole (3.37 ml. 31 mmol) were stirred at 60° C. for 15 h and concentrated under a reduced pressure. The residue was washed with hexane. Methanol (20 ml) and conc. sulfuric acid (0.44 ml) were added. The mixture was heated under reflux for 2 h. 2N sodium hydroxide was added to be alkaline. The mixture was extracted with ethyl acetate. The extracts were washed with water and brine successively, dried and concentrate to give a compound (7) (461 mg; yield 44%).

[0190] Process 4

[0191] 5-(2-Methyl-1-pyrrolylsulfonyl)thiophene-2-carboxylic acid (21.8 mg, 0.85 mmol) and 1-hydroxybenzotriazole (13 mg, 0.09 mmol) were added to a solution of compound (7) (215 mg, 0.85 mmol) in THF (6 ml). 1-Ethyl-3-(3-dimethylaminopropyl)-carbodiimide (137 mg, 1.02 mmol) was further added under cooling in ice. The mixture was stirred at room temperature for 16 h, diluted with ethyl acetate, washed with dilute hydrochloric acid and sodium hydrogencarbonate successively, dried and concentrated. The residue was purified by silica gel chromatography (hexane-ethyl acetate 2:1) to give a compound (I-7N-1b) (328 mg; yield 78%).

[0192] Process 5

[0193] 1 N Sodium hydroxide solution (1.57 ml, 1.57 mmol) was added to a solution of compound (I-7N-1b) (310 mg, 0.63 mmol) in THF (3.2 ml)-methanol (6.3 ml) and the mixture was stirred at room temperature 16 h. 2N Hydrochloric acid was added to acidify and the mixture was extracted with ethyl acetate. The extracts were washed with water and brine successively, dried and concentrated to give a compound (I-7N-1a) (399 mg; yield 73%).

[0194] Process 6

[0195] 10% Palladium-carbon (170 mg, 0.36 mmol) was added to a solution of compound (1-7N-1a) (170 mg, 0.36 mmol) in methanol (5 ml). The mixture was stirred under a hydrogen atmosphere for 17 h and filtered. The filtrate was concentrated to give a compound (I-7M-1a) (162 mg; yield 95%).

Example 3

Preparation of Compounds (I-7I-55a), (II-7I-55b)

[0196] 557

[0197] Potassium t-butoxide (6.73 g, 60.0 mmol) was added to a suspension of 2-(1,3-dioxolan-2-yl)ethyltriphenylphosphonium bromide (13.28 g, 30.0 mmol) in THF (60 ml) at −30° C. The mixture was stirred at −30° C. to 0° C. for 1 h. A solution of compound (8) (5.62 g, 20.0 mmol) in THF (40 ml) was added dropwise at −25° C. during 15 min. The mixture was warmed to 0° C., stirred for 1.5 h, diluted with water and extracted with ethyl acetate. The extracts were washed with water and brine, dried and concentrated. The residue was purified by silica gel chromatography (hexane-ethyl acetate 85:15) to give a compound (9) (6.27 g, yield 86%)

[0198] Process 2

[0199] 10% Palladium-carbon (0.21 g) was added to a solution of compound (9) (4.10 g, 11.2 mmol) in methanol (41 ml). The mixture was stirred under a hydrogen atmosphere for 2 h and filtered. The filtrate was concentrated to give a residue. Pydidinium p-toluenesulfonate (503 mg, 2.0 mmol) was added to a solution of the residue in acetone-water (4:1, 50 ml). The mixture was heated under reflux for 16 h, diluted with water and extracted with ethyl acetate. The extracts were washed with water and brine, dried and concentrated. A mixture of the residue and methyl (triphenylphosphoraniliden)acetate (2.93 g, 8.76 mmol) in toluene (35 ml) was stirred at room temperature for 18 h, diluted with ethyl acetate, washed with water and brine and concentrated. The residue was purified by silica gel chromatography in (hexane-ethyl acetate 35:15) to give a compound (10) (2.71 g; yield 71%).

[0200] Process 3

[0201] Trifluoroacetic acid (3.82 ml, 49.5 mmol) was added to a solution of compound (10) (2.35 g, 6.19 mmol) in dicholoromethane (38 ml) and the mixture was stirred at room temperature for 3 h and concentrated under a reduced pressure. The residue was dissolved in toluene (50 ml) and water (10 ml). 2N Sodium hydroxide was added to be alkaline in the aq. layer. The toluene phase was separated, washed with water and brine, dried and concentrated to give a compound (11) (1.70 g; yield 98%).

[0202] Process 4

[0203] 1-Ethyl-3-(3-dimethylaminopropyl)-carbodiimide (252 mg, 1.62 mmol) was added to a mixture of a compound (11) (433 mg, 1.55 mmol), 5-(2-methyl-1-pyrrolylsulfonyl)thiophen-2-carboxylic acid (400 mg, 1.47 mmol) and 1-hydroxybenzotriazole (20 mg, 0.15 mmol) in THF (6 ml) with cooling in ice. The mixture was stirred at room temperature for 16 h, diluted with ethyl acetate, washed with dilute hydrochloric acid and aq. sodium hydrogencarbonate successively, dried and concentrated. The residue was purified by silica gel chromatography (hexane-ethyl acetate, 4:1) to give a product (II-7I-55b) (585 mg; yield 74%).

[0204] Process 5

[0205] 2N Lithium hydroxide (1.58 ml, 3.15 mmol) was added to a solution of compound (II-7I-55b) (560 mg, 1.05 mmol) in THF (8 ml). A mixture was stirred at room temperature for 48 h, acidified with 2N Hydrochloric acid and extracted with ethyl acetate. The extracts were washed with water and brine successively, dried and concentrated. The residue was purified by silica gel chromatography (hexane-ethyl acetate, 1:3) to give a compound (II-7I-55a) (399 mg; yield 73%).

Example 4

[0206] Preparation of Compounds (I-7A-1e), (I-7E-1e) 558

[0207] Oxalyl chloride (0.236 ml, 2.71 mmol) and N,N-dimethylformamide (a drop) were added to a solution compound (12) (840 mg, 2.26 mmol) in dichloromethane (20 ml) with cooling in ice. The mixture was stirred for 30 min and concentrated under a reduced pressure. The residue was dissolved in dichloromethane (20 ml). Methanesulfonamide (258 mg, 2.71 mmol) and 1,8-diazabicyclo[5.4.0]-7-undecene (0.744 ml, 4.97 mmol) were added. The mixture was stirred for 2.5 h, diluted with ethyl acetate, washed with dilute hydrochloric acid, aq. sodium hydrogencarbonate and brine successively, dried and concentrated. Trifluoroacetic acid (25 ml) and anisole (2 ml, 18.40 mmol) were added to the residue. The mixture was stirred at 50° C. for 13 h and concentrated under a reduced pressure. The oily residue was washed with hexane to give a compound (13) (0.776 g; yield 65%).

[0208] Process 2

[0209] Oxalyl chloride (0.081 ml, 0.929 mmol) and N,N-dimethylformamide (a drop) were added to a solution 5-(1-pyrrolylsulfonyl)thiophene-2-carboxylic acid (209 mg, 0.812 mmol) in dichloromethane (4 ml) with cooling in ice. The mixture was stirred for 20 min and at room temperature for 40 min and concentrated under a reduced pressure. The residue was dissolved in dichloromethane (4 ml). A solution of compound (13) (0.42, 0.774 mmol) in dichloromethane (4 ml)-THF (3 ml) and triethylamine (0.486 ml, 3.49 mmol) were added to the solution with cooling in ice. The mixture was stirred for 1.5 h and at room temperature for 19 h, diluted with ethyl acetate, washed with dilute hydrochloric acid, aq. sodium hydrogencarbonate and brine successively, dried and concentrated. The residue was purified by silica gel chromatography (hexane-ethyl acetate-acetic acid, 1:1:0.003) to give a compound (I-7E-1e) (157 mg; yield 37%).

[0210] Process 3

[0211] 20% Palladium hydroxide-carbon (64 mg) was added to a solution of compound (I-7E-1e) (116 mg, 0.21 mmol) in methanol (3 ml). The mixture was stirred under a hydrogen atmosphere for 20 h and filtered. The filtrate was concentrated to give a compound (I-7A-1e) (109 mg; yield 94%).

Example 5

[0212] Preparation of Compound (Formula: X3—X2—X1—COOH) 559

[0213] 5-Bromothiophene-2-sulfonyl chloride was reacted directly with a pyrrole derivative or the acid chloride was converted to the sulfonamide followed by condensation with 2,5-dimethoxytetrahydro-derivative to give a sulfonylpyrrole derivative. Then, the product was converted to the organolithium or the organomagnesium compound by a halogen-metal exchange reaction, followed by reacting with carbon dioxide to give a desired compound.

[0214] 5-(1-Pyrrolylsulfonyl)-2-thiophenecarboxylic acid

[0215] mp 191-194° C.; 1H-NMR (CDCl3) δ6.36 (2H, t, J=2.4 Hz), 7.18 (2H, t, J=2.4 Hz), 7.61 (1H, d, J=4.2 Hz), 7.74 (1H, d, J=4.2 Hz). ps 5-(2-Methyl-1-pyrrolylsulfonyl)-2-thiophenecarboxylic acid

[0216] mp 159-160° C.; 1H-NMR (CDCl3) δ2.40 (3H, d, J=0.9 Hz), 6.01 (1H, m), 6.23 (1H, t, J=3.0 Hz), 7.20 (1H, dd, J=1.8, 3.6 Hz), 7.58 (1H, d, J=4.2 Hz), 7.76 (1H, d, J=4.2 Hz).

[0217] 5-(2,5-Dimethyl-1-pyrrolylsulfonyl)-2-thiophenecarboxylic acid

[0218] mp 167-171° C.; 1H-NMR (CDCl3) δ2.43 (6H, s), 5.90 (2H, s), 7.52 (1H, d, J=3.9 Hz), 7.75 (1H, d, J=3.9 Hz).

[0219] The structure and physical property of the compound prepared in accordance with the above examples are shown below. Each sign used for —X1—X2—X3 and A in Tables means the sign represented before.

TABLE 1
560
	Compd. No..	—X1—X2—X3	A	R
	I-4A-1a	1	4A	CO2H
	I-4B-1a	1	4B	CO2H
	I-4C-1a	1	4C	CO2H
	I-4D-1a	1	4D	CO2H
	I-4E-1a	1	4E	CO2H
	I-4F-1a	1	4F	CO2H
	I-5A-1a	1	5A	CO2H
	I-5A-1b	1	5A	CO2Me
	I-5A-31a	31	5A	CO2H
	I-5A-47a	47	5A	CO2H
	I-5A-55a	55	5A	CO2H
	I-5A-59a	59	5A	CO2H
	I-5A-59b	59	5A	CO2Me
	I-5A-80a	80	5A	CO2H
	I-5A-88a	88	5A	CO2H
	I-5A-88b	88	5A	CO2Me
	I-5A-104a	104	5A	CO2H
	I-5A-126a	126	5A	CO2H
	I-5A-143a	143	5A	CO2H
	I-5A-197a	197	5A	CO2H
	I-5B-1a	1	5B	CO2H
	I-5B-47a	47	5B	CO2H
	I-5B-59a	59	5B	CO2H
	I-5C-1a	1	5C	CO2H
	I-5C-1b	1	5C	CO2Me
	I-5C-55a	55	5C	CO2H
	I-5C-31a	31	5C	CO2H
	I-5C-47a	47	5C	CO2H
	I-5C-88a	88	5C	CO2H
	I-5D-1a	1	5D	CO2H
	I-5E-1a	1	5E	CO2H
	I-5E-55a	55	5E	CO2H
	I-5F-1a	1	5F	CO2H
	I-5F-47a	47	5F	CO2H
	I-5G-47a	47	5G	CO2H
	I-6A-1a	1	6A	CO2H
	I-6A-31a	31	6A	CO2H
	I-6A-55a	55	6A	CO2H
	I-6A-88a	88	6A	CO2H
	I-6B-1a	1	6B	CO2H
	I-6B-31a	31	6B	CO2H
	I-6B-88a	88	6B	CO2H
	I-6C-1a	1	6C	CO2H

[0220]

TABLE 2
561
Compd. No..	—X1—X2—X3	A	R
I-6D-1a	1	6D	CO2H
I-6E-1a	1	6E	CO2H
I-6E-59a	59	6E	CO2H
I-6F-1a	1	GE	CO2H
I-6G-1a	1	6G	CO2H
I-7A-1a	1	7A	CO2H
I-7A-1b	1	7A	CO2Me
I-7A-1c	1	7A	CONH2
I-7A-1e	1	7A	CONHSO2Me
I-7A-1h	1	7A	CH2OH
I-7A-1i	1	7A	CH2OMe
I-7A-31a	31	7A	CO2H
I-7A-47a	47	7A	CO2H
I-7A-47i	47	7A	CH2OMe
I-7A-55a	55	7A	CO2H
I-7A-59a	59	7A	CO2H
I-7A-80a	80	7A	CO2H
I-7A-88a	88	7A	CO2H
I-7A-88e	88	7A	CONHSO2Me
I-7A-88h	88	7A	CH2OH
I-7A-88i	88	7A	CH2OMe
I-7A-104a	104	7A	CO2H
I-7A-143a	143	7A	CO2H
I-7A-197a	197	7A	CO2H
I-7A-315a	315	7A	CO2H
I-7A-316a	316	7A	CO2H
I-7B-1a	1	7B	CO2H
I-7C-1a	1	7C	CO2H
I-7D-1a	1	7D	CO2H
I-7E-1c	1	7E	CONH2
I-71-1d	1	7E	CONHMe
I-71-1c	1	7E	CONHSO2Me
I-71-1f	1	7E	CON(Me)SO2Me
I-7E-1g	1	7E	5-tetrazolyl
I-7E-1h	1	7E	CH2OH
I-71-1i	1	7E	CH2OMe
I-71-47c	47	7E	CONH2
I-71-47i	47	7E	CH2OMe
I-7E-88e	88	7E	CONHSO2Me
I-7E-88h	88	7E	CH2OH
I-71-88i	88	71	CH2OMe
I-7F-1a	1	7F	CO2H

[0221]

TABLE 3
562
Compd. No..	—X1—X2—X3	A	R
I-7F-31a	31	7F	CO2H
I-7F-47a	47	7F	CO2H
I-7F-88a	88	7F	CO2H
I-7F-143a	143	7F	CO2H
I-7G-1a	1	7G	CO2H
I-7G-88a	88	7G	CO2H
I-7G-126a	126	7G	CO2H
I-7I-1a	1	7H	CO2H
I-7I-1a	1	7I	CO2H
I-7I-1b	1	7I	CO2Me
I-7I-1c	1	7I	CONH2
I-7I-1e	1	7I	CONHSO2Me
I-7I-31a	31	7I	CO2H
I-7I-47a	47	7I	CO2H
I-7I-55a	55	7I	CO2H
I-7I-59a	59	7I	CO2H
I-7I-80a	80	7I	CO2H
I-7I-88a	88	7I	CO2H
I-7I-93a	93	7I	CO2H
I-7I-126a	126	7I	CO2H
I-7I-143a	143	7I	CO2H
I-7I-197a	197	7I	CO2H
I-7I-270a	270	7I	CO2H
I-7I-307a	307	7I	CO2H
I-7I-327a	327	7I	CO2H
I-7I-332a	332	7I	CO2H
I-7I-343a	343	7I	CO2H
I-7I-385a	385	7I	CO2H
I-7I-389a	389	7I	CO2H
I-7I-391a	391	7I	CO2H
I-7J-1a	1	7J	CO2H
I-7J-31a	31	7J	CO2H
I-7K-1a	1	7K	CO2H
I-7K-47a	47	7K	CO2H
I-7K-59a	59	7K	CO2H
I-7K-143a	143	7K	CO2H
I-7L-1a	1	7L	CO2H
I-7M-1a	1	7M	CO2H
I-7M-1b	1	7M	CO2Me
I-7M-1c	1	7M	CONH2
I-7M-1e	1	7M	CONHSO2Me
I-7M-31a	31	7M	CO2H
I-7M-40a	40	7M	CO2H

[0222]

TABLE 4
563
Compd. No..	—X1—X2—X3	A	R
I-7M-43a	43	7M	CO2H
I-7M-47a	47	7M	CO2H
I-7M-55a	55	7M	CO2H
I-7M-59a	59	7M	CO2H
I-7M-80a	80	7M	CO2H
I-7M-88a	88	7M	CO2H
I-7M-88e	88	7M	CONHSO2Me
I-7M-88h	88	7M	CH2OH
I-7M-88i	88	7M	CH2OMe
I-7M-104a	104	7M	CO2H
I-7M-126a	126	7M	CO2H
I-7M-143a	143	7M	CO2H
I-7M-197a	197	7M	CO2H
I-7M-270a	270	7M	CO2H
I-7M-307a	307	7M	CO2H
I-7M-315a	315	7M	CO2H
I-7M-316a	316	7M	CO2H
I-7M-317a	317	7M	CO2H
I-7M-318a	318	7M	CO2H
I-7M-327a	327	7M	CO2H
I-7M-329a	329	7M	CO2H
I-7M-330a	330	7M	CO2H
I-7M-331a	331	7M	CO2H
I-7M-332a	332	7M	CO2H
I-7M-333a	333	7M	CO2H
I-7M-334a	334	7M	CO2H
I-7M-336a	336	7M	CO2H
I-7M-337a	337	7M	CO2H
I-7M-342a	342	7M	CO2H
I-7M-343a	343	7M	CO2H
I-7M-385a	385	7M	CO2H
I-7M-389a	389	7M	CO2H
I-7M-390a	390	7M	CO2H
I-7M-391a	391	7M	CO2H
I-7M-392a	392	7M	CO2H
I-7M-393a	393	7M	CO2H
I-7M-396a	396	7M	CO2H
I-7M-412a	412	7M	CO2H
I-7M-424a	424	7M	CO2H
I-7M-446a	446	7M	CO2H
I-7M-447a	447	7M	CO2H
I-7M-448a	448	7M	CO2H
I-7N-1a	1	7N	CO2H

[0223]

TABLE 5
564
Compd. No..	—X1—X2—X3	A	R
I-7N-1b	1	7N	CO2Me
I-7N-55a	55	7N	CO2H
I-7N-88a	88	7N	CO2H
I-7N-143a	148	7N	CO2H
I-70-1a	1	7O	CO2H
I-7P-1a	1	7P	CO2H
I-7P-1e	1	7P	CONHSO2Me
I-7Q-1a	1	7Q	CO2H
I-7R-1a	1	7R	CO2H
I-7R-59a	59	7R	CO2H
I-7R-88a	88	7R	CO2H
I-7R-270a	270	7R	CO2H
I-7R-307a	307	7R	CO2H
I-7S-1a	1	7S	CO2H
I-7T-1a	1	7T	CO2H
I-8A-1a	1	8A	CO2H
I-8A-47a	47	8A	CO2H
I-8A-88a	88	8A	CO2H
I-8B-1a	1	8B	CO2H
I-8B-47a	47	8B	CO2H
I-8B-88a	88	8B	CO2H
I-8C-1a	1	8C	CO2H
I-8C-88a	88	8C	CO2H
I-9A-1a	1	9A	CO2H
I-9A-47a	47	9A	CO2H
I-9A-88a	88	9A	CO2H
I-9B-1a	1	9B	CO2H
I-9B-47a	47	9B	CO2H
I-9B-88a	88	9B	CO2H

[0224]

TABLE 6
565
	Compd. No..	—X1—X2—X3	A	R
	II-4A-55a	55	4A	CO2H
	II-4B-55a	55	4B	CO2H
	II-4C-55a	55	4C	CO2H
	II-4D-55a	55	4D	CO2H
	II-4E-55a	55	4E	CO2H
	II-4F-SSa	55	4F	CO2H
	II-5A-1a	1	5A	CO2H
	II-5A-1b	1	5A	CO2Me
	II-5A-31a	31	5A	CO2H
	II-5A-47a	47	SA	CO2H
	II-5A-55a	55	5A	CO2H
	II-5A-55c	55	5A	CONH2
	II-5A-55g	55	5A	5-tetrazolyl
	II-5A-59a	59	SA	CO2H
	II-5A-80a	80	SA	CO2H
	II-5A-88a	88	SA	CO2H
	II-5A-88b	88	5A	CO2Me
	II-5A-104a	104	5A	CO2H
	II-5A-126a	126	SA	CO2H
	II-5A-143a	143	SA	CO2H
	II-5A-197a	197	5A	CO2H

[0225]

TABLE 7
566
	Compd. No..	—X1—X2—X3	A	R
	Il-5B-1a	1	5B	CO2H
	II-5B-47a	47	5B	CO2H
	II-5B-55a	55	5B	CO2H
	II-5C-1a	1	5C	CO2H
	II-5C-1b	1	5C	CO2Me
	II-5C-55a	55	5C	CO2H
	II-5C-88a	88	5C	CO2H
	II-5D-1a	1	5D	CO2H
	II-5E-1a	1	5E	CO2H
	II-5E-55a	55	5E	CO2H
	II-5F-31a	31	5F	CO2H
	II-5F-47a	47	5F	CO2H
	II-5F-55a	55	5F	CO2H
	II-5F-88a	88	5F	CO2H
	II-5G-47a	47	5G	CO2H
	Il-6A-1a	1	6A	CO2H
	II-6A-31a	31	6A	CO2H
	II-6A-55a	55	6A	CO2H
	II-6A-88a	88	6A	CO2H
	Il-6B-1a	1	6B	CO2H
	II-6B-31a	31	6B	CO2H
	II-6B-55a	55	6B	CO2H
	II-6B-88a	88	6B	CO2H

[0226]

TABLE 8
567
	Compd. No..	—X1—X2—X3	A	R
	II-6C-31a	31	6C	CO2H
	Il-6D-1a	1	6D	CO2H
	II-6E-1a	1	6E	CO2H
	II-6E-59a	59	6E	CO2H
	II-6F-1a	1	6F	CO2H
	II-6G-1a	1	6G	CO2H
	II-7A-1a	1	7A	CO2H
	II-7A-1b	1	7A	CO2Me
	II-7A-1c	1	7A	CONH2
	II-7A-31a	31	7A	CO2H
	II-7A-47a	47	7A	CO2H
	II-7A-55a	55	7A	CO2H
	II-7A-55e	55	7A	CONHSO2Me
	II-7A-55g	55	7A	5-tetrazolyl
	II-7A-59a	59	7A	CO2H
	II-7A-80a	80	7A	CO2H
	II-7A-88a	88	7A	CO2H
	II-7A-88e	88	7A	CONHSO2Me
	II-7A-88h	88	7A	CH2OH
	II-7A-88i	88	7A	CH2OMe
	II-7A-104a	104	7A	CO2H
	II-7A-143a	143	7A	CO2H
	II-7A-197a	197	7A	CO2H
	II-7A-315a	315	7A	CO2H
	II-7A-316a	316	7A	CO2H
	II-7B-55a	55	7B	CO2H
	II-7C-1a	1	7C	CO2H
	II-7D-1a	1	7D	CO2H
	II-7E-1c	1	7E	CONH2
	II-7E-1d	1	7E	CONHMe
	II-7E-1e	1	7E	CONHSO2Me
	II-7E-1f	1	7E	CON(Me)SO2Me
	II-7E-1g	1	7E	5-tetrazolyl
	II-7E-1h	1	7E	CH2OH
	II-7E-1i	1	7E	CH2OMe
	II-7E-47c	47	7E	CONH2
	II-7E-55c	55	7E	CONH2
	II-7E-55e	55	7E	CONHSO2Me
	II-7E-55g	55	7E	5-tetrazolyl
	II-7E-88e	88	7E	CONHSO2Me
	II-7E-88h	88	7E	CH2OH
	II-7E-88i	88	7E	CH2OMe
	II-7F-1a	1	7F	CO2H

[0227]

TABLE 9
568
	Compd. No..	—X1—X2—X3	A	R
	II-7F-47a	47	7F	CO2H
	II-7F-55a	55	7F	CO2H
	II-7F-88a	88	7F	CO2H
	I1-7F-143a	143	7F	CO2H
	II-7G-1a	1	7G	CO2H
	II-7H-1a	1	7H	CO2H
	II-7I-1a	1	7I	CO2H
	II-7I-1b	1	7I	CO2Me
	II-7I-1c	1	7I	CONH2
	II-7I-1e	1	7I	CONHSO2Me
	II-7I-31a	31	7I	CO2H
	I1-7I-47a	47	7I	CO2H
	1I-7I-55a	55	7I	CO2H
	II-7I-55b	55	7I	CO2Me
	II-7I-59a	59	7I	CO2H
	II-7I-80a	80	7I	CO2H
	II-7I-88a	88	7I	CO2H
	II-7I-104a	104	7I	CO2H
	II-7I-126a	126	7I	CO2H
	II-7I-197a	197	7I	CO2H
	II-7I-239a	239	7I	CO2H
	II-7I-270a	270	7I	CO2H
	II-7I-327a	327	7I	CO2H
	II-7I-332a	332	7I	CO2H
	II-7I-343a	343	7I	CO2H
	II-7I-389a	389	7I	CO2H
	II-7I-391a	391	7I	CO2H
	II-7J-1a	1	7I	CO2H
	II-7J-55a	55	7I	CO2H
	II-7K-1a	1	7K	CO2H
	II-7K-47a	47	7K	CO2H
	II-7K-55a	55	7K	CO2H
	II-7K-59a	59	7K	CO2H
	II-7K-143a	143	7K	CO2H
	II-7L-1a	1	7L	CO2H
	II-7L-55a	55	7L	CO2H
	II-7M-1a	1	7M	CO2H
	II-7M-1b	1	7M	CO2Me
	II-7M-1c	1	7M	CONH2
	II-7M-1e	1	7M	CONHSO2Me
	II-7M-1k	1	7M	CONHSO2Ph
	II-7M-31a	31	7M	CO2H
	II-7M-40a	40	TM	CO2H

[0228]

TABLE 10
569
	Compd. No..	—X1—X2—X3	A	R
	II-7M-43a	43	7M	CO2H
	II-7M-47a	47	7M	CO2H
	II-7M-55a	55	7M	CO2H
	II-7M-59a	59	7M	CO2H
	II-7M-80a	80	7M	CO2H
	II-7M-88a	88	7M	CO2H
	II-7M-88e	88	7M	CONHSO2Me
	II-7M-88h	88	7M	CH2OH
	II-7M-88i	88	7M	CH2OMe
	II-7M-104a	104	7M	CO2H
	II-7M-126a	126	7M	CO2H
	II-7M-143a	143	7M	CO2H
	II-7M-197a	197	7M	CO2H
	II-7M-239a	239	7M	CO2H
	II-7M-270a	270	7M	CO2H
	II-7M-307a	307	7M	CO2H
	II-7M-327a	327	7M	CO2H
	II-7M-329a	329	7M	CO2H
	II-7M-330a	330	7M	CO2H
	II-7M-331a	331	7M	CO2H
	II-7M-332a	332	7M	CO2H
	II-7M-333a	333	7M	CO2H
	II-7M-334a	334	7M	CO2H
	II-7M-336a	336	7M	CO2H
	II-7M-343a	343	7M	CO2H
	II-7M-385a	385	7M	CO2H
	II-7M-389a	389	7M	CO2H
	II-7M-390a	390	7M	CO2H
	II-7M-391a	391	7M	CO2H
	II-7M-392a	392	7M	CO2H
	II-7M-393a	393	7M	CO2H
	II-7N-1a	1	7N	CO2FI
	II-7N-55a	55	7N	CO2H
	II-7N-88a	88	7N	CO2H
	II-7N-143a	143	7N	CO2H
	II-70-55a	55	7O	CO2H
	II-7P-55a	55	7P	CO2H
	II-7P-55e	55	7P	CONHSO2Me
	II-7P-55j	55	7P	CONHSO2CF3
	II-7Q-1a	1	7Q	CO2H
	II-7Q-55a	55	7Q	CO2H
	II-7R-55a	55	7R	CO2H
	II-7R-88a	88	7R	CO2H

[0229]

TABLE 11
570
	Compd. No..	—X1—X2—X3	A	R
	II-7R-270a	270	7R	CO2H
	II-7S-1a	1	7S	CO2H
	II-7S-47a	47	7S	CO2H
	II-7S-55a	55	7S	CO2H
	II-7T-55a	55	7T	CO2H
	II-7U-31a	31	7U	CO2H
	II-7U-55a	55	7U	CO2H
	II-7U-88a	88	7U	CO2H
	II-7V-55a	55	7V	CO2H
	II-8A-1a	1	8A	CO2H
	II-8A-47a	47	8A	CO2H
	II-8A-88a	88	8A	CO2H
	II-8B-1a	1	8B	CO2H
	II-8B-47a	47	8B	CO2H
	II-8B-88a	88	8B	CO2H
	II-8C-55a	55	8C	CO2H
	II-8C-88a	88	8C	CO2H
	II-9A-1a	1	9A	CO2H
	II-9A-47a	47	9A	CO2H
	II-9A-88a	88	9A	CO2H
	II-9B-1a	1	9B	CO2H
	II-9B-47a	47	9B	CO2H
	II-9B-88a	88	9B	CO2H

[0230]

TABLE 12
571
	Compd. No..	—X1—X2—X3	A	R
	III-5A-1a	1	5A	CO2H
	III-5A-47a	47	5A	CO2H
	III-5A-55a	55	5A	CO2H
	III-5A-80a	80	5A	CO2H
	III-7A-1a	1	7A	CO2H
	III-7A-47a	47	7A	CO2H
	III-7A-55a	55	7A	CO2H
	III-7A-80a	80	7A	CO2H

[0231]

TABLE 13
572
	Compd. No..	—X1—X2—X3	A	R
	IV-5A-1a	1	5A	CO2H
	IV-5A-47a	47	5A	CO2H
	IV-7A-1a	1	7A	CO2H
	IV-7A-47a	47	7A	CO2H

[0232]

TABLE 14
573
	Compd. No..	—X1—X2—X3	A	R
	V-5A-88a	88	5A	CO2H
	V-7A-88a	88	7A	CO2H

[0233]

TABLE 15
574
	Compd. No..	—X1—X2—X3	A	R
	VI-6A-1a	1	6A	CO2H
	VI-6A-31a	31	6A	CO2H
	VI-6A-40a	40	6A	CO2H
	VI-6A-47a	47	6A	CO2H
	VI-6A-55a	55	6A	CO2H
	VI-6A-80a	80	6A	CO2H
	VI-6A-88a	88	6A	CO2H
	VI-6A-104a	104	6A	CO2H
	VI-6A-122a	122	6A	CO2H
	VI-6A-123a	123	6A	CO2H
	VI-6A-124a	124	6A	CO2H
	VI-6A-133a	133	6A	CO2H

[0234]

TABLE 16
575
	Compd. No..	—X1—X2—X3	A	R
	VII-6A-1a	1	6A	CO2H
	VII-6A-47a	47	6A	CO2H
	VII-6A-88a	88	6A	CO2H

[0235]

TABLE 17
Compd.
No..     Physical property
I-4B-1a  1                  H-NMR(CD3OD) δ 1.24-2.33(11H, m), 2.46(1H, m),
         3.69-3.76(2H, m), 6.11(1H, dt, J=7.8and33.3Hz),
         6.36(2H, m), 7.23(2H, m), 7.71(2H, m), 8.54(1H, br);
         IR(CHCl3)3442, 2877, 1741, 1657, 1529, 1504, 1456,
         1383, 1167, 1076, 1057, 1036cm−1; [α]D25+37.7±0.7°
         (c=1.05, MeOH)
I-4E-1a  1                  H-NMR(CDCl3) δ 1.26-1.76(7H, m), 2.10(1H, m), 2.47
         (1H, m), 3.35(1H, dd, J=8.4and9.0Hz), 3.58(1H, dd, J=
         6.3and8.4Hz), 3.98(1H, d, J=16.2Hz), 4.08(1H, m),
         4.13(1H, d, J=16.2Hz), 6.27(1H, d, J=8.1Hz), 6.34
         (2H, d, J=4.8Hz), 7.15(2H, d, J=4.8Hz), 7.37(1H, d,
         J=4.2Hz), 7.58(1H, d, J=4.2Hz); IR(CHCl3)3440,
         2958, 2879, 1753, 1734, 1655, 1533, 1508, 1477, 1456,
         1427, 1383, 1315, 1167, 1122, 1057, 1034cm−1; [α]D24+
         41.7±0.8°(c=1.00, CHCl3)Anal.(C19H22N2O6S2·0.6H2O)
         Calcd.(%): C, 50.79; H, 5.20; N, 6.23; S, 14.27Found(%):
         C, 50.76; H, 5.00; N, 6.26; S, 14.09
I-4F-1a  mp126-128°C.; 1H-NMR(CD3OD) δ 1.26-1.66(8H, m),
         2.03(1H, m), 2.48(1H, m), 2.57(1H, m), 3.76(1H, m),
         5.69(1H, dt, J=8.1and21.3Hz), 6.36(2H, m), 7.23
         (2H, m), 7.72(2H, m), 8.53(1H, d, J=5.4Hz); IR
         (CHCl3)3417, 3322, 2958, 2877, 1730, 1653, 1535, 1508,
         1456, 1427, 1379, 1302, 1167, 1128, 1057, 1036cm−1;
         [α]D25+68.3±1.0°(c=1.04, MeOH)Anal.
         (C20H21FN2O5S2·0.9H2O)Calcd.(%): C, 51.52; H, 4.90; N,
         5.98; F, 4.05; S, 13.68Found(%): C, 51.46; H, 4.62; N,
         5.72; F, 3.72; S, 12.93
I-5A-1a  1                  H-NMR(CDCl3) δ 1.02(1H, m), 1.23-1.44(8H, m),
         1.54-1.65(4H, m), 2.00(1H, m), 2.29-2.36(2H, m), 2.49
         (1H, brs), 3.80(1H, m), 6.17(1H, d, J=7.5Hz), 6.33-6.34
         (2H, m), 7.15-7.16(2H, m), 7.35(1H, d, J=3.9Hz),
         7.55(1H, d, J=3.9Hz); IR(CHCl3)3516, 3442, 1709,
         1658, 1529, 1504, 1456, 1383, 1192, 1167, 1057, 1034cm−1;
         [α]D27+48.7±0.9°(c=1.006, MeOH)Anal.
         (C21H26N2O5S2)Calcd.(%): C, 55.98; H, 5.82; N, 6.22; S,
         14.23Found(%): C, 56.10; H, 5.81; N, 6.08; S, 13.77
I-5A-31a 1                  H-NMR(CDCl3) δ 0.95(1H, m), 1.16-1.70(12H, m), 1.97
         (1H, m), 2.32(2H, t, J=7.2Hz), 2.48(1H, m), 3.81(1H,
         m), 4.14(2H, s), 5.83(1H, d, J=6.6Hz), 6.77(1H, d, J=
         3.3Hz), 7.21-7.37(6H, m); IR(CHCl3)3514, 3446, 3427,
         1709, 1643, 1543, 1506, 1456cm−1; [α]D24.0+46.9±0.9°
         (c=1.011, MeOH)Anal.(C24H29NO3S·0.5H2O)Calcd.(%):
         C, 68.54; H, 7.19; N, 3.33; S, 7.62Found(%): C, 68.62;
         H, 7.03; N, 3.47; S, 7.54

[0236]

TABLE 18
Compd.
No..     Physical property
I-5A-47a 1                  H-NMR(CDCl3) δ 1.03(1H, m), 1.18-1.70(12H, m), 1.98
         (1H, m), 2.32(2H, dt, J=8.1, 2.1Hz), 2.50(1H, m), 3.81
         (1H, m), 6.19(1H, d, J=7.8Hz), 7.11
         (1H, dd, J=5.1, 3.9Hz),
         7.39(1H, d, J=3.9Hz), 7.61(1H, d, J=3.9Hz),
         7.70(1H, dd, J=5.1, 1.2Hz), 7.75(1H, dd, J=3.9, 1.2Hz);
         IR(CHCl3)3512, 3442, 3375, 2679, 1709, 1655,
         1529, 1504, 1402, 1336, 1153, 1095, 1022cm−1; [α]D24.0+
         48.6±0.9°(c=1.009, MeOH)Anal.
         (C21H25NO5S3·0.2H2O)Calcd.(%): C, 53.53; H, 5.43; N,
         2.97; S, 20.41Found(%): C, 53.56; H, 5.32; N, 2.92; S,
         20.17
I-5A-55a 1                  H-NMR(CDCl3) δ 1.02(1H, m), 1.25-1.48(8H, m),
         1.55-1.66(4H, m), 2.01(1H, m), 2.32
         (2H, dt, J=2.1, 7.5Hz),
         2.38(3H, s), 2.50(1H, brs), 3.80(1H, m), 5.99(1H,
         m), 6.07(1H, brd, J=5.7Hz), 6.20(1H, t, J=3.3Hz),
         7.18(1H, dd, J=1.8, 3.3Hz), 7.35(1H, d, J=3.9Hz),
         7.54(1H, d, J=3.9Hz); IR(CHCl3)3514, 3442, 3149,
         3101, 1709, 1657, 1529, 1504, 1375, 1182, 1161, 1053cm−1;
         [α]D24+47.1±0.9°(c=1.003, MeOH)Anal.
         (C22H28N2O5S2)Calcd.(%): C, 56.87; H, 6.07; N, 6.03; S,
         13.80Found(%): C, 56.59; H, 6.06; N, 5.91; S, 13.52
I-5A-59a 1                  H-NMR(CDCl3) δ 0.97(1H, m), 1.16-1.68(12H, m), 1.98
         (1H, d, J=3.9Hz), 2.31(2H, t, J=7.5Hz), 2.47(1H, m),
         3.79(1H, m), 5.86(1H, d, J=4.5Hz), 7.01(1H, dd, J=
         5.4, 3.6Hz), 7.04(1H, d, J=3.6Hz), 7.28(1H, dd, J=
         3.6, 1.2Hz), 7.31(1H, d, J=3.6Hz), 7.42(1H, dd, J=
         5.4, 1.2Hz); IR(CHCl3)3516, 3444, 3425, 2671, 1709,
         1645, 1531, 1498, 1421cm−1; [α]D25.0+49.1±0.9°(c=1.003,
         MeOH)Anal.(C21H25NO3S3·0.1H2O)Calcd.(%): C, 57.66;
         H, 5.81; N, 3.20; S, 21.99Found(%): C, 57.47; H, 5.81;
         N, 3.23; S, 22.21
I-5A-59b 1                  H-NMR(CDCl3) δ 0.96(1H, m), 1.16-1.66(12H, m), 1.98
         (1H, d, J=3.6Hz), 2.27(2H, dt, J=7.2, 1.8Hz), 2.49
         (1H, m), 3.62(3H, s), 3.77(1H, m), 5.85(1H, d, J=6.9Hz),
         7.01(1H, dd, J=5.4, 3.6Hz), 7.04(1H, d, J=4.2Hz),
         7.29(1H, dd, J=3.6, 1.2Hz), 7.31(1H, d, J=4.2Hz),
         7.43(1H, dd, J=5.4, 1.2Hz)
I-5A-88a 1                  H-NMR(CDCl3) δ 0.96(1H, m), 1.16-1.70(12H, m), 1.99
         (1H, d, J=3.6Hz), 2.32(2H, t, J=7.5Hz), 2.50(1H, m),
         3.82(1H, m), 4.16(2H, s), 5.85(1H, d, J=8.1Hz), 6.79
         (1H, d, J=3.6Hz), 6.96(1H, dd, J=5.1, 1.5Hz), 7.05
         (1H, m), 7.28(1H, dd, J=5.1, 3.0Hz), 7.35(1H, d, J=
         3.6Hz); IR(CHCl3)3516, 3446, 3427, 1709, 1641, 1545,
         1506, 1458cm−1; [α]D24.0+44.9±0.9°(c=1.003, MeOH)
         Anal.(C22H27NO3S2·0.1H2O)Calcd.(%): C, 63.00; H, 6.54;
         N, 3.34; S, 15.29Found(%): C, 63.06; H, 6.53; N, 3.43; S,
         15.01

[0237]

TABLE 19
Compd.
No..      Physical property
I-5A-104a 1                  H-NMR(CDCl3) δ 0.99(1H, m), 1.18-1.70(12H, m), 1.99
          (1H, m), 2.33(2H, t, J=7.5Hz), 2.50(1H, m), 3.82(1H,
          m), 4.10(2H, s), 5.88(1H, d, J=8.4Hz), 6.70(1H, d, J=
          3.6Hz), 6.95(1H, dd, J=5.4, 3.6Hz), 7.04(1H, dd, J=
          3.6, 1.2Hz), 7.28(1H, d, J=3.6Hz), 7.36(1H, dd, J=5.4,
          1.2Hz); IR(CHCl3)3514, 3446, 2669, 1709, 1643, 1543,
          1506, 1458cm−1; [α]D25.0+44.5±1.3°
          (c=0.670, MeOH)Anal.
          (C22H27NO3S3·0.2H2O)Calcd.(%): C, 58.30; H, 6.09; N,
          3.09; S, 21.22Found(%): C, 58.34; H, 6.09; N, 3.25; S,
          21.10
I-5A-143a 1                  H-NMR(CDCl3) δ 1.01(1H, m), 1.16-1.72(12H, m), 2.00
          (1H, m), 2.33(2H, t, J=7.5Hz), 2.57(1H, m), 3.93(1H,
          m), 4.24(2H, s), 6.03(1H, d, J=7.5Hz), 7.18-7.34(6H, m),
          7.42(1H, t, J=7.8Hz), 7.80
          (1H, s), 8.17(1H, d, J=7.8Hz);
          IR(CHCl3)3514, 3438, 1709, 1651, 1516, 1495cm−1;
          [α]D24.0+41.4±0.8°(c=1.000, MeOH)Anal.(C28H31NO3S·
          0.3H2O)Calcd.(%): C, 72.01; H, 6.82; N, 3.00; S, 6.87
          Found(%): C, 72.05; H, 6.81; N, 3.02; S, 6.75
I-5A-197a 1                  H-NMR(CDCl3) δ 0.96(1H, m), 1.18-1.68(12H, m), 1.97
          (1H, d, J=3.9Hz), 2.32(2H, t, J=7.5Hz), 2.48(1H, m),
          3.22(2H, t, J=8.7Hz), 3.80(1H, m), 4.07(2H, s), 4.57
          (2H, t, J=8.7Hz), 5.83(1H, d, J=7.8Hz), 6.79(1H, t, J=
          7.5Hz), 6.81(1H, d, J=3.9Hz), 6.97(1H, d, J=7.5Hz),
          7.09(1H, d, J=7.5Hz), 7.33(1H, d, J=3.9Hz); IR
          (CHCl3)3516, 3446, 3427, 2679, 1709, 1641, 1543, 1506,
          1458cm−1; [α]D25.0+14.7±0.5°
          (c=1.009, MeOH)Anal.
          (C26H31NO4S·0.6H2O)Calcd.(%): C, 67.24; H, 6.99; N, 3.01;
          S, 6.90Found(%): C, 67.14; H, 6.85; N, 3.03; S, 6.64
I-5B-1a   1                  H-NMR(CDCl3) δ 1.08-1.70(7H, m),
          2.04(1H, m), 2.10-2.18
          (2H, m), 2.53(1H, brs), 3.14(1H, d, J=6.0Hz), 3.81
          (1H, m), 5.52-5.67(2H, m), 6.25
          (1H, d, J=6.9Hz), 6.33-6.34
          (2H, m), 7.14-7.16(2H, m), 7.35(1H, d, J=3.9Hz),
          7.54(1H, d, J=3.9Hz); IR(CHCl3)3512, 3440, 1712,
          1658, 1531, 1504, 1456, 1383, 1192, 1167, 1057, 1034cm−1;
          [α]D27+61.4±1.0°(c=1.008, MeOH)Anal.
          (C21H24N2O5S2·0.3H2O)Calcd.(%): C, 55.56; H, 5.46; N,
          6.17; S, 14.13Found(%): C, 55.47; H, 5.42; N, 6.54; S,
          14.26
I-5C-1a   mp149-152°C.; 1H-NMR(CDCl3) δ 1.07(1H, m),
          1.24-1.32(2H, m), 1.41-1.48(2H, m),
          1.53-1.69(4H, m), 2.01(1H, m),
          2.23-2.30(2H, m), 2.49(1H, brs), 3.87(1H, m), 5.78(1H, d,
          J=15.6Hz), 6.15(1H, d, J=7.2Hz), 6.33-6.34(2H, m),
          7.02(1H, dt, J=15.6and7.2Hz), 7.15-7.17(2H, m), 7.37
          and7.56(each1H, eachd, eachJ=4.2Hz); IR(CHCl3)
          3523, 3440, 2679, 1695, 1655, 1529, 1504, 1456, 1383,
          1192, 1167, 1057, 1034cm−1; [α]D24+38.7±0.8°(c=1.001,
          MeOH)Anal.(C21H24N2O5S2·0.2H2O)Calcd.(%): C, 55.78;
          H, 5.44; N, 6.20; S, 14.18Found(%): C, 55.70; H, 5.36; N,
          6.20; S, 14.08

[0238]

TABLE 20
Compd.
No..     Physical property
I-5C-31a 1                  H-NMR(CDCl3) δ 0.99(1H, m), 1.22-1.29(2H, m),
         1.42-1.49(2H, m), 1.53-1.69(4H, m), 1.99(1H, m),
         2.18-2.33(2H, m), 2.49(1H, brs), 3.88(1H, m), 4.14(2H,
         s), 5.79(1H, d, J=15.6Hz), 5.85(1H, d, J=7.8Hz), 6.78
         (1H, d, J=3.6Hz), 7.03(1H, dt, J=6.9and15.6Hz),
         7.23-7.33(5H, m), 7.36(1H, d, J=3.6Hz); IR(CHCl3)
         3523, 3446, 3427, 2679, 1695, 1649, 1543, 1506, 1456,
         1308, 1282cm−1; [α]D24+41.2±0.8°
         (c=1.011, MeOH)
         Anal.(C24H27NO3S·0.2H2O)Calcd.(%): C, 69.77; H, 6.68;
         N, 3.39; S, 7.76Found(%): C, 69.72; H, 6.55; N, 3.40; S,
         7.65
I-5C-47a 1                  H-NMR(CDCl3) δ 1.09(1H, m), 1.25-1.31(2H, m),
         1.42-1.47(2H, m), 1.56-1.64(4H, m), 2.00(1H, m),
         2.24-2.31(2H, m), 2.49(1H, brs), 3.88(1H, m), 5.78(1H,
         d, J=15.6Hz), 6.25(1H, d, J=8.1Hz), 7.02(1H, dt, J=
         15.6and6.8Hz), 7.12(1H, dd, J=3.6and4.8Hz), 7.42
         and7.61(each1H, eachd, eachJ=3.9Hz), 7.70(1H, dd,
         J=1.5and4.8Hz), 7.75(1H, dd, J=1.5and3.6Hz); IR
         (CHCl3)3523, 3440, 3373, 2681, 1695, 1653, 1529, 1504,
         1335, 1402, 1153, 1095, 1020cm−1;
         [α]D24+39.1±0.8°
         (c=1.000, MeOH)Anal.
         (C21H33NO5S3·0.3H2O)Calcd.(%):
         C, 53.55; H, 5.05; N, 2.97; S, 20.42Found(%): C, 53.58;
         H, 4.97; N, 3.04; S, 20.17
I-5C-88a 1                  H-NMR(CDCl3) δ 1.00(1H, m), 1.23-1.30(2H, m),
         1.43-1.48(2H, m), 1.53-1.69(4H, m), 2.00(1H, m),
         2.19-2.33(2H, m), 2.50(1H, brs), 3.88(1H, m), 4.16(2H,
         s), 5.79(1H, dt, J=15.6and1.5Hz),
         5.90(1H, d, J=8.1Hz),
         6.79(1H, d, J=3.6Hz), 6.95-7.08(3H, m), 7.28(1H,
         dd, J=2.7and4.8Hz), 7.36(1H, d, J=3.6Hz); IR
         (CHCl3)3523, 3446, 3427, 2679, 1695, 1649, 1543, 1506,
         1458, 1284cm−1; [α]D24+39.9±0.8°
         (c=1.011, MeOH)
         Anal.(C24H27NO3S·0.2H2O)Calcd.(%): C, 63.04; H, 6.11;
         N, 3.34; S, 15.30Found(%): C, 63.12; H, 5.96; N, 3.44; S,
         15.22
I-5D-1a  mp150-152°C.; 1H-NMR(CDCl3) δ 1.32-1.66(6H, m),
         1.96(1H, m), 2.12-2.46(5H, m), 2.61(1H, brs), 3.87
         (1H, m), 5.28(1H, m), 5.41(1H, dd, J=9.6, 10.5Hz),
         6.33(2H, t, J=2.4Hz), 6.68(1H, br d, J=7.2Hz), 7.15
         (2H, t, J=2.4Hz), 7.44(1H, d, J=3.9Hz), 7.48(1H, d, J=
         3.9Hz); IR(CHCl3)3510, 3390, 3145, 3101, 2673,
         1709, 1655, 1531, 1506, 1456, 13811192, 1167, 1057,
         1034cm−1; [α]D25+9.2±0.5°
         (c=1.011, MeOH)Anal.
         (C21H24N2O5S2)Calcd.(%): C, 56.23; H, 5.39; N, 6.25; S,
         14.30Found(%): C, 56.20; H, 5.44; N, 6.23; S, 14.23

[0239]

TABLE 21
Compd.
No..     Physical property
I-5E-1a  mp155-159°C.; 1H-NMR(CDCl3) δ 1.18-1.82(9H, m),
         2.00(1H, m), 2.61(1H, m), 3.50-3.59(2H, m), 3.79(1H,
         m), 3.99and4.10(each1H, Abq, J=17.1Hz), 5.54-5.70
         (2H, m), 6.32-6.34(2H, m), 6.47(1H, d, J=6.3Hz),
         7.14-7.17(2H, m), 7.39(1H, d, J=4.2Hz), 7.54(1H, d, J=
         4.2Hz); IR(CHCl3)3423, 1764, 1730, 1655, 1531,
         1506, 1456, 1383, 1192, 1167, 1057cm−1; [α]D23+
         28.9±0.7°(c=1.011, MeOH)Anal.(C20H26N2O6S2)
         Calcd.(%): C, 53.08; H, 5.35; N, 6.19; S, 14.17Found(%):
         C, 53.44; H, 5.62; N, 6.00; S, 13.70
I-6A-1a  mp109-111°C.; 1H-NMR(CDCl3) δ 1.02(1H, m),
         1.24-1.56
         (14H, m), 1.98(1H, brs), 2.29(2H, t, J=7.2Hz),
         2.48(1H, brs), 3.79(1H, m), 6.28(1H, d, J=7.2Hz),
         6.33(2H, t, J=2.4Hz), 7.15(2H, t, J=2.4Hz), 7.38 and
         7.55(each1H, eachd, eachJ=4.2Hz); IR(KBr)3352,
         1709, 1624, 1541, 1512, 1456, 1377, 1192, 1167, 1057,
         1036cm−1; [α]D24.5+47.7±0.9°
         (c=1.003, MeOH)Anal.
         (C22H28N2O5S2·0.2H2O)Calcd.(%): C, 56.44; H, 6.11; N,
         5.98; S, 13.70Found(%): C, 56.50; H, 6.11; N, 6.18; S,
         13.51
I-6B-1a  1                  H-NMR(CDCl3) δ 1.08(1H, m), 1.21-1.31(2H, m),
         1.40-1.45(2H, m), 1.58-1.66(2H, m), 2.03-2.19(3H, m),
         2.32-2.46(4H, m), 2.52(1H, brs), 3.80(1H, m), 5.33-5.45
         (2H, m), 6.24(1H, d, J=7.8Hz), 6.32-6.34(2H, m),
         7.15-7.16(2H, m), 7.36(1H, d, J=3.9Hz), 7.55(1H, d, J=
         3.9Hz); IR(CHCl3)3514, 3440, 1711, 1657, 1531,
         1504, 1456, 1383, 1192, 1167, 1057, 1034cm−1; [α]D24.5+
         69.8±1.1°(c=1.006, MeOH)Anal.
         (C22H26N2O5S2·0.2H2O)Calcd.(%): C, 56.68; H, 5.71; N,
         6.01; S, 13.76Found(%): C, 56.67; H, 5.70; N, 6.14; S,
         13.89
I-6B-31a 1                  H-NMR(CDCl3) δ 1.04(1H, m), 1.17-1.28(2H, m),
         1.41-1.46(2H, m), 1.55-1.66(2H, m), 2.00(1H, m),
         2.04-2.24(2H, m), 2.31-2.44(4H, m), 2.51(1H, brs), 3.82
         (1H, m), 4.13(2H, s), 5.32-5.44(2H, m), 5.96(1H, d, J=
         6.6Hz), 6.76(1H, dt, J=3.6and0.9Hz), 7.22-7.35(5H,
         m), 7.36(1H, d, J=3.6Hz); IR(CHCl3)3514, 3444,
         3427, 2671, 1711, 1643, 1545, 1506, 1454, 1309, 1279cm−1;
         [α]D24+67.7±1.1°(c=1.002, MeOH)Anal.
         (C25H29NO3S)Calcd.(%): C, 70.89; H, 6.90; N, 3.31; S,
         7.57Found(%): C, 70.67; H, 6.95; N, 3.36; S, 7.42
I-6D-1a  1                  H-NMR(CDCl3) δ 1.26-1.34(2H, m), 1.43-1.48(2H, m),
         1.55-1.76(4H, m), 1.96-2.13(4H, m),
         2.32(2H, t, J=7.2Hz),
         2.59(1H, br s), 3.92(1H, m), 5.28-5.44(2H, m), 6.33
         (2H, t, J=2.1Hz), 6.69(1H, br d, J=6.6Hz), 7.15(2H,
         t, J=2.1Hz), 7.39(1H, d, J=4.2Hz), 7.53(1H, d, J=
         4.2Hz); IR(CHCl3)3512, 3368, 1706, 1654, 1532, 1506,
         1455, 1382, 1212, 1132, 1106, 1075, 1016cm−1; Anal.
         (C22H26N2O5S2)Calcd.(%): C, 57.12; H, 5.67; N, 6.06; S,
         13.86Found(%): C, 56.91; H, 5.71; N, 6.18; S, 13.75

[0240]

TABLE 22
Compd.
No..     Physical property
I-7A-1a  mp114-117°C.;
         1                  H-NMR(CDCl3) δ 1.05(1H, m), 1.18-1.70
         (16H, m), 2.00(1H, m), 2.32(2H, t, J=6.9Hz), 2.49
         (1H, m), 3.80(1H, m), 6.05(1H, d, J=7.2Hz), 6.32-6.35
         (2H, m), 7.15-7.18(2H, m), 7.35(1H, d, J=3.9Hz), 7.57
         (1H, d, J=3.9Hz); IR(CHCl3)3442, 1708, 1657, 1529,
         1504, 1456, 1383, 1192, 1167, 1057, 1034cm−1; [α]D24+
         45.9±0.9°(c=1.004, MeOH)Anal.(C23H30N2O5S2)
         Calcd.(%): C, 57.72; H, 6.32; N, 5.85; S, 13.40Found
         (%): C, 57.56; H, 6.44; N, 5.82; S, 13.11
I-7A-1e  1                  H-NMR(CDCl3) δ 1.01(1H, m), 1.29-1.67(16H, m), 1.99
         (1H, m), 2.30(2H, t, J=7.2Hz), 2.45(1H, m), 3.28(3H,
         s), 3.84(1H, m), 6.14(1H, d, J=7.8Hz), 6.34(2H, d, J=
         4.5Hz), 7.16(2H, d, J=4.5Hz), 7.40(1H, d, J=3.9Hz),
         7.58(1H, d, J=3.9Hz); IR(CHCl3)3386, 2954, 2929,
         2877, 2858, 1720, 1651, 1531, 1506, 1456, 1425, 1398,
         1385, 1342, 1167, 1076, 1067, 1034cm−1; [α]D25+
         38.5±0.8°(c=1.01, MeOH)Anal.
         (C24H33N3O6S3·0.8MeOH)Calcd.(%): C, 51.24; H, 6.28; N,
         7.23; S, 16.55Found(%): C, 51.59; H, 6.17; N, 7.40; S,
         16.22
I-7A-1h  mp134-136°C.;
         1                  H-NMR(CDCl3) δ 0.97(1H, m), 1.28-1.69
         (18H, m), 2.01(1H, m), 2.49(1H, brs), 3.61(2H, t, J=
         6.6Hz), 3.81(1H, m), 6.05(1H, d, J=7.8Hz), 6.33-6.35
         (2H, m), 7.16-7.17(2H, m), 7.35and7.57(each1H,
         eachd, eachJ=3.9Hz); IR(Nujol)3357, 3244, 1621,
         1554, 1371, 1186, 1169, 1061, 1038cm−1; [α]D24+
         47.8±0.9°(c=1.005, MeOH)Anal.
         (C23H32N2O4S2·0.2AcOEt)Calcd.(%): C, 59.27; H, 7.02;
         N, 5.81; S, 13.30Found(%): C, 59.53; H, 7.09; N, 5.92; S,
         13.29
I-7A-1i  mp82-84°C.;
         1                  H-NMR(CDCl3) δ 0.95(1H, m), 1.26-1.65
         (18H, m), 2.01(1H, m), 2.49(1H, brs), 3.32(3H, s), 3.34
         (2H, t, J=6.6Hz), 3.80(1H, m), 5.97(1H, d, J=7.5Hz),
         6.33-6.34(2H, m), 7.16-7.17(2H, m), 7.33and7.58(each
         1H, eachd, eachJ=3.9Hz); IR(CHCl3)3442, 1658,
         1529, 1504, 1456, 1385, 1192, 1167, 1113, 1057, 1034cm−1;
         [α]D25+43.9±0.8°(c=1.003, MeOH)Anal.
         (C24H34N2O4S2)Calcd.(%): C, 60.22; H, 7.16; N, 5.85; S,
         13.40Found(%): C, 60.27; H, 7.14; N, 5.79; S, 13.29
I-7A-31a 1                  H-NMR(CDCl3) δ 0.92(1H, m), 1.18-1.66(16H, m), 1.96
         (1H, m), 2.31(2H, t, J=7.5Hz), 2.48(1H, m), 3.81(1H,
         m), 4.13(2H, s), 5.83(1H, d, J=8.1Hz), 6.77(1H, d, J=
         3.9Hz), 7.21-7.36(6H, m); IR(CHCl3)3516, 3446, 3427,
         1709, 1643, 1543, 1506, 1456cm−1;
         [α]D24.0+41.0±0.8°
         (c=1.006, MeOH)Anal.(C26H33NO3S·0.2H2O)Calcd.(%):
         C, 70.46; H, 7.60; N, 3.16; S, 7.23Found(%): C, 70.43;
         H, 7.66; N, 3.21; S, 7.07

[0241]

TABLE 23
Compd.
No..     Physical property
I-7A-47a 1                  H-NMR(CDCl3) δ 0.98(1H, m), 1.16-1.70(16H, m), 1.99
         (1H, m), 2.31(2H, t, J=7.5Hz), 2.49(1H, m), 3.80(1H,
         m), 6.05(1H, d, J=7.8Hz), 7.10(1H, dd, J=4.8, 3.6Hz),
         7.39(1H, d, J=3.9Hz), 7.64(1H, d, J=3.9Hz), 7.69(1H,
         dd, J=4.8, 1.2Hz), 7.75(1H, dd, J=3.6, 1.2Hz); IR
         (CHCl3)3514, 3442, 3375, 2677, 1709, 1655, 1529, 1504,
         1402, 1336, 1153, 1095, 1022cm−1;
         [α]D24.0+45.7±0.9°
         (c=1.010, MeOH)Anal.(C23H29NO5S3·0.2H2O)Calcd.(%):
         C, 55.33; H, 5.94; N, 2.80; S, 19.26Found(%): C, 55.42; H,
         6.04; N, 2.86; S, 19.03
I-7A-47i 1                  H-NMR(CDCl3) δ 0.96(1H, m),
         1.26-1.35(11H, m), 1.40-1.46
         (2H, m), 1.51-1.67(5H, m), 2.01(1H, m), 2.50(1H,
         brs), 3.32(3H, s), 3.34(2H, t, J=6.9Hz), 3.80(1H, m),
         6.03(1H, d, J=7.5Hz), 7.11(1H, dd, J=3.9and4.8Hz),
         7.38and7.65(each1H, eachd, eachJ=3.9Hz), 7.70(1H,
         dd, J=1.5and4.8Hz), 7.76(1H, dd, J=1.5and3.9Hz);
         IR(CHCl3)3442, 1657, 1529, 1504, 1402, 1336, 1153, 1113,
         1095, 1020cm−1; [α]D25+43.7±0.8°
         (c=1.008, MeOH)Anal.
         (C24H33NO4S3·0.1H2O)Calcd.(%): C, 57.94; H, 6.73; N,
         2.82; S, 19.34Found(%): C, 57.81; H, 6.68; N, 2.90; S,
         19.42
I-7A-59a 1                  H-NMR(CDCl3) δ 0.93(1H, m), 1.16-1.68(16H, m), 1.98
         (1H, d, J=3.6Hz), 2.31(2H, t, J=7.2Hz), 2.47(1H, m),
         3.78(1H, m), 5.87(1H, d, J=7.5Hz), 7.00(1H, dd, J=5.7,
         3.9Hz), 7.04(1H, d, J=3.6Hz),
         7.28(1H, dd, J=3.9, 1.2Hz),
         7.31(1H, d, J=3.6Hz), 7.42(1H, dd, J=5.7, 1.2Hz);
         IR(CHCI3)3516, 3444, 3427, 2671, 1709, 1645, 1529, 1498,
         1421cm−1; [δ ]D25.0+41.2±0.8°
         (c=1.003, MeOH)Anal.
         (C23H29NO3S3)Calcd.(%): C, 59.58; H, 6.30; N, 3.02; S,
         20.75Found(%): C, 59.70; H, 6.27; N, 3.03; S, 20.56
I-7A-88a 1                  H-NMR(CDCl3) δ 0.93(1H, m), 1.16-1.68(16H, m), 1.98
         (1H, d, J=3.6Hz), 2.31(2H, t, J=7.5Hz), 2.49(1H, m),
         3.81(1H, m), 4.15(2H, s), 5.86(1H, d, J=7.5Hz), 6.79
         (1H, d, J=3.6Hz), 6.96(1H, dd, J=4.8, 1.2Hz), 7.05(1H,
         dd, J=3.0, 1.2Hz), 7.28(1H, dd, J=4.8, 3.0Hz), 7.35(1H,
         d, J=3.6Hz); IR(CHCl3)3516, 3446, 3427, 1709, 1641,
         1545, 1506, 1458cm−1; [α]D24.0+40.2±0.8°
         (c=1.007, MeOH)
         Anal.(C24H31NO3S2·0.1H2O)Calcd.(%): C, 64.42; H, 7.03;
         N, 3.13; S, 14.33Found(%): C, 64.52; H, 7.00; N, 3.18; S,
         14.04
I-7A-88h mp92-93°C.; 1H-NMR(CDCl3) δ 0.94(1H, m), 1.20-1.34
         (11H, m), 1.42-1.47(2H, m), 1.48-1.63(5H, m), 1.98(1H,
         m), 2.49(1H, brs), 3.61(2H, t, J=6.6Hz), 3.83(1H, m),
         4.16(2H, s), 5.86(1H, d, J=8.1Hz), 6.79(1H, d, J=
         3.6Hz), 6.97(1H, dd, J=1.2and4.8Hz), 7.06(1H, m), 7.29
         (1H, dd, J=3.0and4.8Hz), 7.35(1H, d, J=3.6Hz); IR
         (Nujol)3315, 3259, 1599, 1549, 1527, 1317cm−1; [α]D24+
         45.0±0.9°(c=1.001, MeOH)Anal.(C24H33NO2S2)
         Calcd.(%): C, 66.78; H, 7.71; N, 3.24; S, 14.86Found(%):
         C, 66.85; H, 7.71; N, 3.37; S, 14.57

[0242]

TABLE 24
Compd.
No..      Physical property
I-7A-88i  mp47-48°C.; 1H-NMR(CDCl3) δ 0.93(1H, m),
          1.23-1.32
          (11H, m), 1.41-1.46(2H, m), 1.51-1.63(5H, m), 1.98(1H,
          m), 2.50(1H, brs), 3.31(3H, s), 3.34(2H, t, J=6.6Hz),
          3.81(1H, m), 4.16(2H, s), 5.81(1H, d, J=7.2Hz), 6.79
          (1H, d, J=3.9Hz), 6.97(1H, dd, J=0.9and4.8Hz), 7.06
          (1H, m), 7.29(1H, dd, J=3.0and4.8Hz), 7.34(1H, d, J=
          3.9Hz); IR(CHCl3)3446, 3426, 1643, 1543, 1506, 1460,
          1113cm−1; [α]D25.5+43.0±0.8°
          (c=1.008, MeOH)Anal.
          (C25H35NO2S2)Calcd.(%): C, 67.37; H, 7.92; N, 3.14; S,
          14.39Found(%): C, 67.32; H, 7.91; N, 3.19; S, 14.32
I-7A-104a 1                  H-NMR(CDCl3) δ 0.95(1H, m), 1.18-1.70(16H, m), 2.00
          (1H, d, J=3.6Hz), 2.32(2H, t, J=7.5Hz), 2.50(1H, m),
          3.82(1H, m), 4.10(2H, s), 5.87(1H, d, J=7.2Hz), 6.70
          (1H, d, J=3.6Hz), 6.95(1H, dd, J=5.4, 3.6Hz), 7.04(1H,
          dd, J=3.6, 1.2Hz),
          7.28(1H, d, J=3.6Hz), 7.36(1H, dd, J=
          5.4, 1.2Hz); IR(CHCl3)3516, 3446, 3427, 2671, 1709,
          1643, 1543, 1506, 1458cm−1;
          [α]D25.0+39.4±0.8°.(c=1.004,
          MeOH)Anal.(C24H31NO3S3)Calcd.(%): C, 60.34; H, 6.54;
          N, 2.93; S, 20.14Found(%): C, 60.12; H, 6.51; N, 3.05; S,
          19.95
I-7A-143a 1                  H-NMR(CDCl3) δ 0.97(1H, m), 1.16-1.70(16H, m), 2.00
          (1H, m), 2.31(2H, t, J=7.5Hz), 2.58(1H, m), 3.93(1H,
          m), 4.24(2H, s), 6.01(1H, d, J=7.2Hz), 7.18-7.32(6H, m),
          7.42(1H, t, J=7.8Hz), 7.80(1H, s),
          8.18(1H, d, J=7.2Hz);
          IR(CHCl3)3516, 3438, 1709, 1651, 1516, 1495cm−1;
          [α]D24.0+41.9±0.8°(c=1.006, MeOH)Anal.
          (C30H35NO3S·
          0.2H2O)Calcd.(%): C, 73.05; H, 7.23; N, 2.84; S, 6.50
          Found(%): C, 73.10; H, 7.13; N, 2.86; S, 6.39
I-7A-197a 1                  H-NMR(CDCl3) δ 0.93(1H, m), 1.18-1.68(16H, m), 1.97
          (1H, d, J=3.9Hz), 2.31(2H, t, J=7.5Hz), 2.48(1H, m),
          3.22(2H, t, J=9.0Hz), 3.81(1H, m), 4.07(2H, s), 4.57
          (2H, t, J=9.0Hz), 5.82(1H, d, J=7.5Hz), 6.79(1H, t, J=
          7.2Hz), 6.80(1H, d, J=7.2Hz), 6.96(1H, d, J=7.2Hz),
          7.09(1H, d, J=7.2Hz), 7.33(1H, d, J=7.2Hz); IR
          (CHCl3)3516, 3446, 3427, 2671, 1709, 1641, 1543, 1506,
          1458cm−1; [α]D25.0+37.9±0.8°
          (c=1.003, MeOH)Anal.
          (C28H35NO4S·0.3H2O)Calcd.(%): C, 69.05; H, 7.39; N, 2.88;
          S, 6.58Found(%): C, 69.11; H, 7.24; N, 2.99; S, 6.61
I-7A-315a 1                  H-NMR(CDCl3) δ 1.00(1H, m), 1.23-1.63(16H, m), 2.00
          (1H, m), 2.31(2H, t, J=7.2Hz), 2.58(1H, m), 3.94(1H,
          m), 4.26(2H, s), 6.06(1H, d, J=7.8Hz), 7.00-7.18(5H, m),
          7.42(1H, m), 7.82(1H, s), 8.18(1H, d, J=7.2Hz);
          IR(CHCl3)3516, 3438, 2954, 2927, 2875, 2856, 1709, 1653,
          1516, 1492, 1456, 1396, 1298, 1271cm−1;
          [α]D25.5+39.0±0.8°
          (c=1.04, MeOH)Anal.(C30H34FNO3S·0.5MeOH)Calcd.(%):
          C, 69.95; H, 6.93; N, 2.67; F, 3.63; S, 6.12Found(%): C,
          70.24; H, 6.80; N, 2.98; F, 3.19; S, 6.08

[0243]

TABLE 25
Compd.
No..      Physical property
I-7A-316a 1                  H-NMR(CDCl3) δ 0.98(1H, m), 1.22-1.63(16H, m), 2.00
          (1H, m), 2.31(2H, t, J=7.5Hz), 2.58(1H, m), 3.82(3H,
          s), 3.92(1H, m), 4.23(2H, s), 6.03(1H, d, J=8.1Hz),
          6.85-6.91(2H, m), 7.02-7.23(3H, m), 7.39(1H, m), 7.83
          (1H, s), 8.14(1H, d, J=8.4Hz); IR(CHCl3)3518, 3438,
          2954, 2929, 1709, 1653, 1601, 1516, 1493, 1464, 1439,
          1394, 1246cm−1; [α]D26.0+35.2±0.7°(c=1.03, MeOH)
          Anal.(C31H37NO4S·0.2H2O)Calcd.(%): C, 71.15; H, 7.20;
          N, 2.68; S, 6.13Found(%): C, 71.03; H, 7.35; N, 2.86; S,
          5.99
I-7B-1a   1                  H-NMR(CDCl3) δ 0.98-2.49(20H, m), 1.14(3H, d, J=
          6.9Hz), 3.80(1H, m), 6.05(1H, d, J=5.2Hz), 6.33(2H,
          d, J=4.2Hz), 7.16(2H, d, J=4.2Hz), 7.35(1H, m), 7.57
          (1H, m); IR(CHCl3)3442, 2954, 2929, 2877, 2858, 1705,
          1657, 1529, 1504, 1456, 1383, 1167, 1057, 1034cm−1;
          [α]D24.5+41.6±1.6°(c=0.50, CHCl3)Anal.
          (C24H32N2O5S2·0.4MeOH)Calcd.(%): C, 57.98; H, 6.70; N,
          5.54; S, 12.69Found(%): C, 58.27; H, 6.47; N, 5.50; S,
          12.33
I-7D-1a   1                  H-NMR(CDCl3) δ 0.98(1H, m), 1.22-2.33(17H, m), 2.48
          (1H, m), 3.79(1H, m), 4.92(1H, dt, J=6.0and44.1Hz),
          6.07(1H, d, J=7.2Hz), 6.33(2H, d, J=4.8Hz), 7.16
          (2H, d, J=4.8Hz), 7.36(1H, d, J=3.6Hz), 7.57(1H, d,
          J=3.6Hz); IR(CHCl3)3440, 2956, 2875, 1732, 1657,
          1531, 1504, 1456, 1383, 1167, 1057, 1034cm−1; [α]D25+
          30.2±0.7°(c=1.02, MeOH)Anal.
          (C23H29FN2O5S2·0.3MeOH)Calcd.(%): C, 55.28; H, 6.01;
          N, 5.53; F, 3.75; S, 12.67Found(%): C, 55.58; H, 6.14; N,
          5.61; S, 12.05
I-7E-1c   1                  H-NMR(CDCl3) δ 1.18-1.30(3H, m), 1.40-1.45(2H, m),
          1.57-1.82(5H, m), 1.95-2.28(6H, m), 2.54(1H, br s),
          3.75(1H, m), 5.26(1H, br), 5.30-5.46(2H, m), 5.89(1H,
          br), 6.33(2H, t, J=2.4Hz), 6.69(1H, br d, J=6.0Hz),
          7.17(2H, t, J=2.4Hz), 7.48(1H, d, J=3.9Hz), 7.57
          (1H, d, J=3.9Hz); IR(CHCl3)3527, 3485, 3442, 3411,
          3340, 1674, 1531, 1504, 1456, 1383, 1192, 1167, 1057,
          1034cm−1; [α]D24+79.9±1.2°(c=1.002, MeOH)Anal.
          (C23H29N3O4S2·0.3H2O)Calcd.(%): C, 57.43; H, 6.20; N,
          8.74; S, 13.33Found(%): C, 57.55; H, 6.50; N, 8.76; S,
          13.28
I-7E-1d   1                  H-NMR(CDCl3) δ 1.19-1.27(3H, m), 1.40-1.45(2H, m),
          1.56-1.82(5H, m), 1.97-2.20(6H, m), 2.56(1H, br s), 2.75
          (3H, d, J=4.8Hz), 3.73(1H, m), 5.29-5.42(2H, m), 5.90
          (1H, br), 6.33(2H, t, J=2.1Hz), 6.79(1H, br d, J=7.8Hz),
          7.16(2H, t, J=2.1Hz), 7.54and7.57(each1H,
          ABq, J=3.9Hz); [α]D24+76.1±1.2°(c=1.006, MeOH)
          Anal.(C24H31N3O4S2·0.3H2O)Calcd.(%): C, 58.23; H,
          6.43; N, 8.49; S, 12.95Found(%): C, 58.22; H, 6.64; N,
          8.45; S, 12.81

[0244]

TABLE 26
Compd.
No..    Physical property
I-7E-1e 1                  H-NMR(CDCl3) δ 1.16-2.24(13H, m), 2.32(2H, d, J=
        7.2Hz), 2.57(1H, m), 3.27(3H, s), 3.74(1H, m), 5.25-5.32
        (2H, m), 6.14(1H, d, J=7.5Hz), 6.35(2H, d, J=4.8Hz),
        7.18(2H, d, J=4.8Hz), 7.46(1H, d, J=3.9Hz),
        7.60(1H, d, J=3.9Hz), 9.96(1H, s); IR(CHCl3)2956,
        2879, 1716, 1645, 1533, 1506, 1456, 1385, 1342, 1167,
        1122, 1057, 1034cm−1; [α]D24+90.4±1.3°
        (c=1.00, CHCl3)
        Anal.(C24H31N3O6S3·0.8MeOH)Calcd.(%): C, 51.41; H,
        5.95; N, 7.25; S, 16.60Found(%): C, 51.77; H, 5.70; N,
        7.53; S, 16.22
I-7E-1f 1                  H-NMR(CDCl3) δ 1.07-2.19(13H, m), 2.51(1H, m), 2.58
        (2H, t, J=7.5Hz), 3.22(3H, s), 3.27(3H, s), 3.84(1H,
        m), 5.32-5.43(2H, m), 6.26(1H, d, J=7.8Hz), 6.33(2H,
        d, J=4.5Hz), 7.17(2H, d, J=4.5Hz), 7.39(1H, d, J=
        4.2Hz), 7.58(1H, d, J=4.2Hz); IR(CHCl3)3394, 2956,
        2877, 1699, 1655, 1531, 1504, 1456, 1381, 1354, 1167,
        1057, 1034cm−1; [α]D24.5+47.4±0.9°
        (c=1.00, CHCl3)
        Anal.(C25H33N3O6S3·0.2H2O)Calcd.(%): C, 52.55; H,
        5.89; N, 7.35; S, 16.84Found(%): C, 52.85; H, 5.81; N,
        7.26; S, 16.45
I-7E-1g 1                  H-NMR(CDCl3) δ 1.12-1.86(9H, m), 2.01-2.10(5H, m),
        2.55(1H, br s), 2.96-3.04(2H, m), 3.57(1H, m), 5.27-5.40
        (2H, m), 6.36(2H, t, J=2.1Hz), 7.17(2H, t, J=2.1Hz),
        7.46(1H, d, J=3.9Hz), 7.60(1H, d, J=3.9Hz); IR
        (CHCl3)3462, 3336, 1657, 1531, 1506, 1456, 1383, 1192,
        1167, 1057, 1036cm−1;
        [α]D25+74.0±1.1°(c=1.000,
        MeOH)Anal.(C23H28N6O3S2·0.4Et2O)Calcd.(%): C,
        55.72; H, 6.08; N, 15.85; S, 12.09Found(%): C, 55.45; H,
        6.10; N, 15.85; S, 11.84
I-7E-1h mp123-125°C.; 1H-NMR(CDCl3) δ 1.09(1H, m), 1.16-1.75
        (10H, m), 1.99-2.20(5H, m), 2.52(1H, brs), 3.63
        (2H, t, J=6.5Hz), 3.81(1H, m), 5.28-5.44(2H, m), 6.24
        (1H, d, J=7.2Hz), 6.33-6.34(2H, m), 7.15-7.17(2H, m),
        7.37and7.57(each1H, eachd, eachJ=3.9Hz); IR
        (Nujol)3388, 3255, 1618, 1552, 1373, 1190, 1163, 1057,
        1039cm−1; [α]D25+80.1±1.2°
        (c=1.014, MeOH)Anal.
        (C23H30N2O4S2)Calcd.(%): C, 59.71; H, 6.54; N, 6.06; S,
        13.86Found(%): C, 59.59; H, 6.50; N, 6.08; S, 13.82
I-7E-1i 1                  H-NMR(CDCl3) δ 1.06(1H, m), 1.19-1.31(2H, m),
        1.34-1.44(4H, m), 1.52-1.65(4H, m), 2.01-2.13(5H, m),
        2.53(1H, brs), 3.32(3H, s), 3.37(2H, t, J=6.3Hz), 3.82
        (1H, m), 5.28-5.44(2H, m), 6.15(1H, d, J=7.5Hz),
        6.32-6.34(2H, m), 7.15-7.17(2H, m), 7.35and7.57(each
        1H, eachd, eachJ=4.2Hz); IR(CHCl3)3442, 1658,
        1529, 1504, 1456, 1382, 1192, 1167, 1115, 1057, 1034cm−1;
        [α]D24+73.8±1.1°(c=1.006, MeOH)Anal.
        (C24H32N2O4S2·0.2H2O)Calcd.(%): C, 60.02; H, 6.80; N,
        5.83; S, 13.35Found(%): C, 60.09; H, 6.75; N, 5.79; S,
        13.19

[0245]

TABLE 27
Compd.
No..     Physical property
I-7E-47i 1                  H-NMR(CDCl3) δ 1.08(1H, m), 1.21-1.31(2H, m),
         1.21-1.31(2H, m), 1.37-1.46(4H, m), 2.01-2.13(5H, m),
         2.53(1H, brs), 3.32(3H, s), 3.37(2H, t, J=6.6Hz), 3.82
         (1H, m), 5.28-5.43(2H, m), 6.19(1H, d, J=7.2Hz), 6.19
         (1H, d, J=7.2Hz), 7.11(1H, dd, J=3.9and5.1Hz),
         7.39and7.63(each1H, eachd, eachJ=3.9Hz), 7.69
         (1H, dd, J=1.5and5.1Hz), 7.75
         (1H, dd, J=1.5and3.9Hz);
         IR(CHCl3)3442, 1657, 1529, 1504, 1402, 1336,
         1153, 1115, 1097, 1020cm−1; [α]D24+76.3±1.2°(c=1.011,
         MeOH)Anal.(C24H31NO4S3·0.5H2O)Calcd.(%): C, 57.34;
         H, 6.42; N, 2.79; S, 19.14Found(%): C, 57.25; H, 6.25;
         N, 2.83; S, 19.25
I-7E-88e 1                  H-NMR(CDCl3) δ 1.11-1.66(9H, m), 1.93-2.34(7H, m),
         2.59(1H, m), 3.24(3H, s), 3.70(1H, m), 4.17(2H, s),
         5.21-5.31(2H, m), 5.92(1H, d, J=9.6Hz), 6.84(1H, d,
         J= 3.6Hz), 6.98(1H, dd, J=1.5and4.8Hz), 7.08(1H,
         dd, J=1.2and1.8Hz), 7.30(1H, m),
         7.50(1H, d, J=3.6Hz),
         10.78(1H, s); IR(CHCl3)3444, 3425, 2954, 2877,
         1714, 1630, 1545, 1510, 1456, 1408, 1342, 1169, 1122cm−1;
         [α]D24+66.0±2.1°(c=0.50, MeOH)Anal.
         (C25H32N2O4S3·0.3H2O)Calcd.(%): C, 57.07; H, 6.25; N,
         5.32; S, 18.28Found(%): C, 57.38; H, 6.34; N, 5.52; S,
         17.92
I-7E-88h 1                  H-NMR(CDCl3) δ 1.04(1H, m), 1.19-1.75(10H, m),
         2.02-2.24(5H, m), 2.53(1H, brs), 3.63(2H, t, J=6.6Hz),
         3.83(1H, m), 4.16(2H, s), 5.30-5.44(2H, m), 5.90(1H, d,
         J=6.9Hz), 6.79(1H, d, J=3.6Hz), 6.96(1H, dd, J=1.5
         and4.8Hz), 7.05(1H, dd, J=1.5and3.0Hz), 7.28(1H,
         dd, J=3.0and4.8Hz), 7.35(1H, d, J=3.6Hz); IR
         (CHCl3)3624, 3446, 3429, 1643, 1545, 1506cm−1; [α]D24+
         74.7±1.1°(c=1.009, MeOH)Anal.
         (C24H31NO2S2·0.2H2O)Calcd.(%): C, 66.54; H, 7.31; N,
         3.23; S, 14.80Found(%): C, 66.55; H, 7.26; N, 3.38; S,
         14.57
I-7E-88i 1                  H-NMR(CDCl3) δ 1.03(1H, m), 1.18-1.29(2H, m),
         1.34-1.47(4H, m), 1.53-1.67(4H, m), 2.01-2.14(5H, m),
         2.54(1H, brs), 3.32(3H, s), 3.36(2H, t, J=6.6Hz), 3.84
         (1H, m), 4.16(2H, s), 5.29-5.43(2H, m), 5.90(1H, d, J=
         7.5Hz), 6.79(1H, dt, J=3.9and0.9Hz), 6.96(1H, dd, J=
         1.5and5.1Hz), 7.06(1H, m), 7.29(1H, dd, J=3.0and
         5.1Hz), 7.35(1H, d, J=3.9Hz); IR(CHCl3)3446, 3429,
         1643, 1543, 1506, 1458, 1115cm−1; [α]D25+68.1±1.1°
         (c=1.019, MeOH)Anal.(C25H33NO2S2·0.2H2O)Calcd.(%):
         C, 67.13; H, 7.53; N, 3.13; S, 14.34Found(%): C, 67.10;
         H, 7.53; N, 3.21; S, 14.32

[0246]

TABLE 28
Compd.
No..      Physical property
I-7F-1a   1                  H-NMR(CDCl3) δ 1.09-2.51(16H, m), 1.17(3H, m), 3.80
          (1H, s), 5.28-5.42(2H, m), 6.24(1H, m), 6.33(2H, d, J=
          4.5Hz), 7.15(2H, d, J=4.5Hz), 7.39(1H, d, J=4.2Hz),
          7.56(1H, d, J=4.2Hz); IR(CHCl3)3442, 2956, 2877,
          1705, 1657, 1531, 1504, 1456, 1383, 1167, 1057, 1034cm−1;
          [α]D24+49.0±0.9°(c=1.00, CHCl3)Anal.
          (C24H30N2O5S2·0.7H2O)Calcd.(%): C, 57.28; H, 6.29; N,
          5.57; S, 12.74Found(%): C, 57.49; H, 6.11; N, 5.66; S,
          12.46
I-7G-1a   1                  H-NMR(CDCl3) δ 1.06-2.18(14H, m), 1.21(6H, s), 2.51
          (1H, m), 2.75(1H, m), 5.27-5.43(2H, m), 6.17(1H, d, J=
          6.9Hz), 6.33(2H, dd, J=4.5and2.4Hz), 7.16(2H, dd, J=
          4.5and2.4Hz), 7.37(1H, d, J=4.2Hz), 7.57(1H, d, J=
          4.2Hz); IR(CHCl3)3442, 2956, 2877, 1728, 1699,
          1657, 1531, 1504, 1475, 1456, 1383, 1167, 1074, 1057,
          1034cm−1; [α]D25+43.4±0.8°(c=1.00, CHCl3)
I-7G-88a  1                  H-NMR(CDCl3) δ 1.04-2.24(14H, m), 1.20(3H, s), 1.21
          (3H, s), 2.50(1H, m), 3.85(1H, m), 4.16(2H, s), 5.29-5.43
          (2H, m), 5.97(1H, d, J=7.5Hz), 6.79(1H, d, J=3.9Hz),
          6.96(1H, dd, J=5.1and1.2Hz), 7.05(1H, d, J=
          1.2Hz), 7.29(1H, m), 7.37(1H, J=3.9Hz); IR(CHCl3)
          3446, 3427, 2956, 2877, 1728, 1699, 1743, 1545, 1506,
          1475, 1458, 1282, 1024cm−1; [α]D26+48.6±0.9°(c=1.02,
          CHCl3)Anal.(C26H33NO3S2·0.3H2O)Calcd.(%): C, 65.46;
          H, 7.10; N, 2.94; S, 13.44Found(%): C, 65.66; H, 6.96;
          N, 3.12; S, 13.05
I-7G-126a 1                  H-NMR(CDCl3) δ 0.95(1H, d, J=9.9Hz), 1.08(3H, s),
          1.17(3H, s), 1.90(3H, s), 1.21(3H, s), 1.53-2.51(12H,
          m), 3.84(3H, s), 4.12(2H, s), 4.24(1H, m), 5.39-5.43(2H,
          m), 6.04(1H, d, J=8.7Hz), 6.77(1H, d, J=2.7Hz),
          6.86-6.92(2H, m), 7.14-7.23(2H, m),
          7.31(1H, d, J=3.6Hz);
          IR(CHCl3)3450, 3431, 2924, 1728, 1699, 1641,
          1601, 1543, 1506, 1471, 1406, 1387, 1367, 1319, 1288,
          1126, 1049, 1030cm−1; [α]D25+29.7±0.7°(c=1.00, CHCl3)
          Anal.(C31H41NO4S·0.3H2O)Calcd.(%): C, 70.37; H, 7.92;
          N, 2.65; S, 6.06Found(%): C, 70.50; H, 8.03; N, 2.78; S,
          5.84
I-7I-1a   1                  H-NMR(CDCl3) δ 0.98(1H, m), 1.19-1.49(10H, m),
          1.54-1.67(2H, m), 2.00(1H, m), 2.16-2.24(2H, m), 2.48
          (1H, brs), 3.81(1H, m), 5.79(1H, d, J=15.6Hz), 6.12
          (1H, d, J=7.2Hz), 6.33-6.34(2H, m), 7.03(1H, dt, J=
          15.6and7.2Hz), 7.15-7.17(2H, m), 7.35and7.56(each
          1H, eachd, eachJ=3.9Hz); IR(CHCl3)3523, 3442,
          2681, 1695, 1655, 1529, 1504, 1456, 1425, 1383, 1192,
          1167, 1057, 1034cm−1; [α]D24.5+40.1±0.8°(c=1.003,
          MeOH)Anal.(C23H28N2O5S2·0.3H2O)Calcd.(%): C,
          57.31; H, 5.98; N, 5.81; S, 13.30Found(%): C, 57.59; H,
          5.98; N, 5.86; S, 14.04

[0247]

TABLE 29
Compd.
No..     Physical property
I-7I-31a mp134-136°C.; 1H-NMR(CDCl3) δ 0.94(1H, m), 1.18-1.46
         (10H, m), 1.54-1.68(2H, m), 1.98(1H, m), 2.16-2.23
         (2H, m), 2.48(1H, brs), 3.83(1H, m), 4.14(2H, s), 5.79
         (1H, dt, J=15.6and1.5Hz), 5.83(1H, d, J=6.9Hz),
         6.78(1H, d, J=3.3Hz), 7.03(1H, dt, J=6.8and15.6Hz),
         7.23-7.33(5H, m), 7.35(1H, d, J=3.3Hz); IR(KBr)
         3329, 1695, 1649, 1616, 1549, 1527, 1454, 1319, 1288cm−1;
         [α]D25+35.6±0.8°(c=1.004, MeOH)Anal.
         (C26H31NO3S)Calcd.(%): C, 71.36; H, 7.14; N, 3.20; S,
         7.33Found(%): C, 71.15; H, 7.14; N, 3.28; S, 7.22
I-7I-47a 1                  H-NMR(CDCl3) δ 1.00(1H, m), 1.26-1.46(10H, m),
         1.55-1.65(2H, m), 2.00(1H, m), 2.17-2.24(2H, m), 2.49
         (1H, brs), 3.82(1H, m), 5.79(1H, d, J=15.6Hz), 6.16
         (1H, d, J=7.5Hz), 7.03(1H, dt, J=15.6and7.1Hz),
         7.11(1H, dd, J=3.6and4.8Hz), 7.40and7.63(each1H,
         eachd, eachJ=3.9Hz), 7.70(1H, dd, J=1.2and4.8Hz),
         7.75(1H, dd, J=1.2and3.6Hz); IR(CHCl3)3523,
         3442, 3375, 2681, 1695, 1653, 1529, 1504, 1402, 1336,
         1402, 1153, 1095, 1022cm−1; [α]D24+40.3±0.80°(c=1.015,
         MeOH)Anal.(C23H27NO5S3·0.2H2O)Calcd.(%): C, 55.55;
         H, 5.55; N, 2.82; S, 19.35Found(%): C, 55.52; H, 5.46;
         N, 2.92; S, 19.31
I-7I-88a 1                  H-NMR(CDCl3) δ 0.95(1H, m), 1.21-1.46(10H, m),
         1.55-1.68(2H, m), 1.98(1H, m), 2.16-2.33(2H, m), 2.49
         (1H, brs), 3.83(1H, m), 4.16(2H, s), 5.79(1H, d, J=15.6Hz),
         5.88(1H, d, J=7.5Hz), 6.79(1H, d, J=3.6Hz),
         6.95-7.08(3H, m), 7.28(1H, dd, J=3.0and4.8Hz), 7.35
         (1H, d, J=3.6Hz); IR(CHCl3)3523, 3446, 3427, 2679,
         1695, 1647, 1545, 1506, 1458, 1300, 1281cm−1; [α]D24+
         34.7±0.70°(c=1.004, MeOH)Anal.(C24H29NO3S2)
         Calcd.(%): C, 64.98; H, 6.59; N, 3.16; S, 14.46Found(%):
         C, 64.71; H, 6.61; N, 3.24; S, 14.17
I-7I-93a mp116-120°C.; 1H-NMR(CDCl3) δ 0.95(1H, m), 1.21-1.68
         (12H, m), 1.98(1H, m), 2.17-2.23(2H, m), 2.48(1H,
         brs), 3.84(1H, m), 4.34(2H, s), 5.80(1H, br d, J=15.6Hz),
         5.84(1H, d), 6.85(1H, br d, J=3.3Hz), 6.90(1H,
         m), 6.95(1H, dd, J=3.6, 5.1Hz), 7.02(1H, dt, J=15.9,
         6.9Hz), 7.19(1H, dd, J=1.2, 5.1Hz), 7.35(1H, d, J=
         3.3Hz); IR(Nujol)3032, 1695, 1648, 1542, 1506, 1458,
         1223, 1213cm−1; [α]D26.0+37.6±0.80°(c=1.015, MeOH)
         Anal.(C24H29NO3S2·0.1H2O)Calcd.(%): C, 64.72; H, 6.61;
         N, 3.14; S, 14.40Found(%): C, 64.64; H, 6.58; N, 3.24; S,
         14.50

[0248]

TABLE 30
Compd.
No..      Physical property
I-7I-126a 1                  H-NMR(CDCl3) δ 0.93(1H, m),
          1.20-1.48(10H, m), 1.54-1.64
          (2H, s), 1.97(1H, d, J=3.6Hz), 2.19(2H, dd, J=13.8,
          6.9Hz), 2.47(1H, m), 3.84(3H, s), 4.12(2H, s), 5.80(1H,
          dt, J=15.6, 1.5Hz), 5.81(1H, d, J=6.9Hz),
          6.78(1H, d, J=3.9Hz),
          6.86-6.93(2H, m), 7.01(1H, dt, J=15.6, 6.9Hz), 7.16
          (1H, d, J=7.2Hz), 7.22(1H, d, J=7.2Hz), 7.31(1H, d, J=
          3.9Hz); IR(Nujol)3276, 3079, 3058, 2678, 1691, 1604,
          1552, 1456, 1319, 1247cm−1;
          [α]D27.0+34.3±0.70°
          (c=1.010, MeOH)
          Anal.(C27H33NO4S)Calcd.(%): C, 69.35; H, 7.11; N, 3.00;
          S, 6.86Found(%): C, 69.19; H, 7.10; N, 3.12; S, 6.62
I-7I-143a 1                  H-NMR(CDCl3) δ 1.00(1H, m), 1.21-1.50(10H, m),
          1.59-1.65(2H, m), 2.00(1H, m),
          2.17-2.21(2H, m), 2.57(1H, brs),
          3.94(1H, m), 4.24(2H, s), 5.79(1H, d, J=15.6Hz), 6.07
          (1H, d, J=7.8Hz), 7.03(1H, dt, J=15.6and7.2Hz),
          7.18-7.30(6H, m), 7.42(1H, t, J=7.8Hz),
          7.81(1H, s), 8.18(1H, d, J=
          7.8Hz); IR(CHCl3)3523, 3438, 2683, 1695,
          1651, 1516, 1495cm−1;
          [α]D24+41.7±0.80°(c=1.002, MeOH)Anal.
          (C30H33NO3S)
          Calcd.(%): C, 73.62; H, 6.84; N, 2.86; S, 6.55Found(%): C,
          73.54; H, 6.77; N, 2.92; S, 6.49
I-7I-270a 1                  H-NMR(CDCl3) δ 0.99(1H, m), 1.18-1.70(12H, m), 2.01
          (1H, brd), 2.17-2.24(2H, m), 2.42(6H, s), 2.48(1H, brs),
          3.81(1H, m), 5.79(1H, dt, J=15.6, 1.5Hz), 5.88(2H, s),
          6.05(1H, d, J=7.5Hz), 7.03(1H, dt, J=15.6, 6.9Hz),
          7.35(1H, d, J=
          3.9Hz), 7.50(1H, d, J=3.9Hz); IR(CHCl3)3525, 3442,
          2677, 1695, 1655, 1529, 1504, 1375, 1180, 1119cm−1;
          [α]D25+37.7±0.8°(c=1.009, MeOH)Anal.
          (C25H32N2O5S2·0.3H2O)
          Calcd.(%): C, 58.87; H, 6.44; N, 5.49; S, 12.57
          Found(%): C, 58.99; H, 6.39; N, 5.51; S, 12.48
I-7I-307a mp171-173°C.; 1H-NMR(CDCl3) δ 0.91(1H, m),
          1.17-1.41(10H, m), 1.50-1.59(2H, m),
          1.93(1H, m), 2.12-2.19(2H, m),
          2.44(1H, m), 3.78(1H, m), 3.97(3H, s), 4.59(2H, s), 5.77
          (1H, d, J=15.6Hz), 5.81(1H, d, J=7.2Hz), 6.75(1H, d,
          J=3.6Hz), 7.01(1H, dt, J=15.6, 7.1Hz),
          7.28(1H, d, J=3.6Hz),
          7.25-7.36(3H, m), 7.46(1H, m), 7.78-7.82(1H, m), 7.92
          (1H, d, J=8.7Hz); IR(Nujol)3365, 3059, 2638, 1689, 1622,
          1552, 1527, 1516, 1464, 1263, 1252, 1092cm−1;
          [α]D25.5+
          31.6±0.7°(c=1.001, MeOH)Anal.
          (C31H35NO4S)Calcd.(%):
          C, 71.92; H, 6.81; N, 2.71; S, 6.19Found(%): C, 71.62; H,
          6.90; N, 2.79; S, 6.20
I-7I-327a mp176-179°C.; 1H-NMR(CDCl3)
          δ 0.98(1H, m), 1.20-1.70
          (12H, m), 2.00(1H, d, J=3.6Hz), 2.16-2.24(2H, m), 2.47
          (1H, brs), 3.00(2H, t, J=8.4Hz), 3.80(1H, m), 3.98
          (2H, t, J=8.4Hz), 5.79(1H, dt, J=1.8, 15.3Hz),
          6.01(1H, d, J=7.8Hz),
          6.97-7.24(4H, m), 7.33(1H, d, J=4.2Hz), 7.46(1H, d, J=
          4.2Hz), 7.58(1H, d, J=8.4Hz); IR(Nujol)3332, 2925,
          2854, 1689, 1608, 1554, 1479, 1460, 1365, 1238, 1161cm−1;
          [α]D26+36.3±0.8°(c=1.012%, MeOH);
          Anal.(C27H32N2O5S2)
          Calcd.(%)C, 61.34; H, 6.10; N, 5.30; S, 12.13Found(%)C,
          61.08; H, 6.22; N, 5.24; S, 11.82

[0249]

TABLE 31
Compd.
No..      Physical property
I-7I-332a mp136-139°C.; 1H-NMR(CDCl3)
          δ 0.98(1H, m), 1.20-1.82
          (14H, m), 2.01(1H, d, J=3.0Hz), 2.21(2H, q, J=
          6.9Hz), 2.48(1H, brs), 2.53(2H, t, J=6.6Hz), 3.53
          (2H, t, J=6.3Hz), 3.79-3.87(3H, m), 5.79(1H, dt, J=
          1.5, 15.6Hz), 6.01(1H, d, J=7.2Hz), 6.97-7.26(5H, m),
          7.31(1H, d, J=3.9Hz), 7.77(1H, dd, J=0.9, 7.8Hz); IR
          (Nujol)3371, 3325, 2922, 1728, 1693, 1614, 1549, 1342,
          1163cm−1; [α]D24+35.4±0.8°
          (c=1.009%, MeOH); Anal.
          (C28H34N2O5S2)Calcd.(%)C, 61.97; H, 6.31; N, 5.16; S,
          11.82Found(%)C, 61.94; H, 6.47; N, 5.14; S, 11.69
I-7I-343a 1                  H-NMR(CDCl3) δ 1.07(1H, m), 1.22-1.62(12H, m), 1.98
          (1H, m), 2.22(1H, m), 2.54(1H, m), 3.94(1H, m), 5.80
          (1H, d, J=15.6Hz), 6.27(1H, d, J=8.1Hz), 7.02(1H,
          m), 7.45-7.60(5H, m), 7.89(1H, s), 7.99-8.05(3H, m),
          8.59(1H, d, J=8.1Hz); IR(KBr)3381, 3292, 3066,
          2949, 2927, 2873, 1685, 1655, 1620, 1558, 1477, 1446,
          1385, 1319, 1308, 1284, 1244, 1230, 1209cm−1;
          [α]D26.0+32.6±1.5°
          (c=0.50, DMSO)Anal.(C29H31NO5S2·0.4H2O)
          Calcd.(%): C, 63.92; H, 5.88; N, 2.57; S, 11.77Found(%):
          C, 64.07; H, 5.82; N, 2.75; S, 11.41
I-7I-385a 1                  H-NMR(CDCl3) δ 1.03(1H, m), 1.20-1.74(12H, m), 2.04
          (1H, m), 2.14-2.26(2H, m), 2.57(1H, m), 3.97(1H, m),
          5.77(1H, d, J=15.6Hz), 6.27(2H, t, J=2.4Hz), 6.37
          (1H, d, J=8.4Hz), 7.02(1H, dt, J=15.6, 6.9Hz), 7.22
          (2H, t, J=2.4Hz), 7.57(1H, t, J=7.8Hz), 7.67(1H, d, J=
          7.8Hz), 8.37(1H, d, J=7.8Hz), 8.44(1H, s); IR
          (CHCl3)3452, 3023, 2954, 2877, 1695, 1650, 1516, 1456,
          1373, 1282, 1188, 1163, 1057cm−1;
          [α]D22.0+39.4 ±0.8°
          (c=1.017, MeOH)Anal.(C27H30N2O5S2·0.1H2O)
          Calcd.(%): C, 61.36; H, 5.76; N, 5.30; S, 12.14Found(%):
          C, 61.26; H, 5.89; N, 5.11; S, 11.95
I-7I-389a mp140-143°C.; 1H-NMR(CDCl3) δ 0.96(1H, m),
          1.21-1.46(10H, m), 1.54-1.64(2H, m),
          1.99(1H, m), 2.23(3H,
          s)+2.16-2.23(2H, m), 2.48(1H, m), 3.21(2H, t,
          J=8.7Hz), 3.81(1H, m), 4.62(2H, t, J=8.7Hz), 5.79(1H,
          d, J=15.6Hz), 5.88(1H, d, J=7.8Hz), 6.89(1H, s), 6.96
          (1H, s), 7.02(1H, dd, J=15.6, 6.9Hz),
          7.08(1H, d, J=3.9Hz),
          7.35(1H, d, J=3.9Hz); IR(Nujol)3294, 3066,
          2675, 1695, 1649, 1604, 1550, 1512, 1327, 1203cm−1;
          [α]D25+29.2±0.7°(c=1.013, MeOH)Anal.
          (C28H33NO4S2)Calcd.(%): C, 65.72; H, 650; N, 2.74; S,
          12.53Found(%): C, 65.57; H, 6.62; N, 2.62; S, 12.37

[0250]

TABLE 32
Compd.
No..      Physical property
I-7I-391a mp204-207°C.; 1H-NMR(CDCl3)
          δ 1.01(1H, m), 1.25-1.46
          (10H, m), 1.54-1.64(2H, m), 2.00(1H, m), 2.17-2.23(2H,
          m), 2.31(3H, s), 2.48(1H, m), 3.18(2H, t, J=8.7Hz), 3.81
          (1H, m), 4.71(2H, t, J=8.7Hz), 5.79(1H, d, J=15.6Hz),
          6.20(1H, d, J=7.8Hz), 7.02(1H, dt, J=15.6, 6.9Hz), 7.21
          (1H, s), 7.41(1H, d, J=3.9Hz), 7.50(1H, s), 7.70(1H, d,
          J=3.9Hz); IR(Nujol)3398, 3197, 3086, 1716, 1689, 1639,
          1541, 1313, 1151cm−1;
          [α]D25+37.9±0.8°(c=1.005, MeOH)
          Anal.(C28H33NO6S2)Calcd.(%): C, 61.85; H,
          6.12; N, 2.58; S, 11.80Found(%): C, 61.61; H, 6.08; N,
          2.50; S, 11.69
I-7J-1a   mp116-118°C.; 1H-NMR(CDCl3) δ 0.99(1H, m),
          1.19-1.82(12H, m), 1.79(3H, d, J=1.2Hz), 2.01(1H, m),
          2.17(2H, brq, J=7.8Hz), 2.48(1H, m),
          3.82(1H, m), 6.00(1H, d, J=
          7.8Hz), 6.32-6.35(2H, m), 6.85(1H, m), 7.15-7.17(2H,
          m), 7.33(1H, d, J=3.9Hz), 7.63(1H, d, J=3.9Hz), 7.57
          (1H, d, J=3.9Hz); IR(Nujol)3354, 3141, 3099, 3076,
          2669, 2557, 1682, 1641, 1624, 1539, 1390, 1375, 1302,
          1190, 1167cm−1;
          [α]D2637.1±0.6°(c=1.002, MeOH)Anal.
          (C24H30N2O5S2)Calcd.(%): C, 58.75; H, 6.16;
          N, 5.71; S, 13.07Found(%):
          C, 58.55; H, 6.14; N, 5.70; S, 12.89
I-7K-1a   mp168-171°C.; 1H-NMR(CDCl3)
          δ 0.99(1H, m), 1.20-1.82
          (12H, m), 2.01-2.20(3H, m), 2.12(3H, d, J=0.9Hz), 2.48
          (1H, m), 3.82(1H, m), 4.05(2H, s), 5.65(1H, s), 5.97(1H,
          d, J=7.5Hz), 6.33-6.35(2H, m), 7.16-7.18(2H, m), 7.33
          (1H, d, J=3.9Hz), 7.63(1H, d, J=3.9Hz), 7.58(1H, d, J=
          3.9Hz); IR(Nujol)3330, 3086, 1693, 1633, 1614, 1544,
          1456, 1377, 1250, 1194, 1169, 1057cm−1;
          [α]D26+34.0±1.5°
          (c=0.509, MeOH)Anal.
          (C24H30N2O5S2·0.6CHCl3)
          Calcd.(%): C, 52.55; H, 5.49; N, 4.98; S, 11.41; Cl, 11.35
          Found(%): C, 52.62; H, 5.19; N, 4.93; S, 11.11; Cl, 10.53
I-7M-1a   1                  H-NMR(CDCl3) δ 1.00-1.70(13H, m), 2.01(1H, m), 2.47
          (1H, m), 3.52(2H, t, J=6.6Hz), 3.82(1H, m), 4.04(2H, s),
          5.54-5.70(2H, m), 6.13(1H, d, J=7.2Hz), 6.32-6.35(2H,
          m), 7.15-7.18(2H, m), 7.37(1H, d, J=4.2Hz), 7.57(1H, d,
          J=4.2Hz); IR(CHCl3)3440, 1778, 1731, 1655, 1531, 1504,
          1456, 1383, 1192, 1167, 1128, 1057, 1034cm−1; [α]D24+
          40.9±0.8°(c=1.007, MeOH)Anal.
          (C22H28N2O6S2·0.4H2O)
          Calcd.(%): C, 54.17; H, 5.95; N, 5.74; S, 13.15Found(%):
          C, 54.51; H, 6.00; N, 5.58; S, 12.76
I-7M-1e   1                  H-NMR(CDCl3) δ 1.02-1.70(13H, m), 2.02(1H, m), 2.48
          (1H, m), 3.31(3H, s), 3.50(2H, t, J=6.6Hz), 3.85(1H, m),
          3.99(2H, s), 6.05(1H, d, J=8.1Hz), 6.34(2H, m), 7.16
          (2H, m), 7.36(1H, d, J=3.9Hz), 7.58(1H, d, J=3.9Hz),
          8.88(1H, s); IR(CHCl3)3442, 3352, 2956, 2877, 1730,
          1657, 1531, 1504, 1456, 1423, 1402, 1385, 1350, 1167,
          1076, 1057, 1034cm−1;
          [α]D25.5+35.6±0.8°(c=1.00, MeOH)
          Anal.(C23H31N3O7S3·0.8MeOH)Calcd.(%):
          C, 48.29; H, 5.74; N, 7.34; S, 16.81Found(%):
          C, 48.00; H, 5.68; N, 7.74; S, 17.12

[0251]

TABLE 33
Compd.
No..     Physical property
I-7M-40a 1                  H-NMR(CDCl3) δ 1.03(1H, m), 1.22-1.74(12H, m), 2.01
         (1H, m), 2.51(1H, brs), 3.54(2H, dt, J=1.5, 6.3Hz), 3.91
         (1H, m), 4.05(2H, s), 6.03(1H, d, J=8.1Hz), 7.25-7.64
         (7H, m); IR(CHCl3)2954, 1780, 1732, 1643, 1541, 1510,
         1491, 1454, 1219, 1213, 1132cm−1;
         [α]D25+50.9±0.9°
         (c=1.013%, MeOH); Anal.(C24H29NO4S·0.5H2O)Calcd.(%)
         C, 66.03; H, 6.93; N, 3.21; S, 7.34Found(%)C, 66.14; H,
         6.92; N, 3.26; S, 7.22
I-7M-43a mp132-134°C.; 1H-NMR(CDCl3) δ 1.01(1H, m), 1.20-1.75
         (12H, m), 2.01(1H, d, J=3.0Hz), 2.47(1H, brs), 3.53(2H,
         t, J=6.0Hz), 3.79-3.96(5H, m),
         4.05(2H, s), 6.06(1H, d, J=
         7.8Hz), 6.85(1H, dd, J=1.5, 8.1Hz), 6.96(1H, m), 7.11
         (1H, m), 7.29(1H, d, J=4.2Hz), 7.34(1H, d, J=4.2Hz),
         7.83(1H, dd, J=1.5, 8.1Hz); IR(Nujol)3325, 3084, 2924,
         1730, 1612, 1562, 1491, 1460, 1369,
         1250, 1236, 1165, 1138cm−1;
         [α]D26+53.6±0.9°
         (c=1.009%, MeOH); Anal.
         (C22H27NO4S2)Calcd.(%)C, 60.94; H, 6.28; N, 3.23; S,
         14.79Found(%)C, 60.77; H, 6.32; N, 3.38; S, 14.51
I-7M-47a mp116-118°C.; 1H-NMR(CDCl3) δ 1.06(1H, m),
         1.19-1.70(12H, m), 2.00(1H, m), 2.49(1H, m),
         3.52(2H, t, J=6.3Hz),
         3.84(1H, m), 4.05(2H, s), 6.21(1H, d, J=7.8Hz),
         7.11(1H, dd, J=3.9, 4.5Hz), 7.42(1H, d, J=3.9Hz), 7.63
         (1H, d, J=3.9Hz), 7.70(1H, dd, J=0.9, 4.8Hz), 7.75(1H,
         dd, J=0.9, 3.9Hz); IR(Nujol)3319, 3097, 2557, 1732,
         1618, 1566, 1444, 1432, 1321, 1232, 1151, 1031cm−1;
         [α]D24+
         44.4±0.8°(c=1.009, MeOH)Anal.(C22H27NO6S3)
         Calcd.(%): C, 53.10; H, 5.47; N, 2.81; S, 19.33Found(%):
         C, 52.90; H, 5.37; N, 2.91; S, 19.10
I-7M-59a mp103-104°C.; 1H-NMR(CDCl3) δ 0.99(1H, m),
         1.20-1.70(12H, m), 1.99(1H, d, J=3.3Hz),
         2.45(1H, m), 3.23(2H, t,
         J=8.7Hz), 3.48-3.55(2H, m), 3.84(1H, m), 4.04(2H, s),
         5.89(1H, d, J=8.1Hz), 7.01(1H, dd, J=3.6, 5.1Hz), 7.04
         (1H, d, J=3.9Hz), 7.29(1H, dd, J=1.5, 3.6Hz), 7.33(1H,
         d, J=3.9Hz), 7.43(1H, dd, J=1.5, 5.1Hz); IR(Nujol)
         3332, 2922, 2854, 1930, 1601, 1564, 1458, 1439, 1331,
         1230, 1134cm−1;
         [α]D26+40.0±0.8°(c=1.004%, MeOH);
         Anal.(C22H27NO4S3)Calcd.(%)C, 56.75; H, 5.84; N, 3.01;
         S, 20.66Found(%)C, 56.59; H, 5.81; N, 3.04; S, 20.65
I-7M-88a mp90-91.5°C.; 1H-NMR(CDCl3) δ 1.00(1H, m),
         1.18-1.70
         (12H, m), 1.99(1H, m), 2.46(1H, m), 3.52(2H, dt, J=1.8,
         8.7Hz), 387(1H, m), 4.04and4.16(each2H, s), 4.58(1H,
         brs), 5.91(1H, d, J=8.7Hz), 6.80(1H, d, J=3.6Hz), 6.96
         (1H, dd, J=1.2, 5.1Hz), 7.06(1H, m), 7.29(1H, dd, J=
         3.0, 4.8Hz), 7.37(1H, d, J=3.9Hz); IR(Nujol)3332, 3095,
         3080, 2553, 1735, 1597, 1562, 1537, 1435, 1325, 1304,
         1228, 1146cm−1; [α]D24+39.8±0.8°(c=1.002,
         MeOH)Anal.
         (C23H29NO4S2)Calcd.(%): C, 61.72; H, 6.53; N, 3.13; S,
         14.33Found(%): C, 61.60; H, 6.20; N, 3.24; S, 14.01

[0252]

TABLE 34
Compd.
No..      Physical property
I-7M-126a 1                  H-NMR(CDCl3) δ 0.96(1H, m),
          1.23-1.26(2H, m), 1.38-1.46
          (6H, m), 1.54-1.63(4H, s), 1.97(1H, d, J=3.6Hz),
          2.45(1H, m), 3.48-3.53(2H, m), 3.83(3H, s), 3.85(1H, m),
          4.03(2H, s), 4.12(2H, s), 5.88(1H, d, J=7.8Hz), 6.77(1H,
          d, J=3.6Hz), 6.86-6.90(2H, m),
          7.16(1H, dd, J=4.5, 1.8Hz),
          7.21(1H, dd, J=7.8, 1.8Hz), 7.33(1H, d, J=3.6Hz);
          IR(CHCl3)3427, 2875, 1639, 1504, 1460, 1248, 1221cm−1;
          [α]D27.0+36.8±1.5°(c=0.508, MeOH)Anal.
          (C26H33NO5S·0.3H2O)Calcd.(%): C, 65.47; H, 7.10; N, 2.94;
          S, 6.72Found(%): C, 65.30; H, 7.01; N, 3.02; S, 6.54
I-7M-143a mp123-125°C.;
          1                  H-NMR(CDCl3) δ 1.04(1H, m), 1.20-1.75
          (12H, m), 2.01(1H, brs), 2.55(1H, brs), 3.53(2H, dt, J=
          1.8, 6.0Hz), 3.98(1H, m), 4.02and4.24(2H, s), 6.08(1H,
          d, J=7.8Hz), 7.17-7.45(7H, m), 7.83(1H, s), 8.16(1H, d,
          J=7.8Hz); IR(Nujol)3280, 2924, 1722, 1612, 1566, 1454,
          1242, 1228, 1137cm−1;
          [α]D26+39.2±0.6°(c=1.012%,
          MeOH); Anal.(C29H33NO4S)Calcd.(%)C, 70.85; H, 6.77;
          N, 2.85; S, 6.52Found(%)C, 70.58;
          H, 6.70; N, 2.94; S, 6.40
I-7M-197a 1                  H-NMR(CDCl3) δ 0.98(1H, m), 1.20-1.70(12H, m), 1.98
          (1H, d, J=3.3Hz), 2.45(1H, m), 3.23(2H, t, J=8.7Hz),
          3.49-3.54(2H, m), 3.86(1H, m), 4.03and4.08(2H, s), 4.58
          (2H, t, J=8.7Hz), 5.88(1H, d, J=8.4Hz), 6.20(1H, t, J=
          3.6Hz), 6.77-6.82(2H, m), 6.96(1H, d, J=7.2Hz), 7.10
          (1H, d, J=7.2Hz), 7.35(1H, d, J=3.6Hz); IR(CHCl3)
          2954, 1732, 1641, 1545, 1506, 1477, 1458, 1254, 1225,
          1221, 1213, 1207, 1130cm−1;
          [α]D26+37.2±0.8°(c=1.008%,
          MeOH); Anal.(C27H33NO5S·0.3H2O)Calcd.(%)C,
          66.31; H, 6.93; N, 2.86; S, 6.56Found(%)C,
          66.24; H, 6.91; N, 2.92; S, 6.52
I-7M-270a mp.141-143°C.;
          1                  H-NMR(CDCl3) δ 1.02(1H, br), 1.18-1.70
          (12H, m), 2.01(1H, brd), 2.42(6H, s), 2.48(1H, brs), 3.53
          (2H, dt, J=0.9, 6.6Hz), 3.83(1H, m), 4.06(2H, s), 5.88
          (2H, s), 6.11(1H, d, J=7.8Hz), 7.36(1H, d, J=3.9Hz),
          7.50(1H, d, J=3.9Hz); IR(Nujol)3327, 3097, 3084, 2555,
          1732, 1616, 1556, 1234, 1219, 1176, 1134, 1113cm−1;
          [α]D26+
          40.5±0.8°(c=1.014, MeOH)Anal.(C24H32N2O6S2)
          Calcd.(%): C, 56.67; H, 6.37; N, 5.51; S, 12.61Found(%):
          C, 56.56; H, 6.10; N, 5.48; S, 12.38
I-7M-307a mp131-132°C.;
          1                  H-NMR(CDCl3) δ 0.94(1H, m), 1.20-1.23
          (2H, m), 1.34-1.39(6H, m),
          1.51-1.63(4H, m), 1.94(1H, m),
          2.42(1H, m), 3.45-3.49(2H, m), 3.81(1H, m), 3.98(3H, s),
          4.01(2H, s), 4.59(2H, s), 5.85(1H, d, J=7.5Hz), 6.75(1H,
          d, J=3.3Hz), 7.28-7.36(3H, m,), 7.47(1H, t, J=7.7Hz),
          7.79(1H, d, J=3.9Hz), 7.82(1H, d, J=4.8Hz), 7.92(1H,
          d, J=8.4Hz);
          IR(Nujol)3340, 3068, 2744, 2546, 1738,
          1604, 1560, 1435, 1250, 1236, 1146cm−1;
          [α]D25.5+36.1±0.8°
          (c=1.000, MeOH)Anal.(C30H35NO5S)Calcd.(%): C, 69.07;
          H, 6.76; N, 2.68; S, 6.15Found(%): C, 68.99; H, 6.87; N,
          2.74; S, 6.05

[0253]

TABLE 35
Compd.
No..      Physical property
I-7M-315a 1                  H-NMR(CDCl3) δ 1.04(1H, m), 1.26-1.64(12H, m), 2.03
          (1H, m), 2.55(1H, m), 3.54(2H, t, J=5.1Hz), 3.99
          (1H, m), 4.03(2H, s), 4.26(2H, s),
          6.07-6.10(1H, d, J=7.5Hz),
          7.00-7.23(5H, m), 7.43(1H, m), 7.85(1H, s),
          8.16(1H, d, J=
          8.1Hz); IR(CHCl3)3508, 3437, 2954, 2875,
          1780, 1732, 1651, 1518, 1477, 1456, 1396,
          1363cm−1; [α]D24.0+38.1±0.8°
          (c=1.03, MeOH)Anal.(C29H32FNO4S·0.6MeOH)Calcd.(%):
          C, 67.22; H, 6.56; N, 2.65;F, 3.59; S, 6.06Found(%): C,
          67.31; H, 6.57; N, 2.92;F, 3.21; S, 6.09
I-7M-316a 1                  H-NMR(CDCl3) δ 1.04(1H, m),
          1.23-1.68(11H, m), 2.01
          (1H, m), 2.55(2H, m), 3.54(2H, t, J=6.6Hz), 3.82(3H, s),
          3.99(1H, m), 4.02(2H, s),
          4.23(2H, s), 6.09(1H, d, J=8.1Hz),
          6.83-6.91(2H, m), 7.05-7.23(3H, m), 7.39(1H, m),
          7.85(1H, s), 8.12(1H, d, J=8.1Hz); IR(CHCl3)3437,
          2954, 2875, 1780, 1732, 1651, 1601, 1516, 1493, 1464,
          1394, 1363, 1246cm−1;
          [α]D26.0+35.2±1.5°(c=0.50, MeOH)
          Anal.(C30H35NO5S·0.2H2O)Calcd.(%): C,
          68.60; H, 6.79; N,
          2.67; S, 6.10Found(%): C, 68.56; H, 6.89; N, 2.86; S, 5.93
I-7M-317a 1                  H-NMR(CDCl3) δ 1.03(1H, m), 1.22-1.65(11H, m), 2.02
          (1H, m), 2.57(1H, m), 3.54(2H, d, J=6.0Hz), 4.00(1H,
          m), 4.03(3H, s), 4.35(2H, s), 6.10(1H, d, J=7.8Hz),
          7.08-7.24(4H, m), 7.39-7.44(2H, m), 7.85(1H, s),
          8.18(1H, d, J=8.4Hz);
          IR(CHCl3)3508, 3437, 2954, 2875,
          1780, 1732, 1651, 1568, 1518, 1495, 1475,
          1444, 1394, 1363cm−1;
          [α]D26.0+34.9±0.8°(c=1.00, MeOH)Anal.
          (C29H32ClNO4S)Calcd.(%): C, 66.21; H, 6.13; N, 2.66; Cl,
          6.74; S, 6.10Found(%): C, 66.01; H, 6.32; N, 2.89; Cl, 6.03;
          S, 5.91
I-7M-318a 1                  H-NMR(CDCl3) δ 1.05(1H, m), 1.22-1.64(12H, m), 2.01
          (1H, m), 2.56(1H, m), 3.49-3.52(2H, m), 3.97(2H, s), 3.50
          (1H, m), 4.24(2H, s), 6.12(1H, d, J=6.3Hz), 6.81-6.91
          (2H, m), 7.11-7.18(3H, m), 7.39(1H, m), 7.84(1H, s), 8.12
          (1H, d, J=7.8Hz); IR(CHCl3)3597, 3435, 2954, 2875,
          1780, 1730, 1649, 1518, 1496, 1456, 1394, 1363, 1327cm−1;
          [α]D27.0+36.9±0.8°
          (c=1.01, MeOH)Anal.
          (C29H33NO5S·1.2H2O)Calcd.(%): C, 65.81; H, 6.74; N, 2.65;
          S, 6.06Found(%): C, 65.74;
          H, 6.59; N, 2.79; S, 5.90
I-7M-327a mp137-139°C.; 1H-NMR(CDCl3) δ 1.01(1H, m),
          1.20-1.70(12H, m), 2.00(1H, d, J=3.0Hz),
          2.46(1H, brs), 3.01(2H,
          t, J=8.7Hz), 3.52(2H, t, J=6.3Hz), 3.81(1H, m), 3.98
          (2H, t, J=8.4Hz), 4.04(2H, s), 6.11(1H, d, J=7.5Hz),
          6.98-7.24(3H, m), 7.35(1H, d, J=3.9Hz), 7.46(1H, d, J=
          3.9Hz), 7.57(1H, d, J=8.1Hz); IR(Nujol)3325, 2924,
          1730, 1616, 1566, 1460, 1444, 1373, 1236, 1163, 1138cm−1;
          [α]D26+39.2±0.8°(c=1.006%, MeOH); Anal.
          (C26H32N2O6S2·0.2H2O)Calcd.(%)C, 58.23; H, 6.09; N,
          5.22; S, 11.96Found(%)C, 58.19; H, 6.14; N, 5.22; S,
          11.85

[0254]

TABLE 36
Compd.
No..      Physical property
I-7M-329a mp137-139°C.; 1H-NMR(d6-DMSO) δ 1.14-1.60(13H,
          m), 1.91(1H, d, J=3.0Hz), 2.29(1H, brs), 3.05(2H, t, J=
          8.4Hz), 3.37(2H, t, J=6.3Hz), 3.57(1H, m), 3.91(2H,
          s), 4.01(2H, t, J=8.4Hz), 6.91(1H, m), 7.27-7.37(2H,
          m), 7.78(1H, d, J=3.9Hz), 7.93(1H, d, J=3.9Hz), 8.53
          (1H, d, J=6.9Hz); IR(Nujol)3325, 2924, 1730, 1618,
          1566, 1460, 1444, 1435, 1375, 1234, 1165, 1138, 1070cm−1;
          [α]D25+38.2±0.8°(c=1.015%, MeOH); Anal.
          (C26H31FN2O6S2)Calcd.(%)C, 56.71; H, 5.67;F, 3.45; N,
          5.09; S, 11.65Found(%)C, 56.61; H, 5.47;F, 3.32; N,
          5.12; S, 11.54
I-7M-330a mp158-160°C.; 1H-NMR(d6-DMSO) δ 1.13-1.58(13H,
          m), 1.91(1H, d, J=3.0Hz), 2.29(1H, brs), 2.97(2H, t, J=
          8.4Hz), 3.37(2H, t, J=6.9Hz), 3.57(1H, m), 3.91(2H,
          s), 3.97(2H, t, J=8.4Hz), 7.10(1H, d, J=8.7Hz), 7.43
          (1H, dd, J=4.5, 8.4Hz), 7.72(1H, d, J=3.9Hz), 7.92
          (1H, d, J=3.9Hz), 8.52(1H, d, J=6.9Hz); IR(Nujol)
          3325, 3095, 2924, 1732, 1618, 1566, 1481, 1460, 1444,
          1373, 1236, 1221, 1167, 1140, 1038cm−1; [α]D25+
          38.2±0.8°(c=1.009%, MeOH); Anal.(C26H31FN2O6S2)
          Calcd.(%)C, 56.71; H, 5.67;F, 3.45; N, 5.09; S, 11.65
          Found(%)C, 56.51; H, 5.74;F, 3.30; N, 5.09; S, 11.57
I-7M-331a mp152-154°C.; 1H-NMR(d6-DMSO) δ 1.14-1.60(13H,
          m), 1.92(1H, d, J=2.7Hz),
          2.29(1H, brs), 2.98(2H, t, J=
          8.4Hz), 3.37(2H, t, J=6.6Hz), 3.58(1H, m), 3.91(2H,
          s), 3.99(2H, t, J=8.4Hz),
          6.88(1H, ddd, J=2.4, 8.1, 9.0Hz),
          7.16-7.26(2H, m), 7.82(1H, d, J=4.2Hz), 7.94(1H,
          d, J=4.2Hz), 8.54(1H, d, J=7.5Hz); IR(Nujol)3317,
          3091, 2924, 1734, 1616, 1568, 1491, 1460, 1446, 1435,
          1371, 1261, 1234, 1221, 1176, 1163, 1142, 1092, 1036cm−1;
          [α]D25+38.7±0.8°(c=1.012%, MeOH); Anal.
          (C26H31FN2O6S2)Calcd.(%)C,
          56.71; H, 5.67; F, 3.45; N,
          5.09; S, 11.65Found(%)C, 56.49; H, 5.36;F, 3.34; N,
          5.10; S, 11.27
I-7M-332a mp100-103°C.; 1H-NMR(CDCl3) δ 1.01(1H, m),
          1.20-1.82(14H, m), 2.01(1H, d, J=3.3Hz),
          2.47(1H, brs),
          2.53(2H, t, J=6.6Hz), 3.53(2H, t, J=6.3Hz), 3.79-3.88
          (3H, m), 4.05(2H, s), 6.07(1H, d, J=7.8Hz),
          7.03-7.23(4H, m), 7.32(1H, d, J=3.9Hz), 7.78(1H, dd,
          J=0.9, 8.1Hz); IR(Nujol)3329, 2925, 1730, 1614, 1562,
          1458, 1363, 1346, 1234, 1159cm−1; [α]D24+37.7±0.8°
          (c=1.018%, MeOH); Anal.(C27H34N2O6S2·0.4H2O)
          Calcd.(%)C, 58.55; H, 6.33; N, 5.06; S, 11.58Found(%)
          C, 58.84; H, 6.41; N, 5.02; S, 11.30

[0255]

TABLE 37
Compd. No.. Physical property
I-7M-333a   mp 125-128° C.; 1H-NMR(CDCl3) δ 1.01(1H, m), 1.20-
            1.75(12H, m), 2.01(1H, d, J=3.0Hz), 2.47(1H, brs),
            3.53(2H, t, J=6.0Hz), 3.79-3.96(5H, m), 4.05(2H, s),
            6.06(1H, d, J=7.8Hz), 6.85(1H, dd, J=1.5, 8.1Hz),
            6.96(1H, m), 7.11(1H, m), 7.29(1H, d, J=4.2Hz), 7.34
            (1H, d, J=4.2Hz), 7.83(1H, dd, J=1.5, 8.1Hz); IR
            (Nujol) 3325, 3084, 2924, 1730, 1612, 1562, 1491, 1460,
            1369, 1250, 1236, 1165, 1138cm−1; [α]D26+36.4±0.8°
            (c=1.008%, MeOH); Anal.(C26H32N2O7S2.0.3H2O)
            Calcd.(%) C, 56.36; H, 5.93; N, 5.06; S, 11.57 Found(%)
            C, 56.36; H, 5.72; N, 5.08; S, 11.53
I-7M-334a   mp 127-129° C.; 1H-NMR(CDCl3) δ 1.02(1H, m), 1.20-
            1.70(12H, m), 2.01(1H, d, J=3.3Hz), 2.48(1H, brs),
            3.05(2H, dd, J=5.7, 9.0Hz), 3.53(2H, t, J=6.3Hz),
            3.82(1H, m), 4.03-4.07(4H, m), 6.08(1H, d, J=8.1Hz),
            7.07-7.33(5H, m), 7.67(1H, m); IR(Nujol) 3315, 2924,
            1761, 1728, 1616, 1550, 1467, 1363, 1165cm−1;
            [α]D24+37.1±0.8°(c=1.010%, MeOH); Anal.
            (C26H32N2O6S3.0.1Hexane) Calcd.(%) C, 55.72; H, 5.87;
            N, 4.89; S, 16.78 Found(%) C, 55.86; H, 5.94; N, 4.84; S,
            16.61
I-7M-336a   mp 209-212° C.; 1H-NMR(d6-DMSO) δ 1.11-1.56(13H,
            m), 1.91(1H, m), 2.29(1H, brs), 3.37(2H, t, J=6.3Hz),
            3.58(1H, m), 3.91(2H, s), 4.63(4H, s), 7.20-7.35(4H,
            m), 7.77(1H, d, J=3.9Hz), 7.96(1H, d, J=3.9Hz), 8.51
            (1H, d, J=7.5Hz); IR(Nujol) 3332, 2924, 1736, 1616,
            1562, 1468, 1354, 1240, 1165, 1140, 1092cm−1; Anal.
            (C26H32N2O6S2) Calcd.(%) C, 58.62; H, 6.06; N, 5.26; S,
            12.04 Found(%) C, 58.38; H, 5.98; N, 5.25; S, 11.82
I-7M-337a   1                  H-NMR(CDCl3) δ 1.04(1H, m), 1.23-1.32(3H, m),
            1.43-1.69(8H, s), 2.02(1H, m), 2.52-2.54(2H, m), 3.53
            (2H, t, J=6.3Hz), 4.01(1H, m), 4.03(2H, s), 4.28(2H,
            s), 6.06(1H, d, J=8.1Hz), 7.01-7.07(2H, m), 7.15-7.31
            (4H, m), 7.65(1H, dd, J=7.5, 0.9Hz), 8.17(1H, s); IR
            (CHCl3) 3323, 2656, 2548, 1728, 1621, 1562, 1456, 1234,
            1130cm−1; [α]D27.0+26.7±0.7°(c=1.001, MeOH) Anal.
            (C29H32FNO5.0.5H2O) Calcd.(%): C, 69.31; H, 6.62; N,
            2.79; F, 3.58 Found(%): C, 69.19; H, 6.67; N, 2.82; F,
            3.28
I-7M-342a   1                  H-NMR(CDCl3) δ 1.05(1H, m), 1.22-1.63(12H, m), 2.01
            (1H, m), 2.55(1H, m), 3.49-3.53(2H, m), 3.99(1H, m),
            4.01(2H, s), 6.14(1H, br), 7.18-7.26(5H, m), 7.43-7.54
            (2H, m), 7.85(1H, s), 8.32(1H, d, J=7.8Hz); IR(CHCl3)
            3438, 2954, 2875, 1780, 1730, 1649, 1583, 1516, 1477,
            1456, 1375cm−1; [α]D26.0+38.5±0.8°(c=1.03, MeOH)

[0256]

TABLE 38
Compd. No.. Physical property
I-7M-343a   1                  H-NMR(CDCl3) δ 1.05(1H, m), 1.24-1.63(12H, m), 2.05
            (1H, m), 2.54(1H, m), 3.54(2H, t, J=8.1Hz), 3.94(1H,
            m), 4.03(2H, s), 6.17(1H, d, J=7.5Hz), 7.45-7.63(4H,
            m), 7.94(1H, s), 8.01-8.11(3H, m), 8.62(1H, d, J=8.4Hz);
            IR(CHCl3) 3437, 3375, 2954, 2875, 1780, 1730,
            1518, 1383, 1315, 1309cm−1; [α]D25.0+33.3±0.7°(c=1.04,
            MeOH)
I-7M-385a   1                  H-NMR(CDCl3) δ 1.07(1H, m), 1.20-1.72(12H, m), 2.04
            (1H, m), 2.56(1H, m), 3.52(2H, dt, J=6.3, 1.8Hz), 3.97
            (1H, s), 4.03(2H, s), 6.27(2H, t, J=2.4Hz), 6.42(1H, d,
            J=7.2Hz), 7.21(2H, t, J=2.4Hz), 7.56(1H, t, J=7.8Hz),
            7.68(1H, d, J=7.8Hz), 8.38(1H, dd, J=7.8, 1.2Hz),
            8.43(1H, s); IR(CHCl3) 3450, 3103, 3022, 2954,
            2875, 1732, 1651, 1518, 1456, 1373, 1221, 1188, 1163,
            1057cm−1; [α]D22.0+39.9±0.8°(c=1.006, MeOH) Anal.
            (C26H30N2O6S2.0.1H2O) Calcd.(%): C, 58.65; H, 5.72; N,
            5.26; S, 12.04 Found(%): C, 58.40; H, 5.82; N, 5.08; S,
            11.88
I-7M-389a   mp 94-96° C.; 1H-NMR(CDCl3) δ 0.99(1H, m), 1.21-1.27
            (2H, m), 1.38-1.46(6H, m), 1.55-1.68(4H, m), 1.99(1H,
            m), 2.23(3H, s), 2.46(1H, m), 3.21(2H, t, J=8.7Hz),
            3.46-3.57(2H, m), 3.83(1H, m), 4.05(2H, s), 4.62(2H, t,
            J=8.7Hz), 5.95(1H, d, J=7.8Hz), 6.90(1H, s), 6.96
            (1H, s), 7.07(1H, d, J=3.9Hz), 7.37(1H, d, J=3.9Hz);
            IR(Nujol) 3327, 3074, 2750, 2650, 2613, 2551, 1728,
            1604, 1562, 1234, 1223, 1136cm−1; [α]D23+35.5±0.7°
            (c=1.014, MeOH) Anal.(C27H33NO5S2) Calcd.(%): C,
            62.88; H, 6.45; N, 2.72; S, 12.44 Found(%): C, 62.96; H,
            6.46; N, 2.68; S, 12.33
I-7M-390a   mp 99-101° C.; 1H-NMR(CDCl3) δ 0.99(1H, m), 1.20-
            1.27(2H, m), 1.37-1.45(6H, m), 1.54-1.63(4H, m), 1.98
            (1H, m), 2.39(3H, s), 2.46(1H, m), 3.46-3.56(2H, m), 3.83
            (1H, m), 4.04(2H, s), 5.95(1H, d, J=7.8Hz), 6.72(1H,
            d, J=2.1Hz), 7.09(1H, m), 7.18(1H, d, J=3.9Hz), 7.33
            (1H, m), 7.39(1H, d, J=3.9Hz), 7.63(1H, d, J=2.1Hz);
            IR(CHCl3) 3508, 3444, 3425, 2667, 2567, 1780,
            1732, 1645, 1531, 1500, 1421, 1321, 1130cm−1;
            [α]D24+36.1±0.8°(c=1.008, MeOH) Anal.
            (C27H31NO5S2.0.2H2O) Calcd.(%): C, 62.69; H, 6.12; N,
            2.71; S, 12.40 Found(%): C, 62.54; H, 5.98; N, 2.68; S,
            12.55

[0257]

TABLE 39
Compd. No.. Physical property
I-7M-391a   1                  H-NMR(CDCl3) δ 1.06(1H, m), 1.24-1.29(2H, m), 1.38-1.47
            (6H, m), 1.55-1.59(4H, m), 2.00(1H, m), 2.32(3H, s),
            2.48(1H, m), 3.19(2H, t, J=8.7Hz), 3.52(2H, t, J=6.3Hz),
            3.83(1H, m), 4.05(2H, s), 4.72(2H, t, J=8.7Hz), 6.26(1H, d,
            J=7.8Hz), 7.22(1H, s), 7.43(1H, d, J=3.9Hz), 7.50(1H, s),
            7.70(1H, d, J=3.9Hz); IR(CHCl3) 3508, 3440, 3423, 3377,
            2567, 2463, 1778, 1732, 1653, 1529, 1504, 1481, 1327, 1151cm−1;
            [α]D25+40.6±0.8°(c=1.004, MeOH) Anal.
            (C27H33NO7S2.0.5H2O) Calcd.(%): C, 58.25; H, 6.16; N, 2.52; S, 11.52
            Found(%): C, 58.18; H, 6.07; N, 2.45; S, 11.55
I-7M-392a   mp 136-140° C.; 1H-NMR(CDCl3+CD3OD) δ 1.09(1H, m),
            1.22-1.29(2H, m), 1.33-1.43(5H, m), 1.52-1.58(4H, m), 1.96
            (1H, m), 2.48-2.51(2H, m)+2.51(3H, s), 3.42-3.53(2H, m),
            3.75(1H, m), 4.01(2H, s), 6.68(1H, d, J=7.2Hz), 6.78(1H,
            d, J=2.1Hz), 7.48(1H, d, J=3.9Hz), 7.64(1H, s), 7.74(1H,
            d, J=2.1Hz), 7.76(1H, s), 7.82(1H, d, J=3.9Hz); IR
            (Nujol) 3280, 3141, 3114, 3084, 2750, 2650, 2548, 1732,
            1618, 1566, 1460, 1323, 1223, 1153, 1126cm−1; [α]D25+
            40.5±0.8°(c=1.004, MeOH) Anal.(C27H31NO7S2.0.2H2O)
            Calcd.(%): C, 59.04; H, 5.76; N, 2.55; S, 11.68 Found(%): C,
            59.01; H, 5.77; N, 2.51; S, 11.50
I-7M-393a   mp 104-107° C.; 1H-NMR(CDCl3) δ 0.90(3H, t, J=7.4Hz),
            0.98(1H, m), 1.21-1.64(16H, m), 1.99(1H, m), 2.46-2.51(3H,
            m), 3.23(2H, t, J=8.7Hz), 3.49-3.55(2H, m), 3.84(1H, m),
            4.05(2H, s), 4.62(2H, t, J=8.7Hz), 5.92(1H, d, J=7.8Hz),
            6.93(1H, s), 6.98(1H, s), 7.07(1H, d, J=3.6Hz), 7.36(1H, d,
            J=3.6Hz); IR(CHCl3) 3444, 3425, 2569, 1780, 1732, 1643,
            1531, 1498, 1479, 1464, 1419, 1317, 1132cm−1; [α]D24+
            33.3±0.7°(c=1.009, MeOH) Anal.(C30H39NO5S2.0.2H2O)
            Calcd.(%): C, 64.19; H, 7.07; N, 2.50; S, 11.42 Found(%): C,
            64.09; H, 6.95; N, 2.55; S, 11.36
I-7M-396a   1                  H-NMR(CDCl3) δ 1.06(1H, m), 1.26-1.69(12H, m), 2.03
            (1H, m), 2.56(1H, m), 3.55(2H, t, J=5.1Hz), 4.00(1H, m),
            4.04(2H, s), 6.11(1H, d, J=8.1Hz), 6.88(1H, d, J=7.5Hz),
            7.07-7.19(3H, m), 7.34-7.42(3H, m), 7.89(1H, s), 8.03(1H,
            d, J=8.1Hz); IR(KBr) 3383, 3076, 2949, 2929, 2868, 2520,
            1736, 1604, 1550, 1487, 1466, 1390, 1298, 1281, 1248, 1213,
            1134cm−1; [α]D25.0+35.4±3.0°(c=0.26, MeOH) Anal.
            (C28H31NO5S.0.5H2O) Calcd.(%): C, 66.91; H, 6.42; N, 2.79; S,
            6.38 Found(%): C, 66.98; H, 6.35; N, 2.85; S, 6.29
I-7M-412a   1                  H-NMR(CDCl3) δ 1.05(1H, m), 1.22-1.70(12H, m), 2.01
            (1H, d, J=3.3Hz), 2.50(1H, brs), 3.53(2H, t, J=6.3Hz),
            3.92(1H, m), 4.05(2H, s), 6.11(1H, d, J=7.8Hz), 7.27-7.62
            (6H, m), 7.79(1H, d, J=1.8Hz); IR(CHCl3) 3444, 2954,
            1780, 1732, 1649, 1547, 1514, 1491, 1219, 1213, 1128cm−1;
            [α]D24+49.9±0.9°(c=1.008%, MeOH); Anal.
            (C24H29NO4S.0.3H2O) Calcd.(%) C, 66.58; H, 6.89; N, 3.24; S,
            7.41Found(%) C, 66.73; H, 6.90; N, 3.35 S, 7.29

[0258]

TABLE 40
Compd. No.. Physical property
I-7M-424a   1                  H-NMR(CDCl3) δ 1.00(1H, m), 1.22-1.64(12H, m), 1.98
            (1H, m), 2.55(1H, m), 3.48(2H, t, J=6.9Hz), 3.94(1H,
            m), 3.99(2H, s), 4.15(2H, s), 6.13(1H, d, J=8.1Hz),
            6.84(1H, d, J=2.1Hz), 7.20-7.30(5H, m), 7.74(1H, s),
            7.79(1H, d, J=2.1Hz); IR(KBr) 3433, 3246, 3024,
            2954, 2875, 1730, 1639, 1599, 1518, 1495, 1475, 1454,
            1421, 1352cm−1; [α]D26.0+34.0±0.7°(c=1.00, MeOH)
            Anal.(C29H33NO5S.0.6H2O) Calcd.(%): C, 67.18; H, 6.65;
            N, 2.70; S, 6.18 Found(%): C, 67.21; H, 6.66; N, 2.71; S,
            5.99
I-7M-446a   1                  H-NMR(CDCl3) δ 1.00(1H, m), 1.22-1.64(12H, m),
            1.98(1H, m), 2.55(1H, m), 3.47(2H, t, J=6.3Hz), 3.96
            (1H, m), 3.98(2H, s), 4.17(2H, s), 6.16(1H, d, J=8.1Hz),
            6.82(1H, d, J=2.4Hz), 6.99-7.22(4H, m), 7.76(1H,
            s), 7.82(1H, d, J=2.4Hz); IR(CHCl3) 3593, 3433, 3244,
            2954, 2875, 1728, 1639, 1599, 1518, 1491, 1456, 1421,
            1362cm−1; [α]D22.0+31.2±0.7°(c=1.01, MeOH) Anal.
            (C29H32FNO5S.0.9H2O) Calcd.(%): C, 64.28; H, 6.29; N,
            2.58; F, 3.51; S, 5.92 Found(%): C, 64.39; H, 6.29; N,
            2.52; F, 3.40; S, 5.72
I-7M-447a   1                  H-NMR(CDCl3) δ 1.04(1H, m), 1.22-1.69(12H, m), 2.03
            (1H, m), 2.55(1H, m), 3.55(2H, t, J=6.6Hz), 3.96(1H,
            m), 4.04(2H, s), 6.08(1H, d, J=7.8Hz), 7.16(1H, dd, J=
            8.7 and 2.7Hz), 7.25-7.35(5H, m), 7.88(1H, s), 8.03
            (1H, dd, J=9.6 and 2.7Hz); IR(CHCl3) 3510, 3438,
            2954, 2875, 1780, 1732, 1655, 1591, 1558, 1514, 1477,
            1441, 1383cm−1; [α]D24.0+38.1±0.8°(c=1.01, MeOH)
            Anal.(C28H30FNO4S2.0.9H2O) Calcd.(%): C, 61.83; H,
            5.89; N, 2.58; F, 3.49; S, 11.79 Found(%): C, 61.91; H,
            5.73; N, 2.65; F, 3.56; S, 11.67
I-7M-448a   1                  H-NMR(CDCl3) δ 1.05(1H, m), 1.22-1.63(12H, m), 2.00
            (1H, m), 2.53(1H, m), 3.54(2H, m), 3.90(1H, m), 4.04
            (2H, s), 6.19(1H, d, J=7.8Hz), 7.47-7.83(3H, m), 7.85
            (1H, dd, J=7.8 and 2.4Hz), 8.00-8.05(3H, m), 8.38(1H,
            dd, J=9.3 and 2.4Hz); IR(CHCl3) 3437, 3386, 2954,
            2875, 1780, 1730, 1655, 1601, 1518, 1477, 1446, 1396,
            1325, 1309cm−1; [α]D24.0+31.5±0.7°(c=1.01, MeOH)
            Anal.(C28H30FN6S2.0.9H2O) Calcd.(%):
            C, 58.40; H, 5.57; N, 2.43; F, 3.30; S, 11.14 Found(%):
            C, 58.43; H, 5.54; N, 2.38; F, 3.16; S, 10.78
I-7N-1a     1                  H-NMR(CDCl3) δ 1.10-1.70(7H, m), 2.00-2.32(3H, m),
            2.51(1H, m), 3.83(1H, m), 4.07-4.21(4H, m), 5.54-5.70
            (2H, m), 6.26(1H, d, J=7.5Hz), 6.32-6.35(2H, m),
            7.15-7.18(2H, m), 7.38(1H, d, J=4.2Hz), 7.57(1H, d, J=
            4.2Hz); IR(CHCl3) 3440, 1732, 1655, 1531, 1506,
            1456, 1383, 1192, 1167, 1057, 1034cm−1;
            [α]D24+67.3±1.1°(c=1.005, MeOH) Anal.
            (C22H26N2O6S2.0.3H2O) Calcd.(%): C, 54.60; H, 5.54; N,
            5.79; S, 13.25 Found(%): C, 54.58; H, 5.50; N, 5.65; S,
            13.15

[0259]

TABLE 41
No. fo Compd. Physical property
I-7N-1b       1                  H-NMR(CDCl3) δ 1.16-1.70(7H, m), 2.04(1H, m), 2.12-2.18(2H, m),
              2.56(1H, brs), 3.72(3H, s), 3.78(1H, m),
              4.05-4.16(4H, m), 5.57-5.76(2H, m), 6.32-6.34(2H, m),
              6.39(1H, d, J=6.6Hz), 7.15-7.17(2H, m), 7.40(1H, d, J=
              3.9Hz), 7.56(1H, d, J=3.9Hz)
I-7P-1a       1                  H-NMR(CD3OD) δ 1.28-1.64(8H, m), 2.02-2.13(3H, m),
              2.47(1H, m), 3.71(1H, m), 3.98(2H, s), 4.25(2H, d, J=
              22.2Hz), 5.30(1H, dt, J=8.4 and 22.2Hz), 6.36(2H, m),
              7.23(2H, m), 7.70(1H, d, J=3.9Hz), 7.75(1H, d, J=3.9Hz);
              IR(CHCl3) 3419, 2956, 1635, 1604, 1537, 1508, 1456,
              1431, 1381, 1167, 1076, 1057, 1036cm−1; [α]D25+45.7±0.8°
              (c=1.02, MeOH)
I-7P-1e       1                  H-NMR(CDCl3) δ 1.10-1.72(7H, m), 2.06-2.26(3H, m),
              2.51(1H, m), 3.29(3H, s), 3.84(1H, m), 4.01-4.31(4H, m),
              5.36(1H, dt, J=9.0 and 20.7Hz), 6.15(1H, d, J=6.6Hz),
              6.34(2H, m), 7.16(2H, m), 7.38(1H, d, J=4.2Hz), 7.58
              (1H, d, J=4.2Hz), 9.26(1H, s); IR(CHCl3) 3442, 3352,
              2956, 2829, 1728, 1655, 1531, 1506, 1456, 1452, 1402,
              1383, 1348, 1167, 1109, 1057, 1034cm−1; [α]D25+51.8±0.9°
              (c=1.03, MeOH) Anal.(C23H28FN3O7S30.5MeOH)
              Calcd.(%): C, 47.86; H, 5.13; N, 7.13; F, 3.22; S, 16.31
              Found(%): C, 48.09; H, 5.02; N, 7.38; F, 3.12; S, 16.12
I-7R-1a       1                  H-NMR(CDCl3) δ 1.02(1H, m), 1.23-1.72(12H, m), 2.02
              (1H, d, J=3.9Hz), 2.48(1H, brs), 2.63(2H, t, J=7.2Hz),
              3.21(2H, s), 3.83(1H, m), 6.17(1H, d, J=7.5Hz), 6.32-6.35
              (2H, m), 7.15-7.17(2H, m), 7.37(1H, d, J=3.9Hz),
              7.57(1H, d, J=3.9Hz); IR(Nujol) 3348, 2924, 1711,
              1641, 1622, 1550, 1541, 1456, 1375, 1290, 1190, 1167, 1057cm−1;
              [α]D25+42.8±0.8°(c=1.005%, MeOH); Anal.
              (C22H28N2O5S3) Calcd.(%) C, 53.20; H, 5.68; N, 5.64; S,
              19.37 Found(%) C, 53.41; H, 5.58; N, 5.54; S, 19.08
I-7R-88a      1                  H-NMR(CDCl3) δ 0.99(1H, m), 1.21-1.72(12H, m), 1.98
              (1H, d, J=3.9Hz), 2.47(1H, brs), 2.64(2H, t, J=7.2Hz),
              3.20(2H, s), 3.87(1H, m), 4.16(2H, s), 5.96(1H, d, J=7.5Hz),
              6.79(1H, d, J=3.6Hz), 6.96(1H, d, J=4.8Hz), 7.06
              (1H, d, J=2.1Hz), 7.26-7.30(2H, m), 7.37(1H, d, J=3.9Hz);
              IR(CHCl3) 2877, 1711, 1641, 1545, 1508, 1458, 1298,
              1282, 1225, 1205cm−1; [α]D25+42.8±0.8°(c=1.005%,
              MeOH); Anal.(C23H29NO3S3.0.2H2O) Calcd.(%) C, 59.12;
              H, 6.34; N, 3.00; S, 20.59 Found(%) C, 59.18; H, 6.01; N,
              3.04; S, 20.28
I-7R-270a     1                  H-NMR(CDCl3) δ 1.03(1H, br), 1.18-1.70(12H, m), 2.01
              (1H, brd), 2.41(6H, s), 2.46(1H, brs), 2.62(2H, t, J=7.2Hz),
              3.21(2H, s), 3.82(1H, m), 5.88(2H, s), 6.23(1H, d, J=
              7.2Hz), 7.36(1H, d, J=3.9Hz), 7.49(1H, d, J=3.9Hz);
              IR(CHCl3) 3508, 3442, 2673, 1709, 1657, 1531, 1504, 1375,
              1180, 1119cm−1; [α]D26+39.2±0.8°(c=1.010, MeOH) Anal.
              (C24H32N2O5S3.0.3H2O) Calcd.(%): C, 54.94; H, 6.15; N,
              5.34; S, 18.33 Found(%): C, 54.44; H, 6.04; N, 5.28; S,
              18.08

[0260]

TABLE 42
Compd. No.. Physical property
I-7R-307a   1                  H-NMR(CDCl3) δ 0.93(1H, m), 1.17-1.22(2H, m), 1.34-1.41(6H, m),
            1.52-1.58(4H, m), 1.94(1H, m), 2.43(1H, m), 2.59
            (2H, t, J=7.2Hz), 3.16(2H, s), 3.79(1H, m), 3.97(3H, s),
            4.59(2H, s), 5.90(1H, d, J=7.8Hz), 6.74(1H, d, J=3.9Hz),
            7.29(1H, d, J=3.9Hz), 7.29-7.36(2H, m,), 7.46(1H, m),
            7.78-7.83(2H, m), 7.92(1H, d, J=8.4Hz); IR(CHCl3) 3446,
            3425, 3062, 2877, 2673, 1711, 1639, 1597, 1542, 1512, 1265,
            1254cm−1; [α]D25.5+35.8±0.8°(c=1.007, MeOH) Anal.
            (C30H35NO4S2.0.2H2O) Calcd.(%): C, 66.56; H, 6.59; N, 2.59; S, 11.85
            Found(%): C, 66.53; H, 6.70; N, 2.65; S, 11.78
I-8B-1a     1                  H-NMR(CDCl3) δ 1.06(1H, m), 1.19-1.30(2H, m), 1.34-1.44
            (4H, m), 1.54-1.68(4H, m), 2.04-2.12(5H, m), 2.35(2H, t, J=
            7.5Hz), 2.51(1H, brs), 3.82(1H, m), 5.29-5.42(2H, m), 6.21
            (1H, d, J=6.9Hz), 6.32-6.34(2H, m), 7.15-7.17(2H, m), 7.35
            and 7.56(each 1H, each d, each J=3.9Hz); IR(CHCl3) 3512,
            3442, 2679, 1707, 1657, 1529, 1504, 1456, 1383, 1192, 1167,
            1057, 1034cm−1; [α]D24+69.7±1.1°(c=1.004, MeOH) Anal.
            (C24H30N2O5S2.0.2H2O) Calcd.(%): C, 58.32; H, 6.20; N, 5.67;
            S, 12.98 Found(%): C, 58.30; H, 6.07; N, 5.67; S, 12.84
I-8C-1a     1                  H-NMR(CDCl3) δ 1.01(1H, m), 1.25-1.45(10H, m), 1.53-1.66
            (4H, m), 2.00(1H, m), 2.48(1H, m), 3.52(2H, t, J=7.1Hz),
            3.80(1H, m), 4.08(2H, s), 6.22(1H, d, J=7.5Hz),
            6.33-6.34(2H, m), 7.15-7.17(2H, m), 7.38(1H, d, J=3.9Hz),
            7.57(1H, d, J=3.9Hz); IR(CHCl3) 3440, 3145, 2578,
            1780, 1730, 1657, 1529, 1383, 1192, 1167, 1057cm−1; [α]D25.0+
            45.0±0.8°(c=1.010, MeOH) Anal.(C23H30N2O6S2.0.4H2O)
            Calcd.(%): C, 55.05; H, 6.19; N, 5.58; S, 12.78 Found(%): C,
            55.09; H, 6.08; N, 5.61; S, 12.74
I-8C-88a    1                  H-NMR(CDCl3) δ 0.97(1H, m), 1.23-1.47(10H, m), 1.55-1.61
            (4H, m), 1.97(1H, m), 2.48(1H, m), 3.52(2H, t, J=6.6Hz),
            3.83(1H, m), 4.06(2H, s), 4.16(2H, s), 5.93(1H, d, J=
            7.8Hz), 6.79(1H, dt, J=3.9, 0.9Hz), 6.96(1H, dd, J=5.1, 1.2Hz),
            7.06(1H, m), 7.29(1H, dd, J=5.1, 3.0Hz), 7.37(1H, d, J=
            3.9Hz); IR(CHCl3) 3444, 3427, 3107, 3022, 2954, 2875,
            1780, 1732, 1643, 1545, 1506, 1221, 1211, 1128cm−1; [α]D25.0+
            39.6±0.8°(c=1.016, MeOH) Anal.(C24H31NO4S2.0.3H2O)
            Calcd.(%): C, 61.72; H, 6.82; N, 3.00; S, 13.73 Found(%): C,
            61.79; H, 6.69; N, 3.11; S, 13.59
I-9B-1a     1                  H-NMR(CDCl3) δ 1.06(1H, m), 1.22-1.45(8H, m), 1.59-1.67
            (4H, m), 2.03-2.13(5H, m), 2.33(2H, t, J=7.5Hz), 2.52(1H,
            brs), 3.82(1H, m), 5.26-5.42(2H, m), 6.18(1H, d, J=7.2Hz),
            6.33-6.34(2H, m), 7.15-7.17(2H, m), 7.36 and 7.57(each 1H,
            each d, each J=3.9Hz); IR(CHCl3) 3514, 3442, 2677, 1709,
            1657, 1529, 1504, 1456, 1383, 1192, 1167, 1057, 1034cm−1;
            [α]D24.5+72.2±1.1°(c=1.006, MeOH) Anal.(C25H32N2O5S2)
            Calcd.(%): C, 59.50; H, 6.39; N, 5.55; S, 12.71 Found(%): C,
            59.24; H, 6.48; N, 5.60; S, 12.46

[0261]

TABLE 43
Compd. No.. Physical property
II-4A-55a   1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.09 and
            1.22(3H, s), 1.40-2.40(12H, m), 2.38(3H, s), 4.17(1H,
            m), 4.56(1H, brs), 5.98(1H, m), 6.19(1H, t, J=3.0Hz),
            6.24(1H, d, J=8.7Hz), 7.17(1H, dd, J=1.5, 3.3Hz),
            7.31(1H, d, J=3.9Hz), 7.51(1H, d, J=3.9Hz); IR
            (CHCl3) 3446, 1709, 1657, 1529, 1504, 1375, 1182, 1161,
            1144, 1053cm−1; [α]D23+28.9±0.7°(c=1.011, MeOH)
            Anal.(C23H30N2O5S2.0.4H2O) Calcd.(%): C, 56.86 H,
            6.39; N, 5.77; S, 13.20 Found(%): C, 57.24; H, 6.36; N,
            5.73; S, 12.72.
II-4B-55a   1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.5Hz), 1.10(3H, s),
            1.23(3H, s), 1.43-2.35(10H, m), 2.38(3H, s), 4.20(1H,
            m), 4.96(1H, dt, J=11.4 and 49.2Hz), 5.98(1H, m),
            6.19-6.21(2H, m), 7.17(1H, m), 7.29(1H, d, J=3.9Hz),
            7.51(1H, d, J=3.9Hz); IR(CHCl3) 3446, 2925, 2870,
            1730, 1657, 1529, 1504, 1471, 1375, 1159, 1144, 1053,
            1022cm−1; [α]D24+24.6±0.6°(c=1.04, MeOH) Anal.
            (C23H29FN2O5S2.0.6MeOH) Calcd.(%): C, 54.95;
            H, 6.14; N, 5.43; F, 3.68; S, 12.43 Found(%): C, 54.94;
            H, 5.97; N, 5.65; F, 3.55; S, 12.24
II-4C-55a   1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.5Hz), 1.10 and
            1.24(3H, s), 1.56(1H, ddd, J=2.7, 5.7, 12.0Hz), 1.96-2.70
            (8H, m), 2.37(3H, s), 4.25(1H, m), 5.88(1H, brd, J=
            15.9Hz), 5.99(1H, m), 6.17-6.21(2H, m), 7.03(1H, dt,
            J=7.2, 15.9Hz), 7.17(1H, dd, J=1.5, 3.3Hz), 7.27(1H,
            d, J=3.9Hz), 7.47(1H, d, J=3.9Hz); IR(CHCl3) 3446, 1697,
            1655, 1529, 1504, 1375, 1182, 1161, 1144, 1053cm−1;
            [α]D23+5.4±0.5°(c=1.002, MeOH) Anal.
            (C23H28N2O5S2.0.4H2O) Calcd.(%):C, 57.10; H, 6.00; N,
            5.79; S, 13.26 Found(%): C, 57.14; H, 5.89; N, 5.78; S,
            13.01.
II-4D-55a   1                  H-NMR(CDCl3) δ 0.97(1H, d, J=10.5Hz), 1.09 and
            1.23(3H, s), 1.60(1H, ddd, J=2.7, 5.7, 10.8Hz), 1.96-2.40
            (6H, m), 2.39(3H, s), 2.72-3.01(2H, m), 4.25(1H,
            m), 5.85(1H, brd, J=11.7Hz), 5.98(1H, m), 6.17-6.21
            (2H, m), 6.40(1H, dt, J=7.8, 11.7Hz), 7.18(1H, dd, J=
            1.8, 3.3Hz), 7.32(1H, d, J=4.2Hz), 7.54(1H, d, J=4.2Hz);
            IR(CHCl3) 3519, 3446, 1697, 1658, 1529, 1504,
            1375, 1182, 1161, 1144, 1053cm−1; [α]D23+63.6±1.0°
            (c=1.006, MeOH) Anal.(C23H328N2O5S2.0.3H2O)
            Calcd.(%): C, 57.31; H, 5.98; N, 5.81; S, 13.30 Found(%):
            C, 57.48; H, 5.93; N, 5.75; S, 12.90

[0262]

TABLE 44
Compd. No.. Physical property
II-4F-55a   1                  H-NMR(CDCl3) δ 0.94(1H, d, J=10.5Hz), 1.09(3H, s),
            1.24(3H, s), 1.59(1H, m), 2.03-2.34(5H, m), 2.39(3H,
            s), 2.62(1H, m), 2.92(1H, m), 4.26(1H, m), 5.99(1H, m),
            6.06(1H, dt, J=8.4 and 21.0Hz), 6.20(1H, m), 7.18
            (1H, m), 7.28(1H, m), 7.33(1H, d, J=3.9Hz), 7.53(1H,
            d, J=3.9Hz); IR(CHCl3) 33446, 2925, 2870, 1711, 1658,
            1529, 1504, 1442, 1375, 1161, 1070, 1053, 1018cm−1;
            [α]D25+52.9±0.9°(c=1.02, MeOH)
            Anal. (C23H27FN2O5S2.0.8MeOH) Calcd.(%):
            C, 54.95; H, 5.85; N, 5.38; F, 3.65; S, 12.33 Found(%):
            C, 54.72; H, 5.61; N, 5.67; F, 3.43; S, 12.16
II-5A-1a    1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.08(3H, s),
            1.22(3H, s), 1.33-2.38(14H, m), 4.18(2H, s), 6.08(1H,
            d, J=9.0Hz), 6.34(2H, t, J=2.4Hz), 7.16(2H, t, J=2.4Hz),
            7.28(1H, d, J=3.9Hz), 7.57(1H, d, J=3.9Hz); IR
            (CHCl3) 3512, 3446, 1709, 1657, 1504, 1456, 1385, 1192,
            1167, 1057, 1034cm−1; [α]D25.0+26.2±0.7°(c=1.008,
            MeOH) Anal.(C23H30N2O5S2.0.6H2O.0.3AcOEt)
            Calcd.(%): C, 56.33; H, 6.65; N, 5.45; S, 12.40 Found(%):
            C, 56.31; H, 6.35; N, 5.64; S, 12.08
II-5A-31a   1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.08(3H, s),
            1.20(3H, s), 1.30-2.38(14H, m), 4.13(2H, s), 4.18(1H,
            m), 5.93(1H, d, J=10.2Hz), 6.77(1H, d, J=3.6Hz),
            7.20-7.38(6H, m); IR(CHCl3) 3512, 3450, 3431, 1709,
            1643, 1543, 1506, 1456cm−1; [α]D24.0+20.4±0.6°
            (c=1.011, MeOH) Anal.(C26H33NO3S.0.6H2O) Calcd.(%):
            C, 71.04; H, 7.57; N, 3.19; S, 7.29 Found(%): C, 69.33;
            H, 7.65; N, 3.31; S, 7.11
II-5A-47a   1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.8Hz), 1.08(3H, s),
            1.21(3H, s), 1.30-2.38(14H, m), 4.19(1H, m), 6.08(1H,
            d, J=9.3Hz), 7.11(1H, dd, J=5.1, 3.9Hz), 7.32(1H, d,
            J=3.9Hz), 7.64(1H, d, J=3.9Hz), 7.69(1H, dd, J=
            5.1, 1.2Hz), 7.75(1H, dd, J=3.6, 1.2Hz); IR(CHCl3)
            3516, 3446, 2679, 1709, 1655, 1529, 1504, 1402, 1336,
            1153, 1095, 1074, 1024cm−1; [α]D24.0+23.5±0.6°
            (c=1.004, MeOH) Anal.(C23H29NO5S3.0.5H2O)
            Calcd.(%): C, 54.74; H, 5.99; N, 2.78; S, 19.06 Found(%):
            C, 54.90; H, 5.76; N, 2.85; S, 18.81
II-5A-55a   1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.09 and
            1.22(3H, s), 1.22-2.30(12H, m), 2.33(2H, t, J=7.5Hz),
            2.39(3H, s), 4.19(1H, m), 5.99(1H, m), 6.09(1H, d, J=
            8.7Hz), 6.20(1H, t, J=3.3Hz), 7.19(1H, dd, J=1.8, 6.3Hz),
            7.29(1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz); IR
            (CHCl3) 3446, 1709, 1657, 1529, 1504, 1375, 1205, 1182,
            1161, 1053cm−1; [α]D24+25.3±0.7°(c=1.002, MeOH)
            Anal.(C24H32N2O5S2) Calcd.(%): C, 58.51; H, 6.55; N,
            5.69; S, 13.02 Found(%): C, 58.21; H, 6.53; N, 5.69; S,
            12.93

[0263]

TABLE 45
Compd. No.. Physical property
II-5A-55c   1                  H-NMR(CDCl3) δ 0.89(1H, d, J=10.5Hz), 1.08(3H, s),
            1.22(3H, s), 1.36-2.36(14H, m), 2.39(3H, s), 4.16(1H,
            m), 5.24(1H, brs), 5.50(1H, brs), 5.99(1H, m), 6.20(1H,
            t, J=3.3Hz), 6.20(1H, brs), 7.19(1H, m), 7.32(1H, d, J=
            4.2Hz), 7.56(1H, d, J=4.2Hz); IR(CHCl3) 3529,
            3446, 3411, 3348, 1678, 1591, 1529, 1504, 1375, 1182,
            1161, 1144, 1053cm−1; [α]D26.0+23.0±0.6°(c=1.016,
            MeOH) Anal.(C24H33N3O4S2.0.4H2O) Calcd.(%): C,
            57.78; H, 6.83; N, 8.42; S, 12.86 Found(%): C, 57.79; H,
            6.81; N, 8.37; S, 12.68
II-5A-55g   1                  H-NMR(CDCl3) δ 0.89(1H, d, J=10.5Hz), 1.12(3H, s),
            1.25(3H, s), 1.33-2.35(12H, m), 2.39(3H, s), 2.95-3.11
            (2H, m), 4.19(1H, m), 6.00(1H, m), 6.21(1H, t, J=3.3Hz),
            6.45(1H, d, J=8.7Hz), 7.18(1H, dd, J=3.3, 1.5Hz),
            7.38(1H, d, J=3.9Hz), 7.54(1H, d, J=3.9Hz); IR
            (CHCl3) 3149, 2624, 1641, 1533, 1508, 1375, 1205, 1182,
            1160cm−1; [α]D25.0+17.9±0.6°(c=1.018, MeOH) Anal.
            (C24H32N6O3S2.0.4CHCl3) Calcd.(%): C, 51.62;
            H, 5.79; N, 14.89; S, 11.36 Found(%): C, 51.53; H, 5.99;
            N, 14.82; S, 11.09
II-5A-59a   1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.07(3H, s),
            1.21(3H, s), 1.28-2.36(14H, m), 4.17(1H, m), 5.91(1H,
            d, J=8.4Hz), 7.00(1H, dd, J=5.4, 3.6Hz), 7.05(1H, d,
            J=3.9Hz), 7.25(1H, d, J=3.9Hz), 7.28(1H, dd, J=
            3.6, 1.2Hz), 7.42(1H, dd, J=5.4, 1.2Hz); IR(CHCl3)
            3516, 3450, 3431, 2671, 1709, 1645, 1529, 1500, 1471,
            1421cm−1; [α]D25.0+23.3±0.6°(c=1.013, MeOH) Anal.
            (C23H29NO3S3.0.2H2O) Calcd.(%): C, 59.12; H, 6.34; N,
            3.00; S, 20.58 Found(%): C, 59.12; H, 6.30; N, 3.07; S,
            20.84
II-5A-88a   1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.09(3H, s),
            1.21(3H, s), 1.18-2.33(14H, m), 4.15(2H, s), 4.19(1H,
            m), 5.94(1H, d, J=9.6Hz), 6.79(1H, d, J=3.6Hz),
            6.96(1H, dd, J=5.1, 1.2Hz), 7.05(1H, dd, J=1.8, 1.2Hz),
            7.28(1H, dd, J=5.1, 1.8Hz), 7.30(1H, d, J=3.6Hz);
            IR(CHCl3) 3516, 3450, 3431, 1709, 1641, 1545,
            1506, 1471cm−1; [α]D24.0+19.6±0.6°(c=1.009, MeOH)
            Anal.(C24H31NO3S2.0.3H2O) Calcd.(%):
            C, 63.91; H, 7.06; N, 3.11; S, 14.22 Found(%): C, 63.89;
            H, 6.89; N, 3.31; S, 14.28
II-5A-104a  1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.10(3H, s),
            1.22(3H, s), 1.28-2.38(14H, m), 4.10(2H, s), 4.20(1H,
            m), 5.97(1H, d, J=9.6Hz), 6.70(1H, d, J=3.6Hz),
            6.95(1H, m), 7.04(1H, dd, J=3.3, 1.2Hz), 7.24(1H, d, J=
            3.6Hz), 7.37(1H, dd, J=5.1, 1.2Hz); IR(CHCl3) 3516,
            3450, 2669, 1709, 1643, 1543, 1508, 1471cm−1; [α]D25.0+
            20.8±0.6°(c=1.015, MeOH) Anal.(C24H31NO3S3.
            0.3H2O) Calcd.(%): C, 59.67; H, 6.59; N, 2.90; S, 19.91
            Found(%): C, 59.65; H, 6.49; N, 3.13; S, 20.18

[0264]

TABLE 46
Compd. No.. Physical property
II-5A-143a  1                  H-NMR(CDCl3) δ 0.95(1H, d, J=9.9Hz), 1.04(3H, s),
            1.23(3H, s), 1.32-2.40(14H, m), 4.24(2H, s), 4.32(1H,
            m), 6.11(1H, d, J=9.0Hz), 7.16-7.32(6H, m), 7.42(1H,
            dd, J=8.1, 7.2Hz), 7.76(1H, s), 8.18(1H, d, J=8.1Hz);
            IR(CHCl3) 3516, 3442, 1709, 1651,
            1513, 1495, 1471cm−1;
            [α]D24.0+31.6±0.7°(c=1.000, MeOH) Anal.
            (C30H35NO3S.0.3H2O) Calcd.(%): C, 72.78; H, 7.25; N,
            2.83; S, 6.48 Found(%): C, 72.79; H, 7.27; N, 2.87; S,
            6.44
II-5A-197a  1                  H-NMR(CDCl3) δ 0.90(1H, d, J=9.9Hz), 1.08(3H, s),
            1.20(3H, s), 1.30-2.36(14H, m), 3.22(2H, t, J=9.0Hz),
            4.07(2H, s), 4.18(1H, m), 4.57(2H, t, J=9.0Hz), 5.92
            (1H, d, J=8.4Hz), 6.78(1H, t, J=7.5Hz), 6.80(1H, d, J=
            3.9Hz), 6.95(1H, d, J=7.5Hz), 7.09(1H, d, J=7.5Hz),
            7.28(1H, d, J=3.9Hz); IR(CHCl3) 3516, 3450,
            3431, 1709, 1641, 1543, 1506, 1458cm−1; [α]D25.0+
            41.1±0.8°(c=1.002, MeOH) Anal.(C28H35NO4S.0.3H2O)
            Calcd.(%): C, 69.05; H, 7.37; N, 2.88; S, 6.58 Found(%):
            C, 69.05; H, 7.20; N, 3.06; S, 6.51
II-5B-55a   1                  H-NMR(CDCl3) δ 0.93(1H, d, J=10.5Hz), 1.08 and
            1.23(3H, s), 1.55(1H, m), 1.91-2.42(7H, m), 2.39(3H,
            s), 3.18(2H, d, J=6.6Hz), 4.20(1H, m), 5.56-5.73(2H,
            m), 5.99(1H, m), 6.18-6.23(2H, m), 7.19(1H, dd, J=1.5,
            3.3Hz), 7.30(1H, d, J=3.9Hz), 7.54(1H, d, J=3.9Hz);
            IR(CHCl3) 3446, 1711, 1657, 1529, 1504, 1375, 1182,
            1161, 1144, 1053cm−1;
            [α]D25+38.8±0.8°(c=1.001,
            MeOH) Anal.(C24H39N2O5S2.0.3H2O) Calcd.(%):
            C, 58.11; H, 6.22; N, 5.65; S, 12.93 Found(%): C, 58.13;
            H, 6.09; N, 5.68; S, 12.73.
II-5C-1a    1                  H-NMR(CDCl3) δ 0.95(1H, d, J=10.5Hz), 1.08(3H, s),
            1.23(3H, s), 1.42-2.33(10H, m), 4.22(1H, m), 5.78(1H,
            d, J= 15.9Hz), 6.07(1H, d, J=8.1Hz), 6.33(2H, t, J=
            2.4Hz), 7.03(1H, dt, J=15.9, 6.9Hz), 7.16(2H, t, J=
            2.4Hz), 7.28(2H, d, J=4.2Hz), 7.57(1H, d, J=4.2Hz);
            IR(CHCl3) 3523, 3446, 1697, 1655, 1529, 1504, 1456,
            1385, 1192, 1167, 1057, 1034cm−1; [α]D25.0+29.7±0.7°
            (c=1.005, MeOH) Anal.(C23H28N2O5S2.0.2H2O)
            Calcd.(%): C, 57.52; H, 5.96; N, 5.83; S, 13.35 Found(%):
            C, 57.51; H, 5.89; N, 5.88; S, 13.31
II-5C-55a   1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.5Hz), 1.09 and
            1.23(3H, s), 1.48-2.40(10H, m), 2.39(3H, s), 4.24(1H,
            m), 5.79(1H, d, J=15.6Hz), 5.99(1H, m), 6.09(1H, d, J=
            8.7Hz), 6.20(1H, t, J=3.6Hz), 7.03(1H, dt, J=6.9,
            15.6Hz), 7.19(1H, dd, J=1.8, 3.3Hz), 7.29(1H, d, J=
            4.2Hz), 7.55(1H, d, J=4.2Hz).; IR(CHCl3) 3446, 1697,
            1655, 1529, 1504, 1375, 1182, 1161, 1144, 1053cm−1;
            [α]D26.5+27.9±0.7°(c=1.005, MeOH) Anal.
            (C24H39N2O5S2.0.3H2O) Calcd.(%): C, 58.11; H, 6.22; N,
            5.65; S, 12.93 Found(%): C, 58.12; H, 6.22; N, 5.62; S,
            12.91.

[0265]

TABLE 47
Compd.
No..      Physical property
II-5E-1a  mp 154-155° C.; 1H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz),
          1.10 and 1.23(3H, s), 1.51(1H, ddd, J=2.1, 5.1, 12.9Hz),
          1.72-2.40(7H, m), 3.58-3.64(2H, m), 3.98 and 4.07(each 1H,
          Abq, J=16.8Hz), 4.23(1H, m), 6.27(1H, d, J=8.7Hz),
          6.32-6.35(2H, m), 7.15-7.17(2H, m), 7.31(1H, d, J=3.9Hz),
          7.55(1H, d, J=3.9Hz); IR(CHCl3) 3444, 1730, 1655, 1529,
          1504, 1456, 1385, 1192, 1167, 1057, 1034cm−1; [α]D24
          −2.2±0.4°(c=1.009, MeOH) Anal.(C22H28N2O6S2)
          Calcd.(%): C, 54.98 H, 5.87; N, 5.83; S, 13.34 Found(%):
          C, 54.97; H, 5.92; N, 5.89; S, 13.12
II-5E-55a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=9.9Hz), 1.10 and 1.23
          (3H, s), 1.51(1H, ddd, J=2.7, 4.8, 12.6Hz), 1.74-2.40(7H,
          m), 2.39(3H, s), 3.58-3.64(2H, m), 3.98 and 4.07(each 1H,
          Abq, J=17.1Hz), 4.23(1H, m), 5.99(1H, m), 6.20(1H, t, J=
          3.6Hz), 6.29(1H, d, J=8.1Hz), 7.19(1H, dd, J=1.5, 3.3Hz),
          7.33(1H, d, J=3.9Hz), 7.53(1H, d, J=3.9Hz); IR
          (CHCl3) 3444, 1729, 1655, 1529, 1504, 1375, 1182, 1161,
          1142, 1053cm−1; [α]D24 −2.8±0.4°(c=1.013, MeOH) Anal.
          (C23H30N2O6S2.1.2H2O) Calcd.(%): C, 53.51;
          H, 6.33; N, 5.43; S, 12.42
          Found(%): C, 53.53; H, 5.93; N, 5.45; S, 12.55
II-5F-31a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.09 and 1.22
          (3H, s), 1.47(1H, ddd, J=2.4, 4.8, 12.9Hz), 1.74(1H, m),
          1.91-2.38(6H, m), 2.61-2.80(2H, m), 3.49(2H, s), 4.13(2H,
          s), 4.21(1H, m), 6.07(1H, d, J=8.4Hz), 6.77(1H, dt, J=0.9,
          3.6Hz), 7.22-7.35(6H, m); IR(CHCl3) 2924, 1711, 1641,
          1543, 1508, 1471, 1454, 1286, 1257, 1227,
          1223cm−1; [α]D26+
          30.7±1.4°(c=0.512%, MeOH);
          Anal.(C25H31NO3S2.0.3H2O)
          Calcd.(%) C, 64.85; H, 6.88; N, 3.02; S, 13.85 Found(%) C,
          64.73; H, 6.81; N, 3.13; S, 13.81
II-5F-55a 1                  H-NMR(CDCl3) δ 0.90(1H, d, 10.2Hz), 1.10 and 1.23(3H,
          s), 1.49(1H, ddd, J=2.7, 5.7, 13.5Hz), 1.64-2.38(7H, m),
          2.39(3H, s), 2.60-2.80(2H, m), 3.21(2H, ABq, J=15.0Hz),
          4.19(1H, m), 5.98(1H, m), 6.20(1H, t, J=3.0Hz), 6.25(1H,
          d, J=8.4Hz), 7.18(1H, m), 7.33(1H, d, J=4.2Hz), 7.53
          (1H, d, J=4.2Hz); IR(CHCl3) 2925,
          1710, 1657, 1529, 1504,
          1375, 1227, 1213, 1207, 1182, 1161cm−1;
          [α]D26+29.6±1.4°
          (c=0.503%, MeOH);
          Anal.(C23H30N2O5S3.0.4H2O) Calcd.(%)
          C, 53.34; H, 5.99; N, 5.41; S, 18.57 Found(%) C, 53.41; H,
          6.01; N, 5.47; S, 18.65
II-5F-88a 1                  H-NMR(CDCl3) δ 0.91(1H, d, 10.2Hz), 1.10 and 1.22(3H,
          s), 1.48(1H, m), 1.67-2.38(7H, m), 2.60-2.80(2H, m), 3.21
          (2H, br s), 4.18(2H, d, J=0.9Hz), 4.22(1H, m), 6.08(1H, d,
          J=8.4Hz), 6.79(1H, dt, J=0.9, 3.6Hz), 6.96(1H, dd, J=
          1.5, 5.1Hz), 7.05(1H, m), 7.27-7.33(2H, m);
          IR(CHCl3) 2923, 1710, 1643, 1543, 1508, 1471,
          1286, 1221, 1205cm−1;
          [α]D26+30.3±1.4°(c=0.508%, MeOH); Anal.
          (C23H29NO3S3.0.2H2O)
          Calcd.(%) C, 59.12; H, 6.34; N, 3.00; S,
          20.59 Found(%) C, 59.10; H, 6.31; N, 3.09; S, 20.47

[0266]

TABLE 48
Compd.
No..      Physical property
II-6A-55a 1                  H-NMR(CDCl3) δ 0.88(1H, d, J=10.2Hz), 1.08 and
          1.21(3H, s), 1.22-2.36(16H, m), 2.38(3H, s), 4.16(1H,
          m), 5.98(1H, m), 6.19(1H, t, J=3.3Hz), 6.30(1H, d, J=
          8.7Hz), 7.17(1H, dd, J=1.8, 3.3Hz), 7.33(1H, d, J=
          4.2Hz), 7.52(1H, d, J=4.2Hz); IR(CHCl3) 3446, 1709,
          1657, 1529, 1504, 1375, 1182, 1161, 1144, 1053cm−1;
          [α]D25+22.7±0.6°(c=1.002, MeOH) Anal.
          (C25H34N2O5S2.0.3H2O) Calcd.(%): C, 58.64; H, 6.81; N,
          5.47; S, 12.52 Found(%): C, 58.73; H, 6.68; N, 5.45; S,
          11.93.
II-6B-55a 1                  H-NMR(CDCl3) δ 0.94(1H, d, J=10.5Hz), 1.08 and
          1.22(3H, s), 1.55(1H, ddd, J=2.4, 5.7, 13.2Hz), 1.84-2.50
          (11H, m), 2.39(3H, s), 4.20(1H, m), 5.37-5.52(2H,
          m), 5.99(1H, m), 6.17-6.21(2H, m), 7.18(1H, dd, J=1.8,
          6.3Hz), 7.31(1H, d, J=4.2Hz), 7.54(1H, d, J=4.2Hz);
          IR(CHCl3) 3446, 1711, 1657, 1529, 1504, 1392, 1375,
          1182, 1161, 1144, 1053cm−1; [α]D25+44.6±0.8°(c=1.004,
          MeOH) Anal.(C25H32N2O5S2) Calcd.(%): C, 59.50; H,
          6.39; N, 5.55; S, 12.71 Found(%): C, 59.16; H, 6.27; N;
          5.54; S, 12.44
II-7A-31a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=9.9Hz), 1.08(3H, s),
          1.20(3H, s), 1.22-2.34(18H, m), 4.13(2H, s), 4.19(1H,
          m), 5.92(1H, d, J= 9.0Hz), 6.77(1H, d, J=3.6Hz),
          7.22-7.35(6H, m); IR(CHCl3) 3516, 3450, 3431, 1709,
          1641, 1545, 1506, 1469, 1456cm−1; [α]D24.0+20.4±0.6°
          (c=1.000, MeOH) Anal.(C28H37NO3S.0.2H2O) Calcd.(%):
          C, 71.36; H, 8.00; N, 2.97; S, 6.80 Found(%): C, 71.44;
          H, 7.99; N, 3.02; S, 6.69
II-7A-47a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.09(3H, s),
          1.21(3H, s), 1.22-2.33(18H, m), 4.19(1H, m), 6.06(1H,
          d, J= 9.0Hz), 7.11(1H, dd, J=5.1, 3.9Hz), 7.33(1H, d,
          J=3.9Hz), 7.65(1H, d, J=3.9Hz), 7.70(1H, dd, J=
          5.1, 1.5Hz), 7.76(1H, dd, J=3.6, 1.5Hz); IR(CHCl3)
          3516, 3446, 2679, 1709, 1657, 1529, 1504, 1402, 1336,
          1153, 1095, 1022cm−1; [α]D24.0 30 25.3±0.7°(c=1.004,
          MeOH) Anal.(C25H33NO5S3.0.3H2O) Calcd.(%): C, 56.75;
          H, 6.40; N, 2.65; S, 18.07 Found(%): C, 56.88; H, 6.43;
          N, 2.68; S, 17.79
II-7A-55a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.08 and
          1.22(3H, s), 1.22-2.32(18H, m), 2.39(3H, s), 4.18(1H,
          m), 4.65(1H, br s), 5.99(1H, m), 6.12(1H, d, J=9.0Hz),
          6.20(1H, t, J=3.6Hz), 7.03(1H, dt, J=6.9, 15.6Hz),
          7.19(1H, dd, J=1.8, 3.3Hz), 7.30(1H, d, J=4.2Hz),
          7.54(1H, d, J=3.9Hz); IR(CHCl3) 3446, 1708, 1657,
          1529, 1504, 1375, 1182, 1161, 1144, 1053cm−1;
          [α]D25+25.1±0.6°(c=1.009, MeOH) Anal.
          (C26H36N2O5S2.0.2H2O) Calcd.(%): C, 59.56; H, 7.00; N,
          5.34; S, 12.23 Found(%): C, 59.59; H, 7.01; N, 5.33; S,
          11.85.

[0267]

TABLE 49
Compd.
No..      Physical property
II-7A-55e 1                  H-NMR(CDCl3) δ 0.93(1H, d, J=10.2Hz), 1.10(3H, s),
          1.23(3H, s), 1.32-2.34(16H, m), 2.29(2H, d, J=7.5Hz),
          2.39(3H, s), 3.28(3H, s), 4.21(1H, m), 6.00(1H, m),
          6.17(1H, d, J=9.3Hz), 6.21(1H, m), 7.19(1H, m), 7.36
          (1H, d, J=3.9Hz), 7.56(1H, d, J=3.9Hz), 8.76(1H,
          br); IR(CHCl3) 3386, 2927, 2862, 1718, 1651, 1531,
          1506, 1398, 1375, 1344, 1159, 1053, 1020cm−1;
          [α]D24+20.8±0.6°(c=1.00, MeOH) Anal.
          (C27H39N3O6S3.0.5MeOH) Calcd.(%): C, 53.81; H, 6.73; N,
          6.85; S, 15.67 Found(%): C, 53.91; H, 6.64; N, 7.13; S,
          15.29
II-7A-55g 1                  H-NMR(CDCl3) δ 0.94(1H, d, J=10.5Hz), 1.13(3H, s),
          1.25(3H, s), 1.26-2.40(16H, m), 2.38(3H, s), 2.93-3.00
          (2H, m), 4.28(1H, m), 6.00(1H, m), 6.21(1H, t, J=3.3Hz),
          6.43(1H, d, J=8.7Hz), 7.17(1H, dd, J=3.3, 1.5Hz),
          7.42(1H, d, J=3.9Hz), 7.56(1H, d, J=3.9Hz); IR
          (CHCl3) 3426, 2626, 1639, 1533, 1508, 1375, 1222, 1216,
          1205, 1184, 1160cm−1; [α]D24.0+22.7±0.6°(c=1.002,
          MeOH) Anal.(C26H36N6O3S2.0.6H2O) Calcd.(%): C,
          56.21; H, 6.75; N, 15.03; S, 11.43 Found(%): C, 56.32; H,
          6.52; N, 14.80; S, 11.13
II-7A-59a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.07(3H, s),
          1.20(3H, s), 1.24-2.33(18H, m), 4.17(1H, m), 5.91(1H,
          d, J= 9.0Hz), 7.00(1H, dd, J=5.4, 3.6Hz), 7.05(1H, d,
          J=3.6Hz), 7.26(1H, d, J=3.6Hz), 7.28(1H, dd, J=
          3.6, 1.2Hz), 7.42(1H, dd, J=5.4, 1.2Hz); IR(CHCl3)
          3516, 3450, 3431, 2673, 1709, 1645, 1529, 1500, 1471,
          1421cm−1; [α]D25.0+20.1±0.6°(c=1.010, MeOH) Anal.
          (C25H33NO3S3) Calcd.(%): C, 61.06; H, 6.76; N, 2.85; S,
          19.56 Found(%): C, 60.86; H, 6.87; N, 2.93; S, 19.29
II-7A-88a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.09(3H, s),
          1.21(3H, s), 1.24-2.33(18H, m), 4.15(2H, s), 4.19(1H,
          m), 5.94(1H, d, J= 9.0Hz), 6.79(1H, d, J=3.6Hz), 6.96
          (1H, dd, J=5.1, 1.2Hz), 7.05(1H, m), 7.27(1H, dd, J=
          4.8, 1.2Hz), 7.30(1H, d, J=3.6Hz); IR(CHCl3) 3518,
          3450, 3431, 1709, 1641, 1545, 1506, 1469cm−1;
          [α]D24.0+19.2±0.6°(c=1.012, MeOH) Anal.
          (C26H35NO3S2.0.1H2O) Calcd.(%): C, 65.67; H, 7.46; N,
          2.95; S, 13.09 Found(%): C, 65.81; H, 7.43; N, 2.94; S,
          12.99
II-7A-    1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.5Hz),
104a      1.10(3H, s), 1.22(3H, s), 1.25-2.34(18H, m), 4.10(2H, s),
          4.20(1H, m), 5.95(1H, d, J=8.7Hz), 6.70(1H, d, J=3.3Hz),
          6.95(1H, dd, J=5.1, 3.9Hz), 7.04(1H, dd, J=3.9, 1.2Hz),
          7.25(1H, d, J=3.3Hz), 7.36(1H, dd, J=5.1, 1.2Hz);
          IR(CHCl3) 3516, 3450, 3431, 1709, 1643, 1543,
          1506, 1471cm−1; [α]D25.0+19.8±0.6°(c=1.009, MeOH)
          Anal.(C26H35NO3S3.0.1H2O) Calcd.(%): C, 61.53, H, 6.99,
          N, 2.76; S, 18.95 Found(%): C, 61.42; H, 6.85; N, 2.86; S,
          18.89

[0268]

TABLE 50
Compd.
No..       Physical property
II-7A-143a 1                  H-NMR(CDCl3) δ 0.96(1H, d, J=10.2Hz), 1.10(3H, s),
           1.23(3H, s), 1.26-2.38(18H, m), 4.24(2H, s), 4.32(1H,
           m), 6.11(1H, d, J= 8.7Hz), 7.19-7.28(6H, m), 7.42(1H,
           dd, J=8.1, 7.2Hz), 7.76(1H, s), 8.19(1H, d, J=8.1Hz);
           IR(CHCl3) 3516, 3442, 1709, 1651,
           1514, 1495, 1469cm−1;
           [α]D24.0+34.1±0.7°(c=1.004, MeOH) Anal.
           (C32H39NO3S.0.2H2O) Calcd.(%): C, 73.73; H, 7.62; N,
           2.69; S, 6.15 Found(%): C, 73.72; H, 7.68; N, 2.65; S,
           5.88
II-7A-197a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=9.9Hz), 1.08(3H, s),
           1.20(3H, s), 1.24-2.33(18H, m), 3.22(2H, t, J=8.7Hz),
           4.05(2H, s), 4.19(1H, m), 4.57(2H, t, J=8.7Hz), 5.92
           (1H, d, J=9.3Hz), 6.79(1H, t, J=7.2Hz), 6.80(1H, d, J=
           3.9Hz), 6.96(1H, d, J=7.2Hz), 7.09(1H, d, J=7.2Hz),
           7.28(1H, d, J=3.9Hz); IR(CHCl3) 3516, 3450,
           3431, 2671, 1709, 1639, 1543, 1506, 1458cm−1; [α]D25.0+
           17.4±0.6°(c=1.001, MeOH) Anal.(C30H39NO4S.0.3H2O)
           Calcd.(%): C, 69.95; H, 7.75; N, 2.72; S, 6.22 Found(%):
           C, 69.86; H, 7.65; N, 2.80; S, 6.08
II-7A-315a 1                  H-NMR(CDCl3) δ 0.96(1H, d, J=9.9Hz), 1.11(3H, s),
           1.24(3H, s), 1.33-2.36(16H, m), 2.3(2H, t, J=7.2Hz),
           4.26(2H, s), 4.33(1H, m), 6.12(1H, d, J=9.3Hz),
           7.00-7.23(5H, m), 7.42(1H, m), 7.78(1H, s), 8.20(1H, d,
           J=7.5Hz); IR(CHCl3) 3516, 3442, 2925, 2858, 1709,
           1651, 1585, 1570, 1514, 1492, 1469, 1396cm−1;
           [α]D25.5+33.4±0.7°(c=1.00, MeOH) Anal.
           (C32H38FNO3S.0.5MeOH) Calcd.(%):
           C, 70.75; H, 7.31; N,
           2.54; F, 3.44; S, 5.81 Found(%): C, 70.85; H, 7.34; N,
           2.80; F, 3.06; S, 5.66
II-7A-316a 1                  H-NMR(CDCl3) δ 0.96(1H, d, J=10.2Hz), 1.11(3H, s),
           1.24(3H, s), 1.32-2.36(16H, m), 2.30(2H, t, J=7.2Hz),
           3.82(3H, s), 4.23(2H, s), 4.33(1H, m), 6.12(1H, d, J=
           9.0Hz), 6.82-6.91(2H, m), 7.05-7.22(3H, m), 7.39(1H,
           m), 7.78(1H, s), 8.14(1H, d, J=8.1Hz); IR(CHCl3)
           3516, 3442, 2925, 2858, 1709, 1651, 1601, 1514, 1493,
           1468, 1439, 1394, 1246cm−1; [α]D26.0+31.4±0.7°(c=1.04,
           MeOH) Anal.(C33H41NO4S.0.1H2O) Calcd.(%): C, 72.12;
           H, 7.56; N, 2.55; S, 5.23 Found(%): C, 71.93; H, 7.73; N,
           2.77; S, 5.60
II-7B-55a  1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.08(3H, s),
           1.15(3H, d, J=7.2Hz), 1.22(3H, s), 1.29-2.45(17H, m),
           2.39(3H, s), 4.19(1H, m), 5.98(1H, d, J=2.4Hz), 6.06
           (1H, d, J=9.0Hz), 6.20(1H, dd, J=3.3 and 3.6Hz),
           7.19(1H, dd, J=2.4 and 3.3Hz), 7.29(1H, d, 3.9Hz),
           7.55(1H, d, J=3.9Hz); IR(CHCl3) 3448, 2927, 2860,
           1739, 1705, 1657, 1529, 1504, 1469, 1375, 1281, 1161,
           1144, 1070, 1053, 1022cm−1; [α]D24+21.4±0.6°(c=1.02,
           MeOH) Anal.(C27H38N2O5S2.0.3H2O) Calcd.(%): C,
           60.04; H, 7.20; N, 5.19; S, 11.87 Found(%): C, 60.26; H,
           7.22; N, 5.28; S, 11.50

[0269]

TABLE 51
Compd.
No..      Physical property
II-7E-55c 1                  H-NMR(CDCl3) δ 0.93(1H, d, J=10.5Hz), 1.08(3H, s),
          1.21(3H, s), 1.50-2.40(14H, m), 2.39(3H, s), 4.14(1H, m),
          5.24(1H, brs), 5.33-5.50(2H, m), 5.99(1H, m), 5.99(1H,
          brs), 6.20(1H, t, J=3.3Hz), 6.48(1H, d, J=7.2Hz), 7.19
          (1H, m), 7.39(1H, d, J=4.2Hz), 7.55(1H, t, J=4.2Hz);
          IR(CHCl3) 3527, 3485, 3448, 3411, 3348, 1676, 1591, 1529,
          1504, 1375, 1182, 1161, 1144, 1053cm−1;
          [α]D26.0+55.5±1.0°
          (c=1.010, MeOH) Anal.(C26H35N3O4S2.0.3H2O)
          Calcd.(%): C, 59.70; H, 6.86; N, 8.03; S, 12.26 Found(%):
          C, 59.79; H, 6.75; N, 8.05; S, 12.14
II-7E-55e mp 70-72° C.; 1H-NMR(CDCl3) δ 0.96(1H, d, J=10.8Hz),
          1.09(3H, s), 1.22(3H, s), 1.60-2.37(14H, m), 2.41(3H, s),
          3.25(3H, s), 4.10(1H, m), 5.28-5.47(2H, m), 6.00(1H, m),
          6.06(1H, d, J=8.7Hz), 6.22(1H, dd, J=3.3 and 3.6Hz),
          7.19(1H, dd, J=1.8 and 3.3Hz), 7.41(1H, d, J=3.9Hz),
          7.57(1H, d, J=3.9Hz); IR(CHCl3 ) 3427, 3386, 2927,
          1714, 1647, 1531, 1506, 1454, 1375, 1342, 1161, 1120,
          1053, 1020cm−1; [α]D24+50.0±0.9°(c=1.00, MeOH) Anal.
          (C27H37N3O6S3.0.4H2O) Calcd.(%): C, 53.78; H, 6.32; N,
          6.97; S, 15.95 Found(%): C, 53.89; H, 6.28; N, 7.05; S,
          15.57
II-7E-55g 1                  H-NMR(CDCl3) δ 0.76(1H, d, J=10.8Hz), 1.10(3H, s),
          1.24(3H, s), 1.44-2.31(12H, m), 2.40(3H, s), 2.92-3.08
          (2H, m), 3.98(1H, m), 5.37-5.39(2H, m), 6.01(1H, m), 6.22
          (1H, t, J=3.3Hz), 6.30(1H, d, J=8.4Hz), 7.19(1H, dd, J=
          3.3, 1.8Hz), 7.41(1H, d, J=3.9Hz), 7.58(1H, d, J=3.9Hz);
          IR(CHCl3) 3151, 1639, 1533, 1508, 1375, 1184, 1160cm−1;
          [α]D25.0+40.9±0.8°(c=1.010, MeOH) Anal.
          (C26H34N6O3 S2.1.3H2O) Calcd.(%): C, 55.16; H, 6.52; N,
          14.44; S, 10.43 Found(%): C, 55.44; H, 6.42; N, 14.17; S,
          10.66
II-7F-55a 1                  H-NMR(CDCl3) δ 0.94(1H, d, J=9.9Hz), 1.08(3H, s),
          1.16 or 1.18(3H, d, J=4.2Hz), 1.22(3H, s), 1.47-2.52
          (13H, m), 2.39(3H, s), 4.20(1H, m), 5.38-5.41(2H, m),
          5.99(1H, m), 6.14-6.21(2H, m), 7.19(1H, m), 7.31(1H, m),
          7.54(1H, m); IR(CHCl3) 3446, 2925, 2870, 1738, 1705,
          1657, 1529, 1504, 1469, 1375, 1182, 1161, 1144, 1070,
          1053, 1022cm−1; [α]D24+49.8±0.9°(c=1.02, MeOH) Anal.
          (C27H36N2O5S2.0.4H2O) Calcd.(%): C, 60.06; H, 6.87; N,
          5.19; S, 11.88 Found(%): C, 60.03; H, 6.71; N, 5.31; S,
          11.76
II-7I-1a  mp 111-115° C.; 1H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz),
          1.09 and 1.22(3H, s), 1.22-2.40(12H, m), 4.19(1H,
          m), 5.79(1H, br d, J=15.6Hz), 6.06(1H, d, J=9.3Hz),
          6.32-6.35(2H, m), 7.03(1H, dt, J=7.8, 15.6Hz), 7.15-7.17
          (2H, m), 7.27(1H, d, J=3.9Hz), 7.57(1H, d, J=3.9Hz);
          IR(CHCl3) 3446, 1695, 1654, 1529, 1504, 1456, 1385, 1192,
          1167, 1057, 1034cm−1; [α]D25+20.5±0.6°(c=1.007, MeOH)
          Anal.(C25H32N2O5S2) Calcd.(%): C, 59.50; H, 6.39; N, 5.55;
          S, 12.71 Found(%): C, 59.19; H, 6.39; N, 5.48; S, 12.39

[0270]

TABLE 52
Compd.
No..      Physical property
II-7I-47a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.8Hz), 1.09 and
          1.22(3H, s), 1.22-2.40(12H, m), 4.20(1H, m), 5.79(1H,
          br d, J=15.6Hz), 5.99(1H, m), 6.08(1H, d, J=9.0Hz),
          7.03(1H, dt, J=7.2, 15.6Hz), 7.11(1H, dd, J=3.9, 5.1Hz),
          7.33(1H, d, J=3.9Hz), 7.65(1H, d, J=3.9Hz) 7.70
          (1H, dd, J=1.2, 6.0Hz), 7.76(1H, dd, J=1.2, 3.9Hz);
          IR(CHCl3) 3446, 2680, 1695, 1655, 1529, 1504, 1336,
          1153, 1022cm−1; [α]D24+20.2±0.6°(c=1.000, MeOH)
          Anal.(C25H31NO5S3.0.3H2O) Calcd.(%): C, 56.96; H, 6.04;
          N, 2.66; S, 18.25 Found(%):C, 57.07; H, 6.12; N, 2.72; S,
          17.88
II-7I-55a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.09 and
          1.22(3H, s), 1.22-2.40(12H, m), 2.39(3H, s), 4.20(1H,
          m), 5.79(1H, br d, J=15.6Hz), 5.99(1H, m), 6.06(1H,
          d, J=9.0Hz), 6.20(1H, t, J=3.6Hz), 7.03(1H, dt, J=
          6.9, 15.6Hz), 7.19(1H, dd, J=1.8, 3.3Hz), 7.29(1H, d,
          J=3.9Hz), 7.55(1H, d, J=3.9Hz); IR(CHCl3) 3448,
          1695, 1655, 1529, 1504, 1375, 1182, 1161, 1144, 1053cm−1;
          [α]D25+19.7±0.6°(c=1.007, MeOH) Anal.
          (C26H34N2O5S2.0.2H2O) Calcd.(%): C, 59.79; H, 6.64; N,
          5.36; S, 12.28 Found(%): C, 59.83; H, 6.40; N, 5.42; S,
          12.10.
II-7I-55b 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=9.9Hz), 1.09 and 1.22
          (3H, s), 1.27-1.78(8H, m), 1.99-2.38(6H, m), 2.39(3H,
          s), 3.72(3H, s), 4.19(1H, m), 5.79(1H, dt, J=15.6, 1.5Hz),
          5.98(1H, m), 6.03(1H, d, J=9.0Hz), 6.20(1H, t, J=
          3.3Hz), 6.93(1H, dt, J=15.6, 6.9Hz), 7.19(1H, dd, J=
          1.8, 3.3Hz), 7.28(1H, d, J=3.9Hz), 7.55(1H, d, J=
          3.9Hz).
II-7I-59a mp 143-145° C.; 1H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz),
          1.08 and 1.21(3H, s), 1.24-2.40(14H, m), 4.18(1H,
          m), 5.79(1H, br d, J=15.6Hz), 5.91(1H, d, J=9.0Hz),
          6.98-7.08(3H, m), 7.26(1H, d, J=3.6Hz), 7.29(1H, dd,
          J=1.2, 3.6Hz), 7.42(1H, dd, J=1.2, 5.4Hz); IR(Nujol)
          3419, 3184, 1705, 1670, 1626, 1525, 1500, 1180cm−1;
          [α]D26+12.7±0.6°(c=1.007%, MeOH) Anal.(C25H31NO3S3)
          Calcd.(%): C, 61.31; H, 6.38; N, 2.86; S, 19.64 Found(%):
          C, 61.11; H, 6.41; N, 2.92; S, 19.42
II-7I-88a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.09(3H, s),
          1.21(3H, s), 1.26-2.34(14H, m), 4.15(2H, s), 4.20(1H,
          m), 5.79(1H, dt, J=15.6, 1.2Hz), 5.94(1H, d, J=9.3Hz),
          6.79(1H, d, J=3.6Hz), 6.97(1H, dd, J=4.8, 1.5Hz),
          7.05(1H, m), 7.25-7.33(3H, m); IR(CHCl3) 3523,
          3450, 3431, 2679, 1695, 1647, 1545, 1506, 1471cm−1;
          [α]D26.5+12.7±0.5°(c=1.002, MeOH) Anal.
          (C26H33NO3S2.0.4H2O) Calcd.(%): C, 65.21; H, 6.92; N,
          3.92; S, 13.39 Found(%): C, 65.16; H, 6.63; N, 3.76; S,
          13.48

[0271]

TABLE 54
Compd.
No..       Physical property
II-7I-104a 1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.10(3H, s),
           1.22(3H, s), 1.28-2.36(14H, m), 4.10(2H, s), 4.21(1H,
           m), 5.79(1H, dt, J=15.9, 1.5Hz), 5.96(1H, d, J=9.0Hz),
           6.70(1H, d, J=3.6Hz), 6.95(1H, dd, J=5.1, 3.6Hz),
           7.03(1H, dt, J=15.9, 3.6Hz), 7.04(1H, dd, J=3.6,
           1.2Hz), 7.25(1H, d, J=3.6Hz), 7.37(1H, dd, J=5.1,
           1.2Hz); IR(CHCl3) 3523, 3450, 3431, 2679, 1695, 1649,
           1543, 1506cm−1; [α]D25.0+11.0±0.7°(c=0.709, MeOH)
           Anal.(C26H33NO3S3.0.5H2O) Calcd.(%): C, 60.99; H,
           6.68; N, 2.73; S, 19.06 Found(%): C, 60.69; H, 6.45; N,
           3.12; S, 19.32
II-7I-126a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.08(3H, s),
           1.21(3H, s), 1.27-2.31(14H, m), 3.83(3H, s), 4.12(2H,
           m), 4.20(1H, m), 5.79(1H, dt, J=15.6, 1.5Hz), 5.92
           (1H, d, J=9.3Hz), 6.77(1H, d, J=3.6Hz), 6.86-6.92
           (2H, m), 7.02(1H, dt, J=15.6, 6.9Hz), 7.16(1H, d, J=
           7.5Hz), 7.22(1H, dd, J=7.5, 1.8Hz), 7.27(1H, d, J=
           3.6Hz); IR(CHCl3) 3451, 3433, 2679, 1695, 1647, 1504,
           1288, 1248, 1223, 1213cm−1; [α]D27.0+14.0±0.5°(c=1.001,
           MeOH) Anal.(C29H37NO4S.0.2H2O) Calcd.(%): C, 69.76;
           H, 7.55; N, 2.81; S, 6.42 Found(%): C, 69.50; H, 7.50; N,
           2.88; S, 6.36
II-7I-197a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=32 10.2Hz), 1.08(3H, s),
           1.20(3H, s), 1.26-2.36(14H, m), 3.22(2H, t, J=8.7Hz),
           4.07(2H, s), 4.19(1H, m), 4.57(2H, t, J=8.7Hz), 5.79
           (1H, dt, J=15.6Hz, 1.5Hz), 5.92(1H, d, J=9.0Hz),
           6.79(1H, t, J=7.2Hz), 6.80(1H, d, J=3.6Hz), 6.96
           (1H, d, J=7.2Hz), 7.01(1H, dt, J=15.6, 6.9Hz), 7.10
           (1H, dd, J=7.2, 1.5Hz), 7.29(1H, d, J=3.6Hz); IR
           (CHCl3) 3525, 3450, 3431, 2679, 1695, 1647, 1543, 1506,
           1458cm−1; [α]D25.0+13.0±0.5°(c=1.002, MeOH) Anal.
           (C30H37NO4S.0.2H2O) Calcd.(%): C, 70.47; H, 7.37; N,
           2.74; S, 6.27 Found(%): C, 70.48; H, 7.33; N, 2.74; S,
           6.29
II-7I-239a mp 138-140° C.; 1H-NMR(CDCl3) δ 0.87(1H, d, J=10.2Hz),
           1.07(3H, s), 1.19(3H, s), 1.26-2.31(12H, m), 4.09
           (2H, s), 4.20(1H, m), 5.73(1H, d, J=15.6Hz), 6.08(1H,
           d, J=9.0Hz), 6.79(1H, d, J=3.6Hz), 6.81-6.86(2H, m),
           6.96(1H, dt, J=15.6, 6.9Hz), 7.29(1H, d, J=3.6Hz),
           7.45(1H, s); IR(CHCl3) 3342, 3246, 1720, 1701, 1593,
           1545, 1520, 1456, 1377, 1203cm−1; [α]D25.0+13.8±0.5°
           (c=1.011, MeOH) Anal.(C30H35NO5S) Calcd.(%): C,
           69.07; H, 6.76; N, 2.68; S, 6.15 Found(%): C, 68.91; H,
           6.77; N, 2.75; S, 5.99

[0272]

TABLE 54
Compd.
No..       Physical property
II-7I-270a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.09(3H, s),
           1.23(3H, s), 1.26-1.55(6H, m), 1.62-1.82(2H, m), 1.96-2.38
           (6H, m), 2.42(6H, s), 4.20(1H, m), 5.79(1H, dt, J=
           15.6, 1.5Hz), 5.88(2H, s), 6.06(1H, d, J=9.0Hz), 7.03
           (1H, dt, J=15.6, 6.6Hz), 7.27(1H, d, J=3.9Hz), 7.50
           (1H, d, J=3.9Hz); IR(CHCl3) 3525, 3448, 2679, 1695,
           1655, 1529, 1504, 1375, 1180, 1119cm−1; [α]D25+19.4±0.6°
           (c=1.008, MeOH) Anal.(C27H36N2O5S2.0.2H2O) Calcd.(%):
           C, 60.47; H, 6.84; N, 5.22; S, 11.96 Found(%): C, 60.41; H,
           6.77; N, 5.25; S, 11.90
II-7I-327a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.5Hz), 1.07 and 1.21
           (3H, s), 1.25-2.38(12H, m), 3.00(2H, t, J=8.4Hz), 3.99
           (2H, t, J=8.4Hz), 4.17(1H, m), 5.78(1H, dt, J=1.8, 15.9Hz),
           6.02(1H, d, J=8.7Hz), 6.97-7.24(4H, m), 7.27(1H,
           d, J=4.2Hz), 7.47(1H, d, J=4.2Hz), 7.58(1H, d, J=8.1Hz);
           IR(CHCl3) 2927, 1695, 1653, 1529, 1504, 1479, 1367,
           1165cm−1; [α]D26+21.3±0.6°(c=1.008%, MeOH); Anal.
           (C29H36N2O5S2.0.4H2O) Calcd.(%) C, 61.76; H, 6.58; N,
           4.97; S, 11.37 Found(%) C, 61.68; H, 6.43; N, 5.02; S,
           11.40
II-7I-332a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.07 and 1.22
           (3H, s), 1.30-2.40(16H, m), 2.54(2H, t, J=7.2Hz), 3.84-3.89
           (2H, m), 4.19(1H, m), 5.79(1H, br d, J=14.4Hz),
           6.01(1H, d, J=8.7Hz), 6.97-7.27(5H, m), 7.78(1H, d, J=
           8.4Hz); IR(CHCl3) 2929, 1695, 1653, 1529, 1502, 1363,
           1211, 1161cm−1; [α]D24+19.4±0.6°(c=1.010%, MeOH);
           Anal.(C30H38N2O5S2.0.3H2O) Calcd.(%) C, 62.54; H, 6.75;
           N, 4.86; S, 11.13 Found(%) C, 62.56; H, 6.76; N, 4.87; S,
           10.90
II-7I-343a 1                  H-NMR(CDCl3) δ 0.94(1H, d, J=10.2Hz), 1.11(3H, s),
           1.22(3H, s), 1.39-2.39(14H, m), 4.29(1H, m), 5.78(1H, d,
           J=15.6Hz), 6.15(1H, d, J=9.0Hz), 7.02(1H, m), 7.44-7.64
           (4H, m), 7.85(1H, s), 8.02-8.12(3H, m), 8.65(1H, d, J=
           6.9Hz); IR(CHCl3) 3523, 3444, 2925, 2862, 1695, 1653,
           1516, 1493, 1471, 1446, 1419, 1383, 1315cm−1; [α]D25.0+
           34.8±0.7°(c=1.03, MeOH) Anal.(C31H35NO5S2.0.4H2O)
           Calcd.(%): C, 64.99; H, 6.30; N, 2.44; S, 11.19 Found(%):
           C, 64.97; H, 6.26; N, 2.62; S, 10.86
II-7I-389a mp 119-121° C.; 1H-NMR(CDCl3) δ 0.90(1H, d, J=10.5Hz),
           1.09(3H, s), 1.21(3H, s), 1.33-1.50(6H, m), 1.63-1.78
           (2H, m), 1.98(1H, m), 2.18(1H, m), 2.23(3H, s),
           2.12-2.32(5H, m), 3.21(2H, t, J=8.7Hz), 4.18(1H, m),
           4.62(2H, t, J=8.7Hz), 5.79(1H, d, J=15.6Hz), 5.95(1H,
           d, J=9.3Hz), 6.90(1H, s), 6.95(1H, s), 7.02(1H, dd, J=
           15.6, 6.9Hz), 7.09(1H, d, J=3.6Hz), 7.30(1H, d, J=3.6Hz);
           IR(Nujol) 3361, 2671, 1695, 1649, 1604, 1583, 1533,
           1504, 1415, 1323, 1203cm−1; [α]D25+9.7±0.5°(c=1.012,
           MeOH) Anal.(C30H37NO4S2.0.1H2O) Calcd.(%): C, 66.54;
           H, 6.92; N, 2.59; S, 11.84 Found(%): C, 66.42; H, 6.99; N,
           2.52; S, 11.92

[0273]

TABLE 55
Compd. No.. Physical property
II-7I-391a  1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.09(3H, s),
            1.22(3H, s), 1.33-1.52(6H, m), 1.67-1.77(2H, m), 2.00(1H, m), 2.12(1H,
            m), 2.18-2.25(3H, m), 2.32(3H, s)+2.32(1H,
            m), 3.19(2H, t, J=8.7Hz), 4.20(1H, m), 4.73(2H, t, J=8.7Hz),
            5.79(1H, dt, J=15.6, 1.5Hz), 6.89(1H, d, J=9.0Hz),
            7.03(1H, dt, J=15.6, 7.1Hz), 7.21(1H, s), 7.35(1H, d, J=
            3.9Hz), 7.51(1H, s), 7.74(1H, d, J=3.9Hz); IR(CHCl3)
            3523, 3448, 2681, 1695, 1652, 1527, 1502, 1481, 1329cm−1;
            [α]D25+17.1±0.6°(c=1.016, MeOH) Anal.
            (C30H37NO6S2.0.5H2O) Calcd.(%): C, 62.04; H, 6.60; N, 2.41; S, 11.07
            Found(%): C, 62.16; H, 6.52; N, 2.37; S, 10.85
II-7J-55a   1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.08(3H, s),
            1.22(3H, s), 1.24-2.34(14H, m), 1.78(3H, d, J=1.2Hz), 2.38
            (3H, d, J=1.2Hz), 4.19(1H, s), 5.98(1H, m), 6.04(1H, d, J=
            9.0Hz), 6.19(1H, t, J=3.3Hz), 6.85(1H, dt, J=7.2, 1.2Hz),
            7.19(1H, dd, J=3.3Hz, 1.2Hz), 7.28(1H, d, J=3.9Hz),
            7.55(1H, d, J=3.9Hz); IR(CHCl3) 3525, 3446, 2667, 1685,
            1657, 1529, 1504, 1375, 1281, 1182, 1161, 1053cm−1; [α]D24.0+
            11.5±0.5°(c=1.000, MeOH) Anal.(C27H36N2O5S2.0.4H2O)
            Calcd.(%): C, 60.06; H, 6.87; N, 5.19; S, 11.67 Found(%): C,
            60.15; H, 6.56; N, 5.00; S, 11.37
II-7K-55a   1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.5Hz), 1.08(3H, s),
            1.22(3H, s), 1.24-2.40(14H, m), 2.12(3H, d, J=1.2Hz), 2.39
            (3H, d, J=1.2Hz), 4.20(2H, s), 5.64(1H, d, J=1.2Hz), 5.99
            (1H, m), 6.04(1H, d, J=9.0Hz), 6.20(1H, t, J=3.3Hz), 7.19
            (1H, dd, J=3.3, 1.8Hz), 7.28(1H, d, J=4.2Hz), 7.55(1H, d,
            J=4.2Hz); IR(CHCl3) 3523, 3446, 2575; 1689, 1655, 1530,
            1504, 1375, 1182, 1161, 1053, 1022cm−1; [α]D26.5+18.3±0.6°
            (c=1.009, MeOH) Anal.(C27H36N2O5S2.0.3H2O) Calcd.(%): C,
            60.27; H, 6.86; N, 5.20; S, 11.92 Found(%): C, 60.23; H, 6.66;
            N, 5.17; S, 11.73
II-7L-55a   1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.00(3H, s),
            1.22(3H, s), 1.26-2.61(14H, m), 2.39(3H, s), 4.18(1H, m),
            5.95-6.08(2H, m), 6.16-6.21(2H, m), 7.19(1H, m), 7.32(1H,
            d, J=4.2Hz), 7.55(1H, d, J=4.2Hz); IR(CHCl3) 3510,
            3446, 2927, 2862, 1709, 1658, 1529, 1504, 1441, 1375cm−1;
            [α]D25.0+18.4±0.6°(c=1.00, MeOH) Anal.
            (C26H33FN2O5S2.0.5H2O) Calcd.(%): C, 57.23; H, 6.28; N,
            5.13; F, 3.48; S, 11.75 Found(%): C, 57.44; H, 6.31; N, 5.10;
            F, 3.28; S, 11.27
II-7M-1a    1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.09 and 1.23
            (3H, s), 1.35-2.40(12H, m), 3.54(2H, t, J=6.0Hz), 4.04(2H,
            s), 4.21(1H, m), 6.10(1H, d, J=9.6Hz), 6.32-6.35(2H, m),
            7.15-7.18(2H, m), 7.29(1H, d, J=3.9Hz), 7.57(1H, d, J=
            3.9Hz); IR(CHCl3) 3446, 3431, 1780, 1732, 1657, 1529,
            1504, 1456, 1385, 1192, 1167, 1124, 1057, 1034cm−1; [α]D25.5+
            22.0±0.6°(c=1.000, MeOH) Anal.(C24H32N2O6S2.0.3H2O)
            Calcd.(%): C, 56.08 H, 6.39; N, 5.45; S, 12.48 Found(%):C,
            56.19; H, 6.39; N, 5.48; S, 12.33

[0274]

TABLE 56
Compd.
No..      Physical property
II-7M-1e  1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.10(3H, s),
          1.23(3H, s), 1.26-2.34(12H, m), 3.32(3H, s), 3.51(2H, d, J=
          6.3Hz), 3.99(2H, s), 4.20(1H, m), 6.11(1H, d, J=9.3Hz),
          6.34(2H, m), 7.17(2H, m), 7.29(1H, d, J=3.9Hz),
          7.58(1H, d, J=3.9Hz), 8.90(1H, s); IR(CHCl3) 3448,
          3352, 2925, 2870, 1730, 1657, 1529, 1504, 1471, 1456,
          1423, 1402, 1387, 1354, 1167, 1151, 1120, 1057, 1034cm−1;
          [α]D26 +18.7±1.1°(c=0.52, MeOH) Anal.
          (C25H35N3O7S3.0.7MeOH) Calcd.(%): C, 50.75; H, 6.26; N,
          6.91; S, 15.82 Found(%): C, 50.76; H, 5.68; N, 6.94; S,
          15.49
II-7M-1k  1                  H-NMR(CDCl3) δ 0.93(1H, d, J=10.2Hz), 1.11(3H, s),
          1.23(3H, s), 1.39-2.33(12H, m), 3.46(2H, t, J=6.6Hz),
          3.85(2H, s), 4.22(1H, m), 6.12(1H, d, J=9.0Hz), 6.33
          (2H, m), 7.15(2H, m), 7.29(1H, m), 7.52-7.66(4H, m), 8.09
          (2H, d, J=7.8Hz), 9.03(1H, s); IR(CHCl3) 3446, 3350,
          2924, 2870, 1732, 1657, 1529, 1504, 1473, 1450, 1415,
          1385, 1167, 1120, 1088, 1057, 1034cm−1; [α]D26+14.9±0.6°
          (c=1.00, MeOH) Anal.(C30H37N3O7S3.0.6H2O) Calcd.(%):
          C, 54.71; H, 5.85; N, 6.38; S, 14.61 Found(%): C, 54.81; H,
          5.76; N, 6.60; S, 14.29
II-7M-31a 1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.09 and 1.21
          (3H, s), 1.39-2.37(12H, m), 3.52(2H, t, J=6.3Hz), 4.03
          and 4.14(2H, s), 4.23(1H, m), 6.00(1H, d, J=8.4Hz),
          6.77(1H, d, J=3.6Hz), 7.20-7.37(6H, m); IR(CHCl3)
          2923, 1780, 1732, 1641, 1545, 1508, 1471, 1456, 1365,
          1248, 1219, 1211, 1207, 1124cm−1; [α]D25+14.9±1.1°
          (c=0.509%, MeOH); Anal.(C27H35NO4S2.0.3H2O) Calcd.(%)
          C, 68.27; H, 7.55; N, 2.95; S, 6.75 Found(%) C, 68.25; H,
          7.62; N, 3.02; S, 6.76
II-7M-40a 1                  H-NMR(CDCl3) δ 0.94(1H, d, J=10.2Hz), 1.15 and 1.25
          (3H, s), 1.21-2.38(12H, m), 3.54(2H, t, J=6.3Hz), 4.05
          (2H, s), 4.28(1H, m), 6.11(1H, d, J=9.0Hz), 7.25-7.64
          (7H, m); IR(CHCl3) 2924, 1780, 1732, 1641, 1541, 1510,
          1491, 1471, 1454, 1219, 1211cm−1; [α]D 25+15.7±0.6°
          (c=1.010%, MeOH); Anal.(C26H33NO4S.0.3H2O) Calcd.(%)
          C, 67.74; H, 7.35; N, 3.04; S, 6.96 Found(%) C, 67.68; H,
          7.26; N, 3.107; S, 6.75
II-7M-43a mp 95-97° C.; 1H-NMR(CDCl3) δ 0.94(1H, d, J=10.2Hz),
          1.14 and 1.24(3H, s), 1.24-2.38(12H, m), 3.54(2H, t, J=
          6.3Hz), 4.05(2H, s), 4.27(1H, m), 6.07(1H, d, J=8.7Hz),
          7.04(1H, dd, J=3.9, 4.8Hz), 7.11(1H, d, J=3.9Hz), 7.24
          (1H, dd, J=1.2, 3.6Hz), 7.28(1H, dd, J=1.2, 5.1Hz), 7.37
          (1H, d, 3.9Hz); IR(Nujol) 3346, 2927, 1759, 1728, 1612,
          1525, 1504, 1458, 1377, 1132cm−1; [α]D26+18.7±0.6°
          (c=1.011%, MeOH); Anal.(C24H31NO4S2.0.8H2O)
          Calcd.(%) C, 60.55; H, 6.90; N, 2.94; S, 13.47 Found(%) C,
          60.35; H, 6.61; N, 3.07; S, 13.43

[0275]

TABLE 57
Compd.
No..      Physical property
II-7M-47a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.10 and 1.22
          (3H, s), 1.36-2.40(12H, m), 3.53(2H, t, J=6.0Hz), 4.05
          (2H, s), 4.21(1H, m), 6.14(1H, d, J=9.3Hz), 7.12(1H, dd,
          J=0.9, 4.8Hz), 7.35(1H, d, J=3.9Hz), 7.64(1H, d, J=
          3.9Hz), 7.70(1H, dd, J=1.2, 5.1Hz), 7.76(1H, dd, J=1.2,
          3.9Hz); IR(CHCl3) 3446, 3429, 1780, 1732, 1655, 1529,
          1504, 1336, 1153, 1124, 1074, 1024cm−1; [α]D24+22.5±0.6°
          (c=1.013, MeOH) Anal.(C24H31NO6S3.0.4H2O) Calcd.(%):
          C, 54.09 H, 6.01; N, 2.63; S, 18.05 Found(%): C, 54.29; H,
          5.90; N, 2.81; S, 17.77
II-7M-55a 1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.09 and 1.23
          (3H, s), 1.35-2.40(12H, m), 2.39(3H, s),
          3.53(2H, t, J=6.3Hz),
          4.04(2H, s), 4.21(1H, m), 5.99(1H, m), 6.12(1H, d, J=
          9.6Hz), 6.20(1H, t, J=3.3Hz), 7.19(1H, dd, J=1.5, 3.3Hz),
          7.32(1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz); I IR
          (CHCl3) 3446, 1780, 1731, 1656, 1529, 1504, 1375, 1182,
          1161, 1142, 1053cm−1; [α]D24+20.9±0.6°(c=1.005, MeOH)
          Anal.(C25H34N2O6S2.0.3H2O) Calcd.(%): C, 56.86 H, 6.60;
          N, 5.30; S, 12.14 Found(%):, 56.88; H, 6.60; N, 5.31; S,
          11.76
II-7M-59a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.09 and 1.22
          (3H, s), 1.36-2.38(12H, m), 3.53(2H, t, J=6.0Hz), 4.04
          (2H, s), 4.21(1H, m), 5.98(1H, d, J=8.7Hz), 7.01(1H, dd,
          J=3.6, 5.4Hz), 7.05(1H, d, J=3.9Hz), 7.27(1H, d, J=
          4.2Hz), 7.29(1H, dd, J=1.2, 3.6Hz), 7.43(1H, dd, J=1.5,
          5.4Hz); IR(CHCl3) 3448, 3429, 1780, 1732, 1645, 1529,
          1500, 1471, 1458, 1124cm−1; [α]D26+17.1±0.9°(c=0.608%,
          MeOH) Anal.(C24H31NO4S3.0.3H2O) Calcd.(%): C, 57.75 H,
          6.38; N, 2.81; S, 19.27 Found(%): C, 57.86; H, 6.39; N,
          2.89; S, 19.18
II-7M-88a 1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.11 and 1.22
          (3H, s), 1.42-2.38(12H, m), 3.53(2H, t, J=6.0Hz), 4.03
          and 4.16(2H, s), 4.24(1H, m), 6.01(1H, d, J=9.0Hz),
          6.79(1H, d, J=2.7Hz), 6.96(1H, dd, J=1.2, 5.1Hz), 7.05
          (1H, m), 7.26-7.33(2H, m); IR(CHCl3) 2924, 1780, 1732,
          1641, 1545, 1508, 1471, 1221, 1219, 1211, 1207, 1124cm−1;
          [α]D25+15.5±1.1°(c=0.505%, MeOH);
          Anal. (C25H33NO4S2.0.3H2O)
          Calcd.(%) C, 62.42; H, 7.04; N, 2.91;
          S, 13.33 Found(%) C, 62.57; H, 7.03; N, 2.98; S, 13.15
II-7M-    1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.09(3H, s),
126a      1.21(3H, s), 1.45-2.33(12H, m), 3.51(2H, t, J=6.3Hz),
          3.84(3H, s), 4.02(2H, s), 4.11(2H, s), 4.22(1H, m), 5.99
          (1H, d, J=9.0Hz), 6.77(1H, d, J=3.9Hz), 6.86-6.92(2H,
          m), 7.15(1H, dd, J=7.2, 1.8Hz), 7.22(1H, dd, J=4.8, 1.8Hz),
          7.29(1H, d, J=3.9Hz); IR(CHCl3) 3431, 1669, 1506,
          1463, 1247, 1128cm−1 [α]D27.0+14.4±0.5°(c=1.009, MeOH)
          Anal.(C28H37NO5S.0.2H2O) Calcd.(%): C, 66.82; H, 7.49; N,
          2.78; S, 6.37 Found(%): C, 66.59; H, 7.41; N, 2.82; S, 6.17

[0276]

TABLE 58
Compd.
No..       Physical property
II-7M-197a 1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.10 and
           1.21(3H, s), 1.39-2.38(12H, m), 3.22(2H, t, J=9.0Hz),
           3.52(2H, t, J=6.3Hz), 4.02 and 4,07(2H, s), 4.23(1H,
           m), 4.58(2H, t, J=9.0Hz), 6.00(1H, d, J=8.4Hz),
           6.80-7.12(4H, m), 7.30(1H, d, J=3.6Hz); IR(CHCl3)
           2923, 1780, 1732, 1639, 1545, 1506, 1477, 1458, 1441,
           1365, 1254, 1205, 1126cm−1; [α]D26+13.4±1.1°
           (c=0.506%, MeOH); Anal.(C29H37NO5S.0.4H2O)
           Calcd.(%) C, 67.13; H, 7.34; N, 2.70; S, 6.18 Found(%) C,
           67.19; H, 7.21; N, 2.75; S, 6.18
II-7M-239a mp 179-180° C.;
           1                  H-NMR(d6-DMSO) δ 0.78(1H, d, J=9.6Hz),
           1.05(3H, s), 1.13(3H, s), 1.20-2.30(12H, m),
           3.40(2H, t, J=6.3Hz), 3.84(1H, m), 3.93(2H, s),
           4.17(2H, s), 6.73(1H, dd, J=8.7, 2.4Hz), 6.79(1H, d, J=
           2.4Hz), 6.95(1H, d, J=3.6Hz), 7.34(1H, d, J=8.7Hz),
           7.66(1H, d, J=3.6Hz), 7.79(1H, d, J=6.9Hz),
           7.82(1H, s); IR(KBr) 3338, 3244, 2602, 1739, 1606,
           1557, 1550, 1525, 1458, 1367, 1261, 1211cm−1; [α]D25.0+
           14.0±0.5°(c=1.009, MeOH) Anal.(C29H35NO6.0.3H2O)
           Calcd.(%): C, 65.59; H, 6.76; N, 2.36; S, 6.04 Found(%):
           C, 65.62; H, 6.82; N, 2.81; S, 5.92
II-7M-270a mp.147-149° C.;
           1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz),
           1.09(3H, s), 1.23(3H, s), 1.34-2.38(12H, m), 2.42
           (6H, s), 3.54(2H, t, J=6.3Hz), 4.05(2H, s), 4.21(1H,
           m), 5.88(2H, s), 6.12(1H, d, J=9.0Hz), 7.28(1H, d, J=
           3.9Hz), 7.49(1H, d, J=3.9Hz); IR(Nujol) 3267, 3099,
           2549, 1726, 1610, 1562, 1230,
           1211, 1176, 1126, 1113cm−1;
           [α]D26+19.8±0.6°(c=1.010, MeOH) Anal.
           (C26H36N2O6S2) Calcd.(%): C, 58.18; H, 6.76; N, 5.22; S,
           11.95 Found(%): C, 58.05; H, 6.74; N, 5.16; S, 11.71
II-7M-307a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.5Hz), 1.06(3H, s),
           1.19(3H, s), 1.38-1.79(8H, m), 1.96(1H, m), 2.06(1H,
           m), 2.15-2.31(2H, m), 3.49(2H, t, J=6.6Hz), 3.99(3H,
           s), 4.20(1H, m), 4.60(2H, s), 5.95(1H, d, J=9.0Hz),
           6.74(1H, brd, J=3.6Hz), 7.22(1H, d, J=3.6Hz), 7.32
           (1H, d, J=9.3Hz), 7.34(1H, ddd, J=1.5, 6.9, 8.4Hz),
           7.47(1H, ddd, J=1.5, 6.9, 8.4Hz), 7.80(1H, brd, J=8.4Hz),
           7.82(1H, d, J=9.3Hz), 7.93(1H, brd, J=8.4Hz);
           IR(Nujol) 3450, 3060, 1780, 1732, 1639, 1597, 1510,
           1471, 1265, 1252, 1217cm−1; [α]D26+16.1±0.6°(c=1.005,
           MeOH) Anal.(C32H39NO5S.0.4H2O) Calcd.(%): C, 69.01;
           H, 7.20; N, 2.51; S, 5.76 Found(%): C, 68.97; H, 7.13; N,
           2.56; S, 5.62

[0277]

TABLE 59
Compd.
No..       Physical property
II-7M-327a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.07 and
           1.21(3H, s), 1.36-2.35(12H, m), 3.01(2H, t, J=8.4Hz),
           3.52(2H, t, J=6.6Hz), 3.99(2H, t, J=8.4Hz), 4.03(2H,
           s), 4.19(1H, m), 6.09(1H, d, J=8.7Hz), 6.99-7.24(3H,
           m), 7.29(1H, d, J=3.9Hz), 7.47(1H, d, J=3.9Hz), 7.58
           (1H, d, J=8.1Hz); IR(CHCl3) 2924, 1780, 1732, 1655,
           1529, 1504, 1479, 1460, 1367, 1240, 1225, 1213, 1205,
           1165, 1122, 1105cm−1; [α]D26+22.2±0.6°(c=1.009%,
           MeOH); Anal.(C28H36N2O6S2.0.5H2O) Calcd.(%) C,
           59.03; H, 6.55; N, 4.92; S, 11.26 Found(%) C, 58.93; H,
           6.75; N, 5.14; S, 11.27
II-7M-329a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.08 and
           1.22(3H, s), 1.36-2.38(12H, m), 3.04(2H, t, J=8.4Hz),
           3.53(2H, t, J=6.3Hz), 4.04(2H, s), 4.04(2H, t, J=8.4Hz),
           4.20(1H, m), 6.11(1H, d, J=8.7Hz), 6.75(1H, m),
           7.20(1H, m), 7.30(1H, d, J=3.9Hz), 7.37(1H, brd, J=
           7.5Hz), 7.49(1H, d, J=3.9Hz); IR(CHCl3) 2924, 1780,
           1732, 1655, 1626, 1529, 1504, 1473, 1460, 1369, 1244,
           1223, 1213, 1167cm−1; [α]D26+21.4±0.6°(c=1.009%,
           MeOH); Anal.(C28H35FN2O6S2.0.4H2O) Calcd.(%) C,
           57.40; H, 6.16; F, 3.24; N, 4.78; S, 10.95 Found(%) C,
           57.37; H, 5.82; F, 3.06; N, 4.86; S, 10.80
II-7M-330a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.08 and
           1.22(3H, s), 1.36-2.39(12H, m), 2.97(2H, t, J=8.4Hz),
           3.53(2H, t, J=6.3Hz), 4.02(2H, t, J=8.7Hz), 4.04(2H,
           s), 4.19(1H, m), 6.10(1H, d, J=8.4Hz), 6.82-6.94(2H,
           m), 7.44(1H, d, J=3.9Hz), 7.53(1H, dd, J=4.5, 8.7Hz);
           IR(CHCl3) 2924, 1780, 1732, 1655, 1529, 1504,
           1481, 1367, 1225, 1165cm−1; [α]D26+21.7±0.6°
           (c=1.008%, MeOH); Anal.(C28H35FN2O6S2.0.5H2O)
           Calcd.(%) C, 57.22; H, 6.17; F, 3.23; N, 4.77; S, 10.91
           Found(%) C, 57.26; H, 6.14; F, 3.19; N, 4.85; S, 10.76
II-7M-331a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz), 1.08 and
           1.22(3H, s), 1.36-2.38(12H, m), 3.04(2H, t, J=8.4Hz),
           3.53(2H, t, J=6.3Hz), 4.04(2H, s), 4.04(2H, t, J=8.4Hz),
           4.20(1H, m), 6.11(1H, d, J=8.7Hz), 6.75(1H, m),
           7.20(1H, m), 7.30(1H, d, J=3.9Hz), 7.37(1H, brd, J=
           7.5Hz), 7.49(1H, d, J=3.9Hz); IR(CHCl3) 2924, 1780,
           1732, 1655, 1606, 1529, 1492, 1369, 1261, 1227, 1205,
           1165, 1142, 1095cm−1; [α]D25+21.4±0.6°(c=1.009%,
           MeOH); Anal.(C28H35FN2O6S2.0.3H2O) Calcd.(%) C,
           57.57; H, 6.14; F, 3.25; N, 4.80; S, 10.98 Found(%) C,
           57.28; H, 5.85; F, 3.20; N, 4.86; S, 10.97

[0278]

TABLE 60
Compd.
No..   Physical property
II-7M- 1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.08 and 1.23
332a   (3H, s), 1.36-2.40(14H, m), 2.55(2H, t, J=6.6Hz), 3.53
       (2H, t, J=6.6Hz), 3.84-3.87(2H, m), 4.05(2H, s), 4.20
       (1H, m), 6.05(1H, d, J=9.0Hz), 7.04-7.27(5H, m), 7.78
       (1H, dd, J=0.9, 8.1Hz); IR(CHCl3) 2925, 1780, 1732,
       1655, 1529, 1504, 1489, 1363, 1236, 1225, 1213, 1207,
       1161, 1122cm−1; [α]D24+19.5±0.6°(c=1.015%, MeOH);
       Anal.(C29H38N2O6S2.0.4H2O) Calcd.(%) C, 59.85; H, 6.72;
       N, 4.81; S, 11.02 Found(%) C, 59.84; H, 6.75; N, 4.92; S,
       11.16
II-7M- 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.08 and 1.23
333a   (3H, s), 1.36-2.40(12H, m), 3.53(2H, t, J=6.3Hz), 3.87-3.96
       (4H, m), 4.05(2H, s), 4.20(1H, m), 6.09(1H, d, J=9.0Hz),
       6.85(1H, dd, J=1.5, 8.4Hz), 6.96(1H, m), 7.11(1H,
       m), 7.26-7.30(2H, m), 7.83(1H, dd, J=1.5, 8.1Hz); IR
       (CHCl3) 2924, 1780, 1732, 1655, 1529, 1502, 1491, 1367,
       1248, 1215, 1207, 1165, 1126cm−1; [α]D26+20.5±0.6°
       (c=1.004%, MeOH); Anal.(C28H36N2O7S2.0.4H2O)
       Calcd.(%) C, 57.59; H, 6.35; N, 4.80; S, 10.98 Found(%)
       C, 57.59; H, 6.24; N, 4.89; S, 10.78
II-7M- 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.08 and 1.23
334a   (3H, s), 1.36-2.40(12H, m), 3.05(2H, dd, J=5.4, 9.0Hz),
       3.54(2H, t, J=6.3Hz), 4.03-4.07(4H, m), 4.21(lH, m),
       6.07(1H, d, J=8.7Hz), 7.09-7.27(5H, m), 7.67(1H, m); IR
       (CHCl3) 2924, 1780, 1732, 1655, 1529, 1504, 1473, 1363,
       1161cm−1; [α]D24+24.4±0.6°(c=1.013%, MeOH); Anal.
       (C28H36N2O6S3.0.4H2O) Calcd.(%) C, 56.05; H, 6.18; N,
       4.67; S, 16.03 Found(%) C, 56.18; H, 6.09; N, 4.69; S,
       15.74
II-7M- mp 166-168° C.;
       1                  H-NMR(d6-DMSO) δ 0.79(1H, d, J=9.6Hz),
336a   1.03 and 1.22(3H, s), 1.22-1.58(8H, m), 1.91(1H, m),
       2.08-2.30(4H, m), 3.39(2H, t, J=6.0Hz), 3.85(1H, m),
       3.92(2H, s), 4.63(4H, s), 7.20-7.35(4H, m), 7.77(1H, d, J=
       3.9Hz), 7.94(1H, d, J=3.9Hz), 8.24(1H, d, J=6.9Hz);
       IR(Nujol) 3369, 3093, 2924, 1730, 1612, 1541, 1516, 1466,
       1377, 1344, 1215, 1165, 1126, 1084cm−1; [α]D25+19.0±0.6°
       (c=1.003%, MeOH); Anal.(C28H36N2O6S2.0.7H2O)
       Calcd.(%) C, 58.66; H, 6.57; N, 4.89; S, 11.19 Found(%) C,
       58.38; H, 6.40; N, 4.99; S, 11.48
II-7M- 1                  H-NMR(CDCl3) δ 0.94(1H, d, J=10.2Hz), 1.11(3H, s),
343a   1.23(3H, s), 1.44-2.36(12H, m), 3.49(2H, t, J=6.9Hz),
       3.99(2H, t, J=6.9Hz), 4.29(1H, m), 6.27(1H, d, J=9.3Hz),
       7.44-7.63(4H, m), 7.89(1H, s), 8.01-8.11(3H, m), 8.63
       (1H, d, J=7.5Hz); IR(CHCl3) 3442, 2924, 2870, 1780,
       1730, 1653, 1518, 1417, 1446, 1383, 1317cm−1; [α]D26.0+
       24.3±0.6°(c=1.01, MeOH) Anal.(C30H35NO6S2.1.7H2O)
       Calcd.(%): C, 60.02; H, 6.45; N, 2.33; S, 10.68 Found(%):
       C, 60.14; H, 6.18; N, 2.40; S, 10.3

[0279]

TABLE 61
Compd.
No..       Physical property
II-7M-385a 1                  H-NMR(CDCl3) δ 0.96(1H, d, J=10.2Hz), 1.16(3H, s),
           1.23(3H, s), 1.37-2.39(12H, m), 3.52(2H, t, J=6.3Hz),
           4.02(2H, s), 4.35(1H, m), 6.26(2H, t, J=2.4Hz), 6.48
           (1H, d, J=7.8Hz), 7.21(2H, t, J=2.4Hz), 7.57-7.59
           (2H, m), 8.39(1H, m), 8.44(1H, s); IR(CHCl3) 3456,
           3103, 3022, 2924, 1732, 1651, 1516, 1371, 1221, 1188,
           1163, 1057cm−1; [α]D22.0+42.9±0.8°(c=1.008, MeOH)
           Anal.(C28H34N2O6S2.0.1H2O) Calcd.(%): C, 60.00; H,
           6.15; N, 5.00; S, 11.44 Found(%): C, 59.85; H, 6.29; N,
           4.82; S, 11.28
II-7M-389a mp 112-114° C.;
           1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.5Hz),
           1.09(3H, s), 1.21(3H, s), 1.39-1.52(4H, m), 1.59-1.81
           (4H, m), 1.98(1H, m), 2.11(1H, m), 2.23(3H, s) +
           2.18-2.34(2H, m), 3.21(2H, t, J=8.7Hz), 3.52(2H, t, J=
           6.5Hz), 4.05(2H, s), 4.20(1H, m), 4.62(2H, t, J=8.7Hz),
           6.00(1H, d, J=9.0Hz), 6.90(1H, s), 6.96(1H, s),
           7.08(1H, d, J=4.2Hz), 7.32(1H, d, J=4.2Hz); IR
           (Nujol) 3406, 3338, 2729, 1757, 1738, 1614, 1583, 1533,
           1503, 1203, 1124cm−1; [α]D23+12.2±0.5°(c=1.013,
           MeOH) Anal.(C29H37NO5S2.0.2H2O) Calcd.(%): C, 63.64;
           H, 6.89; N, 2.56; S, 11.72 Found(%): C, 63.68; H, 6.83;
           N, 2.55; S, 11.54
II-7M-390a mp 120-122° C.;
           1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz),
           1.08(3H, s), 1.21(3H, s), 1.38-1.52(4H, m), 1.56-1.78
           (4H, m), 1.98(1H, m), 2.10(1H, m), 2.17-2.33(2H,
           m), 2.39(3H, s), 3.52(2H, t, J=6.3Hz), 4.04(2H, s),
           4.20(1H, m), 6.00(1H, d, J=9.0Hz), 6.72(1H, d, J=2.1Hz),
           7.09(1H, m), 7.18(1H, d, J=3.9Hz), 7.33(1H, m) +
           7.34(1H, d, J=3.9Hz), 7.63(1H, d, J=2.1Hz) ; IR
           (CHCl3) 3508, 3448, 3429, 2667, 2568, 1780, 1732, 1645,
           1529, 1500, 1471, 1421, 1323, 1246, 1130,cm−1;
           [α]D24+12.5±0.5°(c=1.008, MeOH) Anal.
           (C29H35NO5S2.0.3H2O) Calcd.(%): C, 63.66; H, 6.56; N,
           2.56; S, 11.72 Found(%): C, 63.74; H, 6.44; N, 2.54; S,
           11.78
II-7M-391a mp 177-179° C.;
           1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz),
           1.10(3H, s), 1.22(3H, s), 1.40-1.53(4H, m), 1.57-1.71
           (3H, m), 1.79(1H, m), 2.00(1H, m), 2.11(1H, m),
           2.19-2.35(2H, m)+2.32(3H, s), 3.19(2H, t, J=8.7Hz),
           3.53(2H, t, J=6.5Hz), 4.05(2H, s), 4.21(1H, m), 4.73
           (2H, t, J=8.7Hz), 6.17(1H, d, J=9.0Hz), 7.21(1H, s),
           7.36(1H, d, J=3.9Hz), 7.51(1H, s), 7.74(1H, d, J=3.9Hz);
           IR(Nujol) 3249, 2754, 2677, 2553, 1736, 1622,
           1564, 1331, 1225, 1196, 1155, 1134cm−1;
           [α]D25+17.1±0.6°(c=1.006, MeOH) Anal.
           (C29H37NO7S2.0.2H2O) Calcd.(%): C, 60.12; H, 6.51; N,
           2.42; S, 11.07 Found(%): C, 60.09; H, 6.47; N, 2.32; S,
           11.06

[0280]

TABLE 62
Compd.
No..       Physical property
II-7M-392a mp 155-156° C.;
           1                  H-NMR(CDCl3) δ 0.89(1H, d, J=9.9Hz),
           1.08(3H, s), 1.20(3H, s), 1.36-1.52(4H, m), 1.55-1.69
           (3H, m), 1.78(1H, m), 1.99(1H, m), 2.10(1H, m),
           2.17-2.34(2H, m), 2.51(3H, s), 3.51(2H, t, J=6.5Hz),
           4.04(2H, s), 4.19(1H, m), 6.17(1H, d, J=8.7Hz), 6.78
           (1H, d, J=2.1Hz), 7.36(1H, d, J=3.9Hz), 7.64(1H, m),
           7.75(1H, d, J=2.1Hz), 7.77(1H, m), 7.83(1H, d, J=3.9Hz);
           IR(Nujol) 3323, 1734, 1624, 1536, 1321, 1153,
           1126cm−1; [α]D25+20.4±0.6°(c=1.006, MeOH) Anal.
           (C29H35NO7S2.0.6H2O) Calcd.(%): C, 59.59; H, 6.24; N,
           2.40; S, 10.97 Found(%): C, 59.57; H, 6.12; N, 2.37; S,
           10.77
II-7M-393a 1                  H-NMR(CDCl3) δ 0.90(3H, t, J=7.2Hz), 0.91(1H, d, J=
           9.3Hz), 1.09(3H, s), 1.21(3H, s), 1.25-1.79(12H, m),
           1.98(1H, m), 2.10(1H, m), 2.17-2.34(2H, m), 2.47(2H,
           t, J=7.7Hz), 3.23(2H, t, J=8.7Hz), 3.52(2H, t, J=6.3Hz),
           4.04(2H, s), 4.21(1H, m), 4.62(2H, t, J=8.7Hz),
           5.99(1H, d, J=9.0Hz), 6.93(1H, s), 6.98(1H, s), 7.07
           (1H, d, J=3.9Hz), 7.31(1H, d, J=3.9Hz); IR(CHCl3)
           3058, 3448, 3429, 1780, 1732, 1643, 1529, 1500, 1466,
           1419, 1248, 1124cm−1; [α]D24+12.7±0.5°(c=1.014,
           MeOH) Anal.(C32H43NO5S2.0.2H2O) Calcd.(%): C, 65.21;
           H, 7.42; N, 2.38; S, 10.88 Found(%): C, 65.09; H, 7.37;
           N, 2.35; S, 11.02
II-7N-55a  1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.5Hz), 1.08 and
           1.23(3H, s), 1.56(1H, ddd, J=2.7, 6.0, 13.5Hz), 1.90-2.46
           (7H, m), 2.39(3H, s), 4.11(2H, d, J=1.2Hz), 4.14-4.19
           (3H, m), 5.57-5.76(2H, m), 5.99(1H, m), 6.17-6.21
           (2H, m), 7.19(1H, dd, J=1.8, 3.3Hz), 7.34(1H, d, J=3.9Hz),
           7.55(1H, d, J=3.9Hz); IR(CHCl3) 3446, 1732,
           1657, 1529, 1504, 1375, 1182, 1161,
           1142, 1119, 1053cm−1;
           [α]D24+40.4±0.8°(c=1.001, MeOH) Anal.
           (C25H32N2O6S2.0.3H2O) Calcd.(%): C, 57.08 H, 6.25; N,
           5.32; S, 12.19 Found(%): C, 57.07; H, 6.18; N, 5.39; S,
           11.91
II-7O-55a  1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.09 and
           1.23(3H, s), 1.55(1H, ddd, J=2.7, 5.7, 13.5Hz), 1.85-2.40
           (7H, m), 2.39(3H, s), 3.93-4.05(4H, m), 4.25(1H,
           m), 5.58-5.79(2H, m), 6.00(1H, m), 6.11(1H, d, J=9.0Hz),
           6.20(1H, t, J=3.3Hz), 7.19(1H, dd, J=1.5, 3.3Hz),
           7.32(1H, d, J=4.2Hz), 7.55(1H, d, J=4.2Hz); IR
           (CHCl3) 3444, 1778, 1732, 1657, 1529, 1504, 1375, 1182,
           1161, 1144, 1053cm−1; [α]D24.5+15.8±0.6°(c=1.008,
           MeOH) Anal.(C25H32N2O6S2.0.4H2O) Calcd.(%): C, 56.88
           H, 6.26; N, 5.31; S, 12.15 Found(%): C, 56.91; H, 6.17;
           N, 5.30; S, 12.14

[0281]

TABLE 63
Compd.
No..      Physical property
II-7P-55a 1                  H-NMR(CDCl3) δ 0.89(1H, d, J=10.2Hz), 1.09(3H, s),
          1.23(3H, s), 1.54(1H, m), 1.95-2.35(7H, m), 2.39(3H, s),
          4.14-4.31(5H, m), 5.39(1H, dt, J=7.8Hz and 20.7Hz),
          5.99(1H, m), 6.20(1H, m), 6.29(1H, d, J=5.4Hz), 7.18
          (1H, m), 7.36(1H, d, J=3.9Hz), 7.53(1H, d, J=3.9Hz);
          IR(CHCl3) 3446, 2925, 1732, 1655, 1531, 1504, 1375, 1161,
          1142, 1053, 1022cm−1; [α]D24+30.1±0.7°(c=1.01, MeOH)
          Anal.(C25H31FN2O6S2.0.7MeOH) Calcd.(%): C, 55.01; H,
          6.07; N, 4.99; F, 3.39; S, 11.43 Found(%): C, 55.21; H,
          5.92; N, 5.11; F, 3.49; S, 11.16
II-7P-55e 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.10(3H, s),
          1.25(3H, s), 1.97-2.37(8H, m), 2.39(3H, s), 3.28(3H, s),
          3.99-4.28(5H, m), 5.41(1H, dt, J=8.7 and 20.4Hz), 5.99
          (1H, m), 6.13(1H, d, J=8.4Hz), 6.20(1H, m), 7.19(1H,
          m), 7.33(1H, d, J=4.2Hz), 7.55(1H, d, J=4.2Hz); IR
          (CHCl3) 3448, 3352, 2925, 1728, 1657, 1529, 1504, 1425,
          1402, 1375, 1348, 1157, 1053, 1020cm−1; [α]D24+32.7±1.5°
          (c=0.49, MeOH) Anal.(C26H34FN3O7S3.0.45MeOH)
          Calcd.(%): C, 50.41; H, 5.73; N, 6.67; F, 3.01; S, 15.26
          Found(%): C, 50.80; H, 5.81; N, 6.63; F, 2.85; S, 14.87
II-7P-55j 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.09(3H, s),
          1.24(3H, s), 1.51-2.37(8H, m), 2.39(3H, s), 3.97(2H, s),
          4.17-4.25(3H, m), 5.39(1H, dt, J=9.0 and 20.7Hz), 5.99
          (1H, m), 6.20(1H, m), 6.37(1H, d, J=8.1Hz), 6.71(1H, s),
          7.19(1H, m), 7.39(1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz);
          IR(CHCl3) 3519, 3402, 2925, 2870, 1745, 1689, 1657,
          1574, 1529, 1504, 1471, 1448, 1375, 1161, 1144, 1092,
          1053, 1022cm−1; [α]D25+40.8±1.6°(c=0.51, MeOH)
II-7Q-55a 1                  H-NMR(CDCl3) δ 0.90(1H, d, J=10.2Hz), 1.11 and 1.23
          (3H, s), 1.53(1H, ddd, J=2.1, 5.7, 13.5Hz), 1.70-2.38(7H,
          m), 2.38(3H, s), 3.52(2H, t, J=6.3Hz), 3.96-4.13(2H, m),
          4.23(1H, m), 5.97-6.04(2H, m), 6.14(1H, d, J=9.3Hz),
          6.20(1H, t, J=3.6Hz), 6.96(1H, dt, J=4.2, 15.6Hz), 7.18
          (1H, m), 7.27(1H, d, J=3.9Hz), 7.54(1H, d, J=3.9Hz);
          IR(CHCl3) 2925, 1701, 1657, 1529, 1504, 1375, 1215, 1182,
          1161, 1142cm−1; [α]36526 −42.1±0.8°(c=1.001%, MeOH);
          Anal.(C25H32N2O6S2.0.4H2O) Calcd.(%) C, 56.88; H, 6.26;
          N, 5.31; S, 12.15 Found(%) C, 56.95; H, 6.11; N, 5.35; S,
          12.11
II-7R-55a 1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.2Hz), 1.09 and 1.22
          (3H, s), 1.35-2.40(12H, m), 2.39(3H, s),
          2.64(2H, t, J=7.2Hz),
          3.20(2H, s), 4.20(1H, m), 4.52(1H, brs), 5.99(1H,
          m), 6.16(1H, d, J=8.7Hz), 6.20(1H, t, J=3.3Hz), 7.19
          (1H, dd, J=1.8, 3.3Hz), 7.31(1H, d, J=3.9Hz), 7.55(1H,
          d, J=3.9Hz); IR(CHCl3) 3446, 2675, 2565, 1711, 1657,
          1529, 1504, 1375, 1182, 1161, 1144, 1053cm−1; [α]D24+
          23.5±0.6°(c=1.007, MeOH) Anal.(C25H34N2O5S3.0.3H2O)
          Calcd.(%): C, 55.18; H, 6.41; N, 5.15; S, 17.68 Found(%): C,
          55.29; H, 6.31; N, 5.12; S, 17.46

[0282]

TABLE 64
Compd.
No..       Physical property
II-7R-88a  1                  H-NMR(CDCl3) δ 0.93(1H, d, J=10.2Hz), 1.10 and
           1.22(3H, s), 1.36-2.40(12H, m), 2.65(2H, t, J=6.9Hz),
           3.17 and 3.22(each 1H, ABq, J=14.7Hz), 4.16(2H, s),
           4.23(1H, m), 4.60(1H, brs), 6.04(1H, d, J=9.3Hz),
           6.79(1H, brd, J=3.9Hz), 6.96(1H, dd, J=1.5, 5.1Hz),
           7.05(1H, m), 7.28(1H, dd, J=3.0, 4.8Hz), 7.32(1H, d, J=
           3.6Hz); IR(CHCl3) 3450, 3430, 1711, 1641, 1545,
           1508, 1471, 1460, 1294, 1263, 1126cm−1; [α]D24+
           18.0±0.6°(c=1.003, MeOH) Anal.
           (C25H33NO3S3.0.3H2O) Calcd.(%): C, 60.40; H, 6.81; N,
           2.82; S, 19.35 Found(%): C, 60.42; H, 6.60; N, 2.99; S,
           19.47
II-7R-270a mp.150-152° C.;
           1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.5Hz),
           1.09(3H, s), 1.23(3H, s), 1.34-2.38(12H, m), 2.42
           (6H, s), 2.64(2H, t, J=7.2Hz), 3.20(2H, s), 4.21(1H,
           m), 5.88(2H, s), 6.15(1H, d, J=9.0Hz), 7.29(1H, d, J=
           3.9Hz), 7.49(1H, d, J=3.9Hz); IR(Nujol) 3365, 3084,
           1709, 1622, 1549, 1367, 1176, 1126cm−1; [α]D27+
           22.7±0.6°(c=1.001, MeOH) Anal.
           (C26H36N2O5S3.0.2(C6H14O))
           Calcd.(%): C, 57.31; H, 6.86;
           N, 4.91; S, 16.88 Found(%): C, 57.18; H, 6.78; N, 4.89; S,
           16.95
II-7S-47a  1                  H-NMR(CDCl3) δ 0.86(1H, d, J=10.2Hz), 1.08 and
           1.20(each 3H, s), 1.38-2.40(10H, m), 3.89-4.20(4H, m),
           6.68-6.72(2H, d, m), 7.11(1H, dd, J=3.6, 4.8Hz), 7.44
           (1H, d, J=4.2Hz), 7.59(1H, d, J=4.2Hz), 7.71(1H, dd,
           J=3.6, 5.1Hz), 7.74(1H, dd, J=1.2, 3.9Hz); IR(CHCl3)
           3346, 3097, 1730, 1649, 1533, 1506, 1402, 1335, 1153,
           1024cm−1; [α]D24+27.5±0.7°(c=1.003, MeOH) Anal.
           (C24H30N2O6S3.0.5H2O) Calcd.(%): C, 52.63; H, 5.70; N,
           5.11; S, 17.56 Found(%): C, 52.45; H, 5.39; N, 5.211; S,
           17.62
II-7S-55a  mp 99-101° C.;
           1                  H-NMR(CDCl3) δ 0.87(1H, d, J=10.2Hz),
           1.08 and 1.21(each 3H, s), 1.40-2.40(10H, m), 2.38
           (3H, s), 3.91-4.20(3H, m), 5.99(1H, m), 6.20(1H, t, J=
           3.6Hz), 6.53-6.60(2H, d, m), 7.17(1H, dd, J=1.8, 3.3Hz),
           7.41(1H, d, J=4.2Hz), 7.53(1H, d, J=4.2Hz); IR
           (Nujol) 3321, 3089, 1736, 1709, 1660, 1633, 1550, 1377,
           1236, 1184, 1159, 1051cm−1; [α]D24+28.5±0.7°(c=1.006,
           MeOH) Anal.(C25H33N3O6S2) Calcd.(%): C, 56.05; H,
           6.21; N, 7.84; S, 11.97 Found(%): C, 55.74; H, 6.17; N,
           7.71; S, 11.81

[0283]

TABLE 65
Compd.
No..      Physical property
II-7T-55a 1                  H-NMR(CDCl3) δ 0.86(1H×1/2, d, J=10.5Hz), 0.90
          (1H×1/2, d, J=10.5Hz), 1.05, 1.08, 1.20 and 1.22(each
          3H×1/2, s), 1.40-2.57(10H, m), 2.39(3H, s), 4.18(1H, m),
          4.47 and 4.57(each 1H×1/2, ABq, J=17.1Hz), 4.49 and
          4.59(each 1H×1/2, ABq, J=17.1Hz), 5.99(1H, m), 6.20
          (1H, m), 6.36(1H, m), 6.73(1H×1/2, t, J=6.0Hz), 7.18
          (1H, m), 7.32(1H×1/2, d, J=3.9Hz), 7.38(1H×1/2, d, J=
          3.9Hz), 7.46(1H×1/2, t, J=6.0Hz), 7.53(1H, d, J=3.9Hz);
          IR(CHCl3) 3446, 1765, 1732, 1655, 1531, 1504, 1375,
          1182, 1161, 1144, 1053, 1022cm−1; [α]D25 −4.2±0.4°
          (c=1.008, MeOH) Anal.(C24H31N3O6S2) Calcd.(%): C, 55.26;
          H, 5.99; N, 8.06; S, 12.29 Found(%): C, 55.20; H, 5.88; N,
          7.81; S, 11.94
II-7U-31a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.10 and 1.22
          (3H, s), 1.47(1H, m), 1.64-2.63(12H, m), 4.13(2H, s), 4.20
          (1H, m), 6.07(1H, d, J=8.4Hz), 6.77(1H, d, J=3.9Hz),
          7.22-7.36(6H, m); IR(CHCl3) 2924, 1709, 1643, 1543,
          1506, 1471, 1454, 1284, 1223, 1213, 1205cm−1; [α]D26+
          25.1±1.3°(c=0.507%, MeOH); Anal.
          (C27H35NO3S2.0.3H2O)
          Calcd.(%) C, 66.03; H, 7.31; N, 2.83;
          S, 13.06 Found(%) C, 66.03; H, 7.37; N, 2.96; S, 13.09
II-7U-55a 1                  H-NMR(CDCl3) δ 0.89(1H, d, J=10.2Hz), 1.10 and 1.22
          (3H, s), 1.48(1H, ddd, J=2.4, 5.4, 13.2Hz), 1.65-2.60
          (12H, m), 2.40(3H, s), 4.18(1H, m), 5.99(1H, m), 6.20(1H,
          t, J=3.3Hz), 6.23(1H, d, J=8.4Hz), 7.19(1H, dd, J=1.8,
          3.3Hz), 7.33(1H, d, J=4.2Hz), 7.55(1H, d, J=4.2Hz);
          IR(CHCl3) 2925, 1741, 1709, 1657, 1529, 1504, 1375, 1221,
          1211, 1207, 1182, 1161, 1144cm−1;
          [α]D25+29.1±0.7°
          (c=1.008%, MeOH);
          Anal.(C25H34N2O5S3.0.3H2O) Calcd.(%)
          C, 55.18; H, 6.41; N, 5.15; S, 17.68 Found(%) C, 55.20; H,
          6.25; N, 5.21; S, 17.71
II-7U-88a 1                  H-NMR(CDCl3) δ 0.91(1H, d, J=10.2Hz), 1.11 and 1.22
          (3H, s), 1.47(1H, m), 1.64-2.63(12H, m), 4.16(2H, s), 4.21
          (1H, m), 6.08(1H, d, J=8.7Hz), 6.79(1H, d, J=3.9Hz),
          6.96(1H, dd, J=1.2, 5.1Hz), 7.05(1H, m), 7.27-7.34(3H,
          m); IR(CHCl3) 2924, 1709, 1643, 1543, 1508, 1471, 1284,
          1238, 1217cm−1; [α]D25+24.9±0.6°(c=1.014%, MeOH);
          Anal.(C25H33NO3S3.0.4H2O) Calcd.(%) C, 60.18; H, 6.83;
          N, 2.81; S, 19.28 Found(%) C, 60.20; H, 6.77; N, 2.94; S,
          19.34
II-7V-55a 1                  H-NMR(CDCl3) δ 0.92(1H, d, J=10.8Hz), 1.09(3H, s),
          1.23(3H, s), 1.26-2.34(14H, m), 2.39(3H, s), 4.20(1H, m),
          5.99-6.07(2H, m), 6.13-6.29(2H, m), 7.19(1H, m), 7.29
          (1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz); IR(CHCl3)
          3512, 3446, 2927, 2862, 2553, 1711, 1658, 1529, 1504,
          1431, 1375, 1279cm−1; [α]D26.0+16.0±1.1°(c=0.50, MeOH)
          (C26H33FN2O5S2.0.6MeOH) Calcd.(%): C, 57.47; H,
          6.42; N, 5.04; F, 3.42; S, 11.5 Found(%): C, 57.77; H, 6.28;
          N, 4.95; F, 3.33; S, 11.15

[0284]

TABLE 66
Compd.
No..      Physical property
II-8C-55a 1                  H-NMR(d6-DMSO) δ 0.77(1H, d, J=9.6Hz), 1.03(3H, s),
          1.12(3H, s), 1.13-1.52(9H, m), 1.89(1H, m), 2.06-2.30
          (4H, m), 2.32(3H, s), 3.39(2H, m), 3.62(2H, s), 3.84(1H,
          m), 6.10(1H, m), 6.27(1H, t, J=3.3Hz), 7.25(1H, dd, J=
          3.3, 1.5Hz), 7.87(1H, d, J=3.9Hz), 7.98(1H, d, J=3.9Hz),
          8.45(1H, d, J=7.2Hz); IR(Nujol) 3332, 1623, 1536,
          1457, 1375, 1182, 1160cm−1; [α]D24.0+15.1±0.6°(c=1.006,
          DMSO) Anal.(C26H36N2O6S2.2.0H2O) Calcd.(%): C, 53.52;
          H, 7.04; N, 4.89; S, 11.10 Found(%): C, 53.38; H, 6.74; N,
          4.82; S, 10.88
II-8C-88a 1                  H-NMR(d6-DMSO) δ 0.77(1H, d, J=9.3Hz), 1.05(3H, s),
          1.13(3H, s), 1.14-1.66(8H, m), 1.86-2.28(6H, m), 3.38
          (2H, m), 3.60(2H, s), 3.85(1H, m), 4.13(2H, s), 6.88(1H,
          d, J=3.6Hz), 6.99(1H, dd, J=5.1, 0.9Hz), 7.28(1H, m),
          7.48(1H, dd, J=5.1, 3.0Hz), 7.67(1H, d, J=3.6Hz), 7.82
          (1H, d, J=7.2Hz);
          IR(Nujol) 3413, 1623, 1508, 1459, 1091cm−1;
          [α]D24.0+12.6±1.1°(c=0.500, DMSO) Anal.
          (C26H35NO4S2.2.0H2O) Calcd.(%): C, 58.40; H, 7.28; N,
          2.66; S, 12.00 Found(%): C, 58.43; H, 7.01; N, 2.73; S,
          11.73
VI-6A-1a  1                  H-NMR(CDCl3) δ 0.86(1H, m), 1.04-1.66(15H, m),
          1.95(1H, m), 2.15(1H, brs), 2.33(2H, t, J=7.5Hz), 3.26
          (1H, m), 3.49(1H, m), 6.11(1H, brt), 6.33(2H, t, J=2.4Hz),
          7.16(2H, t, J=2.4Hz), 7.33 and 7.57(each 1H, each
          d, each J=4.2Hz); IR(CHCl3) 3514, 3446, 2679, 1709,
          1658, 1535, 1509, 1456, 1385, 1274, 1192, 1192, 1167,
          1057, 1034cm−1; [α]D26+8.7±0.5°(c=1.002, MeOH) Anal.
          (C23H30N2O5S2.0.1H2O) Calcd.(%): C, 57.50; H, 6.34; N,
          5.83; S, 13.35 Found(%): C, 57.56; H, 6.46; N, 5.91; S,
          13.04
VI-6A-47a 1                  H-NMR(CDCl3) δ 0.87(1H, m), 1.04-1.66(15H, m), 1.95
          (1H, m), 2.16(1H, brs), 2.33(2H, t, J=7.5Hz), 3.27(1H,
          m), 3.49(1H, m), 6.24(1H, brt), 7.11(1H, dd, J=3.6 and
          4.8Hz), 7.39 and 7.63(each 1H, each d, each J=3.9Hz),
          7.70(1H, dd, J=1.2 and 4.8Hz), 7.75(1H, dd, J=1.2 and
          3.6Hz); IR(CHCl3) 3514, 3446, 1709, 1657, 1533, 1506,
          1402, 1336, 1153, 1097, 1024cm−1; [α]D26+7.4±0.5°
          (c=1.014, MeOH) Anal.(C23H29NO5S3.0.4H2O) Calcd.(%):
          C, 55.93; H, 5.97; N, 2.79; S, 19.13 Found(%): C, 55.08; H,
          6.09; N, 2.93; S, 19.03
VI-6A-88a 1                  H-NMR(CDCl3) δ 0.87(1H, m), 1.04-1.68(15H, m), 1.94
          (1H, m), 2.17(1H, brs), 2.33(2H, t, J=7.5Hz), 3.20(1H,
          m), 3.53(1H, m), 4.15(2H, s), 5.87(1H, brt), 6.78(1H, m),
          6.96(1H, dd, J=1.2 and 5.1Hz), 7.05(1H, m), 7.28(1H,
          dd, J=3.0 and 5.1Hz), 7.34(1H, d, J=3.6Hz); IR(CHCl3)
          3516, 3452, 1709, 1645, 1547, 1513, 1462cm−1; [α]D26+
          8.4±0.5°(c=1.015, MeOH) Anal.(C24H31NO3S2.0.2H2O)
          Calcd.(%): C, 64.17; H, 7.04; N, 3.12; S, 14.28 Found(%):
          C, 64.16; H, 7.13; N, 3.18; S, 14.09

[0285]

TABLE 67
Compd. No.. Physical property
VII-GA-1a   1                  H-NMR (CDCl3) δ 0.86 (1H, m), 1.08-1.60 (15H, m),
            1.95(1H, m), 2.15 (1H, brs), 2.33 (2H, t, J=7.5 Hz), 3.26
            (1H, m), 3.49 (1H, m), 6.15 (1H, brt, J=5.1 Hz), 6.33
            (2H, t, J=2.4 Hz), 7.16 (2H, t, J=2.4 Hz), 7.33 and 7.57
            (each 1H, each d, each J=3.9 Hz); IR (CHCl3) 3514,
            3446, 2677, 1709, 1660, 1533, 1508, 1456, 1385, 1275,
            1192, 1167, 1057, 1034 cm−1; ]α]D24 − 7.6 ± 0.5° (c=1.006
            MeOH) Anal. (C23H30N2O5S2·0.3H2O) Calcd.(%): C,
            57.07; H, 6.37; N, 5.79; S, 13.25 Found (%): C, 57.16; H,
            6.27; N, 5.81; S, 13.19
VII-6A-47a  1                  H-NMR (CDCl3) δ 0.87 (1H, m), 1.10-1.63 (15H, m),
            1.95 (1H, m), 2.16 (1H, brs), 2.33 (2H, t, J=7.5 Hz),
            3.27 (1H, m), 3.49 (1H, m), 6.23 (1H, brt, J=5.6 Hz),
            7.11 (1H, dd, J=3.9 and 5.1 Hz), 7.38 and 7.63 (each 1H,
            each d, each J=3.9 Hz), 7.70 (1H, dd, J=1.5 and 5.1 Hz),
            7.75 (1H, dd, J=1.5 and 3.9 Hz); IR (CHCl3) 3514,
            3446, 1709, 1657, 1533, 1506, 1402, 1336, 1275, 1153,
            1097, 1024 cm−1; [α]D24 − 8.1 ± 0.5° (c=1.008, MeOH)
            Anal. (C23H29NO5S3·0.3H2O) Calcd.(%): C, 55.13; H,
            5.95; N, 2.80; S, 19.20 Found (%): C, 55.15; H, 5.94;
            N, 3.06; S, 19.14
VII-6A-88a  1                  H-NMR (CDCl3) δ 0.86 (1H, m), 1.09-1.61 (15H, m),
            1.94 (1H, m), 2.17 (1H, brs), 2.32 (2H, t, J=7.5 Hz),
            3.21 (1H, m), 3.52 (1H, m), 4.15 (2H, s), 5.89 (1H, brt,
            J=5.4 Hz), 6.78 (1H, d, J=3.6 Hz), 6.96 (1H, dd,
            J=1.8 and 5.1 Hz), 7.05 (1H, m), 7.28 (1H, dd, J=3.0
            and 5.1 Hz), 7.34 (1H, d, J=3.6 Hz); IR (CHCl3) 3517,
            3450, 1709, 1645, 1547, 1514, 1462 cm−1;
            [α]D24 − 9.4 ± 0.5° (c=1.012, MeOH)
            Anal. (C24H31NO3S2) Calcd.(%): C, 64.68; H, 7.01; N,
            3.14; S, 14.39 Found (%): C, 64.51; H, 6.90; N, 3.17; S,
            14.53

[0286] The structure and physical property of the compound prepared as the example of reference are shown below. A compound with a beginning number “I-” means a compound of the formula: 576

[0287] A compound with a beginning number “II-” means a compound of the formula: 577

[0288] A compound with a beginning number “III-” means a compound of the formula: 578

[0289] A compound with a beginning number “IV-” means a compound of the formula: 579

[0290] A compound with a beginning number “V-” means a compound of the formula: 580

[0291] A compound with a beginning number “VI-” means a compound of the formula: 581

[0292] Furthermore, a number following the number (I, II, III, IV, V, and VI) represents a structure of the group of the formula: —X1—X2—X3 and each number is the same meaning as that used in the list of the structure of the formula: —X1—X2—X3.

[0293] Compound Number I-1

[0294] mp.113-114° C.; 1H-NMR(CDCl3) δ: 1.09(1H, m), 1.17-1.32(2H, m), 1.34-1.52(2H, m), 1.56-1.75(4H, m), 2.00-2.18(5H, m), 2.35 (2H, t, J=7.2 Hz), 2.52(1H, m), 3.80(1H, m), 5.31-5.43(2H, m), 6.22(1H, d, J=6.0 Hz), 6.35 and 7.17(each 2H, each t, each J=2.1 Hz), 7.37 and 7.56(each 1H, each d, each J=3.9 Hz). IR(Nujol): 3369, 3143, 3124, 3068, 2678, 1710, 1626, 1593, 1374, 1200, 1171 cm−1. [α]D26.5+75.5±1.2°(c=1.004, MeOH) Anal. (C23H28N2O5S2) Calcd.(%): C, 57.96.; H, 5.92; N, 5.88; S, 13.45. Found(%): C, 57.99; H, 5.88; N, 5.66; S, 13.50.

[0295] Compound Number I-3

[0296] 1 H-NMR (CDCl3-CD3OD) δ: 1.23(1H, m), 1.28-1.32(2H, m), 1.44-1.53(2H, m), 1.57-1.74(4H, m), 2.03-2.14(5H, m), 2.32(2H, t, J=7.2 Hz), 2.56(1H, m), 3.82(1H, m), 5.33-5.47(2H, m), 6.80(1H, m), 7.09-7.12(2H, m), 7.22(1H, t, J=8.1 Hz), 7.63 and 7.86(each 1H, each d, each J=8.1 Hz). IR(CHCl3): 3593 3442, 3111, 1710, 1644, 1519, 1449 cm−1. [α]D25+77.6±1.20°(c=1.010, MeOH) Anal. (C25H29NO4S.0.2H2O) Calcd.(%): C, 67.76; H, 6.69; N, 3.16; S, 7.23. Found(%): C, 67.64; H, 6.77; N, 3.17; S, 7.18.

[0297] Compound Number I-4

[0298] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.17-1.32(2H, m), 1.40-1.50(2H, m), 1.56-1.80 (4H, m), 2.00-2.22(5H, m), 2.33(2H, t, J=7.2 Hz), 2.53(1H, m), 3.84 (3H, s), 3.85(1H, m), 5.29-5.42(2H, m), 6.18(1H, d, J=6.9 Hz), 6.93, 7.10, 7.44 and 7.59 (each 2H, each d-like). IR(CHCl3): 3516, 3448, 1708, 1650, 1594, 1514, 1494, 1483, 1288, 1248, 1032 cm−1. [α]D26+82.8±1.2°(c=1.000, MeOH) Anal. (C28H33NO4S.0.2H2O) Calcd.(%): C, 69.59; H, 6.97; N, 2.90; S, 6.64. Found(%): C, 69.69; H, 6.93; N, 3.20; S, 6.57.

[0299] Compound Number I-5

[0300] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.16-1.32(2H, m), 1.36-1.50(2H, m), 1.54-1.80 (4H, m), 2.00-2.22(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m), 3.82 (1H, m), 3.83(3H, s), 5.29-5.42(2H, m), 6.14(1H, d, J=7.2 Hz), 6.92 (2H, d-like), 7.20-7.30(2H, m), 7.41-7.51(4H, m). IR(CHCl3): 3509, 3444, 2666, 1708, 1654, 1592, 1570, 1510, 1494, 1468, 1288, 1247, 1082 cm−1. [α]D26+58.4±1.4°(c=0.704, MeOH) Anal. (C28H33NO4S.0.2H2O) Calcd.(%): C, 69.59; H, 6.97; N, 2.90; S, 6.64. Found(%): C, 69.55; H, 6.93; N, 3.03; S, 6.57.

[0301] Compound Number I-6

[0302] 1 H-NMR(CDCl3) δ: 1.11(1H, m), 1.20-1.34(2H, m), 1.42-1.52(2H, m), 1.56-1.78(4H, m), 2.00-2.23(5H, m), 2.35(2H, t, J=7.2 Hz), 2.57(1H, m), 3.89 (1H, m), 5.31-5.45(2H, m), 6.30(1H, d, J=7.2 Hz), 6.37 and 7.12(each 2H, each 2H, each J=2.1 Hz), 7.42 and 7.83(each 2H, each d-like). IR(CHCl3): 3518, 3448, 2662, 1708, 1653, 1609, 1499, 1334 cm−1. [α]D23+94.9±1.3°(c=1.005, MeOH) Anal. (C25H30N2O3.0.1H2O) Calcd.(%): C, 73.54; H, 7.45; N, 6.86. Found(%): C, 73.43; H, 7.46; N, 7.01.

[0303] Compound Number I-7

[0304] 1 H-NMR(CDCl3) δ: 1.12-1.76(9H, m), 1.96-2.24(5H, m), 2.33(2H, t, J=7.2 Hz), 2.53(1H, m), 3.86(1H, m), 5.30-5.47(2H, m), 6.60(1H, d, J=6.9 Hz), 7.05-7.23(5H, m), 7.55(1H, brs), 7.67 and 7.74(each 2H, each d, each J=8.7 Hz). IR(CHCl3): 3516, 3439, 3368, 1708, 1653, 1600, 1519, 1496, 1487, 1401, 1347, 1165 cm−1. [α]D25+69.9±1.1°(c=1.019, MeOH) Anal. (C27H34N2O5S.0.1H2O) Calcd.(%): C, 64.80; H, 6.89; N, 5.60; S, 6.41. Found(%): C, 64.73; H, 6.56; N, 5.74; S, 6.41.

[0305] Compound Number I-8

[0306] 1 H-NMR(CDCl3) δ: 1.19-1.27(3H, m), 1.35-1.43(2H, m), 1.55-1.80(4H, m), 1.90-2.08(3H, m), 2.11-2.21(2H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m), 3.74 (1H, m), 5.29-5.48(2H, m), 6.44(1H, d, J=6.9 Hz), 7.15(1H, d, J=1.5 Hz), 7.46(2H, t, J=7.8 Hz), 7.57(1H, m), 7.60(1H, d, J=1.5 Hz), 7.76-7.78 (2H, m), 7.89(1H, s). IR(CHCl3): 3440, 3360, 3107, 1708, 1637, 1518, 1448, 1329, 1163 cm−1. [α]D20+55.5±1.0°(c=1.003, MeOH) Anal. (C25H30N2O5S2.0.2H2O) Calcd.(%): C, 59.31; H, 6.05; N, 5.53; S, 12.67. Found(%): C, 59.19; H, 6.12; N, 5.66; S, 12.50.

[0307] Compound Number I-9

[0308] mp.193-194° C.; 1H-NMR (d6-DMSO) δ: 1.18-1.59 (9H, m), 1.93 (1H, d, J=2.4 Hz), 1.99-2.07(4H, m), 2.21(2H, t, J=7.2 Hz), 2.36(1H, m), 5.30-5.40(2H, m), 7.25(1H, d, J=1.5 Hz), 7.54-7.63(3H, m), 7.69(1H, d, J=1.5 Hz), 7.99-8.02 (3H, m), 11.6(1H, s), 12.00(1H, brs). IR(Nujol): 3367, 3221, 3186, 3091, 3055, 2654, 1711, 1631, 1566, 1541, 1321 cm−1. [α]D21+74.6±1.1°(c=1.006, MeOH) Anal. (C26H30N2O4S) Calcd.(%): C, 66.93; H, 6.48; N, 6.00; S, 6.87. Found(%): C, 66.76; H, 6.44; N, 5.88; S, 6.76.

[0309] Compound Number I-10

[0310] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.18-1.34(2H, m), 1.40-1.50(2H, m), 1.56-1.77(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.55(1H, m), 3.86 (1H, m), 5.31-5.54(2H, m), 6.26(1H, d, J=7.8 Hz), 6.31 and 7.14(each 2H, each t, each J=2.1 Hz), 7.84 and 7.88(each 2H, each d, each J=8.4 Hz). IR(CHCl3): 3515, 3441, 3144, 2669, 1708, 1662, 1515, 1486, 1455, 1376 cm−1. [α]D22+77.4±1.2°(c=1.004, MeOH) Anal. (C25H30N2O5S.0.2H2O) Calcd.(%): C, 63.32; H, 6.46; N, 6.91; S, 6.76. Found(%): C, 63.23; H, 6.49; N, 5.88; S, 6.67.

[0311] Compound Number I-11

[0312] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.18-1.29(2H, m), 1.42-1.46(2H, m), 1.56-1.79 (4H, m), 2.03-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.52(1H, m), 3.82(1H, m), 4.12(2H, s), 5.29-5.43(2H, m), 6.04(1H, d, J=7.5 Hz), 7.09(1H, d, J=1.5 Hz), 7.22-7.34(5H, m), 7.67(1H, d, J=1.5 Hz). IR (CHCl3): 3517, 3446, 2669, 1708, 1647, 1549, 1508, 1454 cm−1. [α]D21.5+68.8±1.1°(c=1.016, MeOH) Anal. (C26H31NO3S.0.1H2O) Calcd.(%): C, 71.07; H, 7.16; N, 3.19; S, 7.30. Found(%): C, 71.05; H, 7.11; N, 3.38; S, 7.33.

[0313] Compound Number I-12 1H-NMR(CDCl3) δ: 1.09(1H, m), 1.10-1.30(2H, m), 1.40-1.46(2H, m), 1.56-1.77 (4H, m), 2.00-2.22(5H, m), 2.33(2H, t, J=7.2 Hz), 2.52(1H, m), 3.83(1H, m), 5.28-5.42 (2H, m), 6.26(1H, d, J=6.9 Hz), 7.15 and 7.63(each 2H, each d, each J=8.7 Hz), 7.53(1H, m), 7.78-7.82(2H, m). IR(CHCl3): 3515, 3446, 3371, 3138, 1708, 1648, 1610, 1496, 1163 cm−1. [α]D22.5+66.5±1.1°(c=1.004, MeOH) Anal. (C27H34N2O5S.0.4H2O) Calcd.(%): C, 64.11; H, 6.93; N, 5.54; S, 6.34. Found(%): C, 64.05; H, 6.63; N, 5.56; S, 6.12.

[0314] Compound Number I-13

[0315] 1 H-NMR(CDCl3) δ: 1.19-1.31(3H, m), 1.36-1.44(2H, m), 1.55-1.78(4H, m), 1.85-2.02(2H, m), 2.05(1H, m), 2.13-2.47(4H, m), 2.57(1H, m), 3.71(1H, m), 5.31-5.54(2H, m), 6.53(1H, d, J=6.9 Hz), 7.14-7.32(5H, m), 7.47(1H, br), 8.05 and 8.13 (each 1H, each d, each J=1.5 Hz). IR(CHCl3): 3509, 3360, 3262, 1709, 1649, 1542, 1496, 1349, 1160 cm−1. [α]D23+59.1±1.1°(c=1.001, MeOH) Anal. (C25H30N2O5S2.0.2H2O) Calcd.(%): C, 59.31; H, 6.05; N, 5.53; S, 12.67. Found(%): C, 59.17; H, 6.01; N, 5.49; S, 12.37.

[0316] Compound Number I-14

[0317] 1 H-NMR(CDCl3) δ: 1.18-1.32(3H, m), 1.38-1.47(2H, m), 1.55-1.78(4H, m), 1.90-2.08(3H, m), 2.15-2.31(2H, m), 2.32-2.49(2H, m), 2.59(1H, m), 3.74 (1H, m), 5.33-5.53(2H, m), 6.35 and 7.17(each 2H, each t, each J=2.4 Hz), 6.47(1H, d, J=6.3 Hz), 8.21 and 8.22(each 1H, each d, each J=1.5 Hz). IR(CHCl3): 3506, 3412, 3144, 3107, 1727, 1709, 1656, 1540, 1504, 1456, 1382, 1166 cm−1. [α]D23+63.8±1.0°(c=1.005, MeOH) Anal. (C23H28N2O5S2.0.2H2O) Calcd.(%): C, 57.53; H, 5.96; N, 5.83; S, 13.35. Found(%): C, 57.44; H, 5.96; N, 6.00; S, 13.35.

[0318] Compound Number I-15

[0319] mp.128-130° C.; 1H-NMR(CDCl3) δ: 1.16-1.34(3H, m), 1.40-1.81(6H, m), 2.37 (2H, t, J=7.2 Hz), 2.57(1H, m), 3.89(1H, m), 5.35-5.51(2H, m), 6.37 and 7.20 (each 2H, each d, each J=2.4 Hz), 7.23(1H, d, J=8.7 Hz). IR (Nujol): 3371, 3097, 2662, 1716, 1703, 1671, 1652, 1530, 1367, 1361, 1187, 1162 cm−1. [α]D25+47.5±0.9°(c=1.003, MeOH) Anal. (C23H28N2O5S2) Calcd.(%): C, 57.96; H, 5.92; N, 5.88; S, 13.45. Found(%): C, 58.05; H, 5.91; N, 5.83; S, 13.38.

[0320] Compound Number I-16

[0321] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.20-1.32(2H, m), 1.42-1.47(2H, m), 1.58-1.75(4H, m), 2.01(3H, d, J=2 Hz), 2.00-2.16(5H, m), 2.35(2H, t, J=7.2 Hz), 2.55(1H, m), 3.86(1H, m), 5.31-5.44(2H, m), 6.14(1H, dd, J=1.5 and 3.0 Hz), 6.29(1H, d, J=7.5 Hz), 6.86(1H, m), 7.04(1H, t, J=3.0 Hz), 7.84 (4H, s). IR(CHCl3): 3517, 3441, 2667, 1708, 1661, 1515, 1485, 1375, 1260, 1178 cm−1. [α]D25+73.8±1.1°(c=1.001, MeOH) Anal. (C26H32N2O5S.0.1H2O) Calcd.(%): C, 64.20; H, 6.67; N, 5.76; S, 6.59. Found(%): C, 64.14; H, 6.65; N, 5.85; S, 6.86.

[0322] Compound Number I-17

[0323] 1 H-NMR(CDCl3) δ: 1.20-1.31(3H, m), 1.40-1.47(2H, m), 1.57-1.80(4H, m), 2.00-2.30(5H, m), 2.37(2H, t, J=6.9 Hz), 2.60(1H, m), 3.84(1H, m), 5.32-5.50(2H, m), 6.32(2H, t, J=2.4 Hz), 6.63(1H, d, J=6.6 Hz), 7.16(2H, t, J=2.4 Hz), 7.55(1H, t, J=8.0 Hz), 7.89(1H, m), 8.06(1H, d, J=7.8 Hz), 8.30(1H, t, J=1.7 Hz). IR(CHCl3): 3394, 3145, 1726, 1709, 1659, 1374 cm−1. [α]D25+60.3±1.0°(c=1.000, MeOH) Anal. (C25H30N2O5S.0.2H2O) Calcd.(%): C, 63.32; H, 6.46; N, 5.91; S, 6.76. Found(%): C, 63.39; H, 6.50; N, 6.16; S, 6.80.

[0324] Compound Number I-18

[0325] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.20-1.32(2H, m), 1.45(2H, t, J=6.9 Hz), 1.58-1.74(4H, m), 2.04-2.16(5H, m), 2.28(3H, s), 2.35(2H, t, J=6.9 Hz), 2.55 (1H, m), 3.87(1H, m), 5.31-5.44(2H, m), 5.96(1H, m), 6.18(1H, t, J=3.3 Hz), 6.32 (1H, d, J=7.5 Hz), 7.25(1H, dd, J=1.8 and 3.3 Hz), 7.78 and 7.85(each 2H, each d, each J=8.7 Hz). IR(CHCl3): 3514, 3441, 1708, 1661, 1515, 1487, 1368, 1164 cm−1. [α]D25+74.0±1.1°(c=1.004, MeOH) Anal. (C26H32N2O5S.0.2H2O) Calcd.(%): C, 63.96; H, 6.69; N, 5.74; S, 6.57. Found(%): C, 63.97; H, 6.69; N, 5.98; S, 6.54.

[0326] Compound Number I-19

[0327] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.18-1.31(2H, m), 1.41-1.49(2H, m), 1.56-1.76(4H, m), 2.00-2.21(5H, m), 2.34(2H, t, J=7.2 Hz), 2.55(1H, m), 3.86 (1H, m), 5.09(2H, s), 5.29-5.43(2H, m), 6.19(2H, t, J=2.1 Hz), 6.25(1H, d, J=7.5 Hz), 6.67(2H, t, J=2.1 Hz), 7.13 and 7.70(each 2H, each d, each J=8.4 Hz). IR(CHCl3): 3517, 3446, 3103, 2667, 1708, 1653, 1523, 1497 cm−1. [α]D25+57.7±1.0°(c=1.010, MeOH) Anal. (C26H32N2O3) Calcd.(%): C, 73.63; H, 7.70; N, 6.60. Found(%): C, 73.72; H, 7.77; N, 6.76.

[0328] Compound Number I-20

[0329] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.15-1.30(2H, m), 1.36-1.45(2H, m), 1.55-1.72 (4H, m), 2.00-2.14(5H, m), 2.32(2H, t, J=7.2 Hz), 2.51(1H, m), 3.82 (1H, m), 5.28-5.42(2H, m), 6.22(2H, d, J=7.5 Hz), 6.68(1H, d, J=3.6 Hz), 7.22-7.34(2H, m), 7.52-7.55(2H, m), 7.76 and 7.88(each 2H, each d, each J=8.7 Hz), 7.97(1H, d, J=8.1 Hz). IR(CHCl3): 3510, 3480, 3440, 3145, 3117, 1708, 1661, 1516, 1485, 1445, 1377, 1130 cm−1. [α]D25+65.9±1.1°(c=1.010, MeOH) Anal. (C29H32N2O5S.0.3H2O) Calcd.(%): C, 66.21; H, 6.25; N, 5.33; S,6.10. Found(%): C, 66.34; H, 6.30; N, 5.63; S,5.84.

[0330] Compound Number I-21

[0331] 1 H-NMR(CDCl3) δ: 1.13(1H, m), 1.20-1.31(2H, m), 1.44(2H, t, J=6.8 Hz), 1.59-1.72(4H, m), 2.03-2.20(5H, m), 2.32(2H, t, J=7.2 Hz), 2.54(1H, m), 3.83 (1H, m), 4.62(2H, s), 5.31-5.45(2H, m), 6.25-6.26(2H, m), 6.57(1H, d, J=7.2 Hz), 7.25(1H, m), 7.81(4H, s). IR(CHCl3): 3581, 3518, 3440, 3149, 1708, 1660, 1517, 1486, 1371, 1150 cm−1. [α]D27+72.2±1.1°(c=1.007, MeOH) Anal. (C26H32N2O6S) Calcd.(%): C, 62.38; H, 6.44; N, 5.60; S,6.40. Found(%): C, 62.17; H, 6.52; N, 5.71; S,6.40.

[0332] Compound Number I-22

[0333] 1 H-NMR(d6-DMSO) δ: 1.18-1.33(3H, m), 1.43-1.60(6H, m), 1.92-2.30(5H, m), 2.20(2H, t, J=7.5 Hz), 2.38(1H, m), 3.67(1H, m), 5.30-5.36(2H, m), 6.85 (1H, d, J=4.8 Hz), 7.27(1H, d, J=4.8 Hz), 7.86 and 7.94(each 2H, each d, each J=8.7 Hz), 8.37(1H, d, J=6.9 Hz). IR(KBr): 3360, 3151, 3103, 1707, 1635, 1569, 1530, 1328, 1284, 1140 cm−1. [α]D27+67.4±1.1°(c=1.007, DMSO) Anal. (C24H29N3O5S2.0.3H2O) Calcd.(%): C, 56.62; H, 5.86; N, 8.24; S,12.60. Found(%): C, 56.74; H, 5.96; N, 8.30; S,12.31.

[0334] Compound Number I-23

[0335] mp.231-232° C.; 1H-NMR(d6-DMSO) δ: 1.19-1.61(9H, m), 1.95-2.08(5H, m), 2.21(2H, t, J=7.2 Hz), 2.40(1H, m), 3.71(1H, m), 5.34-5.37(2H, m), 7.31 and 7.59(each 1H, each d, each J=3.6 Hz), 7.98 and 8.16(each 2H, each d, each J=8.7 Hz), 8.41(1H, d, J=7.2 Hz). IR(KBr): 3336, 3185, 2541, 1675, 1631, 1548, 1324, 1295, 1163 cm−1. [α]D27+84.5±1.3°(c=1.000, DMSO) Anal. (C24H29N3O4S) Calcd.(%):.C, 64.22; H, 6.25; N, 8.99; S,6.86. Found(%): C, 64.13; H, 6.10; N, 8.92; S,7.08.

[0336] Compound Number I-24

[0337] 1 H-NMR(CDCl3) δ: 1.14(1H, m), 1.22-1.35(2H, m), 1.44-1.53(2H, m), 1.58-1.78 (4H, m), 2.02-2.28(5H, m), 2.36(2H, t, J=7.2 Hz), 2.58(1H, m), 3.87(1H, m), 5.15-5.48(2H, m), 6.29 and 7.18(each 2H, each t, J=2.4 Hz), 6.38(1H, d, J=7.2 Hz), 7.77(1H, dd, J=1.8 and 8.7 Hz), 7.82(1H, s), 7.91(1H, d, J=8.7 Hz), 8.34(1H, d, J=1.8 Hz). IR(CHCl3): 3512, 3441, 3423, 3144, 2670, 1708, 1530, 1501, 1374, 1164 cm−1. [α]D26+96.1±1.4°(c=1.006, MeOH) Anal. (C27H30N2O5S2.0.2H2O) Calcd.(%): C, 61.16; H, 5.78; N, 5.28; S, 12.09. Found(%): C, 61.17; H, 5.74; N, 5.35; S, 12.12.

[0338] Compound Number I-25

[0339] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.17-1.31(2H, m), 1.39-1.48(2H, m), 1.56-1.77(4H, m), 1.99-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m), 3.84 (1H, m), 5.29-5.42(2H, m), 6.20(1H, d, J=7.2 Hz), 7.10-7.17(3H, m), 7.32 (1H, dd, J=1.2 and 3.6 Hz), 7.54(1H, dd, J=1.2 and 5.4 Hz), 7.60-7.64 (2H, m). IR(CHCl3): 3518, 3447, 2669, 1708, 1651, 1596, 1515, 1483 cm−1. [α]D26+84.7±1.2°(c=1.003, MeOH) Anal. (C25H29NO3S2.0.1H2O) Calcd.(%): C, 65.64; H, 6.43; N, 3.06; S, 14.02. Found(%): C, 65.58; H, 6.41; N, 3.10; S, 13.82.

[0340] Compound Number I-26

[0341] 1 H-NMR(CDCl3) δ: 1.13(1H, m), 1.20-1.33(2H, m), 1.41-1.50(2H, m), 1.56-1.77(4H, m), 2.00-2.21(5H, m), 2.37(2H, t, J=7.2 Hz), 2.55(1H, m), 3.87(1H, m), 5.31-5.45(2H, m), 6.48(1H, d, J=7.2 Hz), 7.10(1H, dd, J=3.9 and 5.1 Hz), 7.68(1H, dd, J=1.2 and 5.1 Hz), 7.69(1H, dd, J=1.2 and 3.9 Hz), 7.84-7.88 and 7.95-7.99(each 2H, each m). IR(CHCl3): 3518, 3441, 3382, 1708, 1659, 1515, 1329, 1158 cm−1. [α]D26+75.7±1.2°(c=1.000, MeOH) Anal. (C25H29NO5S2) Calcd.(%): C, 61.58; H, 5.99; N, 2.87; S, 13.15. Found(%): C, 61.36; H, 6.05; N, 2.91; S, 13.13.

[0342] Compound Number I-27

[0343] mp.213-215° C.; 1H-NMR(d6-DMSO) δ: 1.18-1.61(9H, m), 1.95-2.10 (5H, m), 2.21(2H, t, J=7.5 Hz), 2.40(1H, m), 3.71(1H, m), 5.33-5.38(2H, m), 7.19(1H, m), 7.87(1H, m), 7.96 and 8.10(each 2H, each d, each J=8.2 Hz), 8.21(1H, d, J=8.6 Hz), 8.40(1H, m), 10.92(1H, s), 12.05(1H, brs). IR (Nujol): 3337, 3249, 3205, 3132, 2524, 1678, 1632, 1545, 1433, 1305 cm−1. [α]D23+85.2±2.5°(c=0.505, MeOH) Anal. (C27H31N3O4.0.3H2O) Calcd.(%): C, 69.72; H, 6.80; N, 9.03. Found(%): C, 69.76; H, 6.75; N, 8.76.

[0344] Compound Number I-28

[0345] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.18-1.32(2H, m), 1.40-1.50(2H, m), 1.56-1.78(4H, m), 2.00-2.21(5H, m), 2.34(2H, t, J=7.2 Hz), 2.54(1H, m), 3.85 (1H, m), 5.29-5.42(2H, m), 6.17(1H, d, J=6.9 Hz), 7.07(1H, dd, J=1.2 and 5.1 Hz), 7.15(2H, d J=8.7 Hz), 7.43(1H, dd, J=3.0 and 5.1 Hz), 7.51(1H, dd, J=1.2 and 3.0 Hz), 7.62(2H, d, J=8.7 Hz). IR(CHCl3): 3510, 3447, 3110, 2666, 1708, 1651, 1596, 1515, 1482 cm−1. [α]D27+85.9±1.3°(c=1.007, MeOH) Anal. (C25H29NO3S2) Calcd.(%): C, 65.90; H, 6.42; N, 3.07; S, 14.07. Found(%): C, 65.60; H, 6.36; N, 3.36; S, 13.86.

[0346] Compound Number I-29

[0347] mp.123-125° C.; 1H-NMR (CDCl3) δ: 1.12(1H, m), 1.18-1.34(2H, m), 1.42-1.50(2H, m), 1.56-1.78(4H, m), 2.02-2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.55(1H, m), 3.88(1H, m), 5.31-5.45(2H, m), 6.42(1H, d, J=6.0 Hz), 7.31 (1H, d, J=5.1 Hz), 7.40(1H, dd, J=3.0 and 5.1 Hz), 7.87 and 7.96(each 2H, each d, each J=8.7 Hz), 8.11(1H, d, J=3.0 Hz). IR(Nujol): 3286, 3108, 2671, 1701, 1641, 1546, 1327, 1156 cm−1. [α]D27+75.3±1.2°(c=1.004, MeOH) Anal. (C25H29NO5S2) Calcd.(%): C, 61.58; H, 5.99; N, 2.87; S, 13.15. Found(%): C, 61.39; H, 5.94; N, 3.02; S, 12.99.

[0348] Compound Number I-30

[0349] 1 H-NMR(CDCl3) δ: 1.12(1H, m), 1.23-1.34(2H, m), 1.43-1.52(2H, m), 1.58-1.79(4H, m), 2.02-2.24(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m), 3.87 (1H, m), 5.32-5.45(2H, m), 6.11(1H, d, J=3.6 Hz), 6.28(1H, d, J=7.5 Hz), 6.35 and 7.09(each 2H, each t, each J=2.1 Hz), 7.16(1H, d, J=3.6 Hz). IR (CHCl3): 3512, 3438, 3142, 1741, 1709, 1653, 1623, 1564, 1508 cm−1. [α]D25+102.4±1.4°(c=1.006, MeOH) Anal. (C23H28N2O4.0.2H2O) Calcd.(%): C, 69.05; H, 7.15; N, 7.00. Found(%): C, 69.12; H, 7.10; N, 6.95.

[0350] Compound Number I-31

[0351] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.08-1.28(2H, m), 1.41-1.46(2H, m), 1.55-1.78(4H, m), 1.99-2.16(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.81(1H, m), 4.13(2H, s), 5.29-5.42(2H, m), 5.96(1H, d, J=8.1 Hz), 6.77(1H, ddd, J=0.9, 0.9 and 3.9 Hz), 7.20-7.35(5H, m), 7.37(1H, d, J=3.9 Hz). IR (CHCl3): 3511, 3445, 2670, 1708, 1642, 1544, 1507, 1455 cm−1. [α]D26+67.1±1.1°(c=1.015, MeOH) Anal. (C26H31NO3S) Calcd.(%): C, 71.36; H, 7.14; N, 3.20; S, 7.33. Found(%): C, 71.19; H, 7.16; N, 3.34; S, 7.26.

[0352] Compound Number I-32

[0353] 1 H-NMR(CDCl3) δ: 1.22-1.85(9H, m), 1.95-2.53(7H, m), 2.66(1H, m), 3.84(1H, m), 5.37-5.60(2H, m), 6.79(1H, d, J=6.0 Hz), 7.01-7.17(5H, m), 7.83 (1H, dd J=1.5 and 8.7 Hz), 7.53(1H, d, J=8.7 Hz), 7.89(1H, s), 8.35 (1H, s), 8.83(1H, d, J=1.5 Hz). IR(CHCl3): 3509, 3437, 3364, 3209, 1710, 1634, 1495, 1344, 1158 cm−1. [α]D26+36.6±0.8°(c=1.005, MeOH) Anal. (C29H32N2O5S2.0.2H2O) Calcd.(%): C, 62.61; H, 5.87; N, 5.04; S, 11.53. Found(%): C, 62.53; H, 5.87; N, 5.21; S, 11.42.

[0354] Compound Number I-33

[0355] 1 H-NMR(CDCl3) δ: 1.13(1H, m), 1.20-1.37(2H, m), 1.46-1.56(2H, m), 1.60-1.80 (4H, m), 2.02-2.28(5H, m), 2.38(2H, t, J=7.2 Hz), 2.64(1H, m), 3.94 (1H, m), 5.35-5.50(2H, m), 6.21(1H, d, J=7.2 Hz), 6.28 and 7.21(each 2H, each t, each J=2.4 Hz), 7.81(1H, dd, J=1.8 and 8.7 Hz), 7.91(1H, d, J=8.7 Hz), 7.99(1H, s), 8.97(1H, d, J=1.8 Hz). IR(CHCl3): 3513, 3438, 3144, 3096, 1708, 1656, 1518, 1374 cm−1. [α]D26+40.1±0.8°(c=1.010, MeOH) Anal. (C27H30N2O5S2.0.2H2O) Calcd.(%): C, 61.16; H, 5.78; N, 5.28; S,12.09. Found(%): C, 61.16; H, 5.76; N, 5.43; S, 12.05.

[0356] Compound Number I-34

[0357] 1 H-NMR(CDCl3) δ: 1.18-1.35(3H, m), 1.40-1.48(2H, m), 1.57-1.79(4H, m), 1.99-2.21(5H, m), 2.37(2H, t, J=7.2 Hz), 2.50(1H, m), 3.80(1H, m), 5.32-5.47(2H, m), 6.38(2H, t, J=2.4 Hz), 6.54(1H, d, J=7.5 Hz), 7.12 and 7.13(each 1H, each d, each J=3.6 Hz), 7.20(2H, t, J=2.4 Hz). IR(CHCl3): 3512, 3433, 3144, 2686, 1708, 1669, 1591, 1528, 1475, 1457, 1394 cm−1. [α]D26+74.3±1.1°(c=1.007, MeOH) Anal. (C23H28N2O5S) Calcd.(%): C, 59.98; H, 6.13; N, 6.08; S, 6.96. Found(%): C, 59.71; H, 6.22; N, 6.10; S, 7.02.

[0358] Compound Number I-35

[0359] mp.102-1.03° C.; 1H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.30(2H, m), 1.38-1.48(2H, m), 1.55-1.78(4H, m), 1.99-2.19(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81(1H, m), 5.20(2H, d, J=0.9 Hz), 5.30-5.42(2H, m), 5.99 (1H, d, J=7.2 Hz), 6.20 and 6.71 (each 2H, each t, each J=2.1 Hz), 6.86(1H, td, J=0.9 and 3.9 Hz), 7.37(1H, d, J=3.9 Hz). IR(Nujol): 3393, 3093, 6064, 2669, 1704, 1616, 1523, 1522 cm−1. [α]D26+71.1±1.1°(c=1.005, MeOH) Anal. (C24H30N2O3S) Calcd.(%): C, 67.58; H, 7.09; N, 6.57; S, 7.52. Found(%): C, 67.45; H, 7.09; N, 6.58; S, 7.67.

[0360] Compound Number I-36

[0361] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.18-1.31(2H, m), 1.40-1.48(2H, m), 1.56-1.78(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m), 3.82 (1H, m), 5.31-5.43(2H, m), 6.02(1H, d, J=7.2 Hz), 7.15 and 7.44 (each 1H, each d, each J=3.9 Hz), 7.20-7.33(5H, m). IR(CHCl3): 3511, 3444, 3426, 3031, 2665, 1708, 1646, 1530, 1499, 1477, 1421, 1318 cm−1. [α]D26+74.8±1.1°(c=1.004, MeOH) Anal. (C25H29NO3S2) Calcd.(%): C, 65.90; H, 6.42; N, 3.07; S, 14.07. Found(%): C, 65.61; H, 6.40; N, 3.19; S, 14.18.

[0362] Compound Number I-37

[0363] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.17-1.31(2H, m), 1.38-1.47(2H, m), 1.54-1.74(4H, m), 2.00-2.17(5H, m), 2.34(2H, t, J=7.2 Hz), 2.52(1H, m), 3.80 (1H, m), 5.30-5.43(2H, m), 6.27(1H, d, J=7.2 Hz), 7.41(1H, d, J=4.2 Hz), 7.51-7.64(4H, m), 7.98(2H, m). IR(CHCl3): 3515, 3442, 3366, 1708, 1656, 1530, 1504, 1327, 1156 cm−1. [α]D26+73.1±1.1°(c=1.004, MeOH) Anal. (C25H29NO5S2.0.2H2O) Calcd.(%): C, 61.13; H, 6.03; N, 2.85; S, 13.05. Found(%): C, 60.94; H, 6.02; N, 2.86; S, 3.12.

[0364] Compound Number I-38

[0365] mp.163-165° C. 1H-NMR(CDCl3) δ: 1.24-1.43(3H, m), 1.52-1.87 (8H, m), 2.10(1H, d, J=3.0 Hz), 2.30-2.55(4H, m), 2.71(1H, m), 3.66(1H, m), 5.38 and 5.63(each 1H, each m), 7.13(1H, d, J=1.5 Hz), 7.34(1H, d, J=5.4 Hz), 7.49-7.60(3H, m), 7.86-7.89(2H, m), 8.49(1H, s), 8.69(1H, d, J=1.5 Hz). IR(KBr): 3367, 3261, 3090, 1726, 1645, 1618, 1589, 1577, 1535, 1513, 1426, 1396, 1289, 1197 cm−1. [α]D23+84.5±1.2°(c=1.006, MeOH) Anal. (C26H30N2O4S) Calcd.(%): C, 66.93; H, 6.48; N, 6.00; S, 6.87. Found(%): C, 66.97; H, 6.36; N, 6.01; S, 6.89.

[0366] Compound Number I-39

[0367] 1 H-NMR(CDCl3) δ: 1.25-1.80(9H, m), 1.87-2.05(3H, m), 2.14-2.29(2H, m), 2.37(2H, t, J=6.9 Hz), 2.57(1H, m), 3.73(1H, m), 5.35 and 5.49(each 1H, each m), 6.71(1H, d, J=6.6 Hz), 6.87(1H, d, J=1.5 Hz), 7.43-7.48(2H, m), 7.56 (1H, m), 7.63(1H s), 7.64((1H, d, J=1.5 Hz), 7.73-7.76(2H, m). IR (CHCl3): 3510, 3379, 3247, 3108, 1709, 1637, 1556, 1516, 1448, 1365, 1319, 1161 cm−1. [α]D23+61.1±1.0°(c=1.004, MeOH) Anal. (C25H30N2O5S2.0.2H2O) Calcd.(%): C, 59.31; H, 6.05; N, 5.53; S, 12.67. Found(%): C, 59.38; H, 6.11; N, 5.75; S, 12.41.

[0368] Compound Number I-40

[0369] 1 H-NMR(CDCl3) δ: 1.11(1H, m), 1.24-1.31(2H, m), 1.44-1.52(2H, m), 1.60-1.79 (4H, m), 2.00-2.21(5H, m), 2.37(2H, t, J=7.2 Hz), 2.56(1H, m), 3.86 (1H, m), 5.32-5.46(2H, m), 6.11(1H, d, J=7.8 Hz), 7.25 and 7.49(each 1H, each d, each J=4.2 Hz), 7.30-7.43(3H, m), 7.60-7.63(2H, m). IR(CHCl3): 3510, 3445, 3428, 1739, 1708, 1643, 1540, 1510, 1491, 1454 cm−1. [α]D35+88.0±1.3°(c=1.012, MeOH) Anal. (C25H29NO3S.0.2H2O) Calcd.(%): C, 70.29; H, 6.94; N, 3.28; S, 7.51. Found(%): C, 70.35; H, 7.01; N, 3.59; S, 7.46.

[0370] Compound Number I-41

[0371] 1 H-NMR(CDCl3) δ: 1.13(1H, m), 1.22-1.32(2H, m), 1.46-1.51(2H, m), 1.60-1.76(4H, m), 2.04-2.17(5H, m), 2.36(2H, t, J=7.2 Hz), 2.57(1H, m), 3.86(1H, m), 5.32-5.46(2H, m), 6.30(1H, d, J=8.4 Hz), 7.48-7.65(5H, m), 7.84-7.88(2H, m). IR(CHCl3): 3511, 3443, 3425, 1708, 1643, 1529, 1506, 1448 cm−1. [α]D25+92.4±1.3°(c=1.000, MeOH) Anal. (C26H29NO4S2.0.2H2O) Calcd.(%): C, 68.61; H, 6.51; N, 3.08; S, 7.04. Found(%): C, 68.55; H, 6.52; N, 3.13; S, 7.03.

[0372] Compound Number I-42

[0373] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.27-1.31(2H, m), 1.49(2H, brs), 1.59-1.80 (4H, m), 2.00-2.20(5H, m), 2.36(2H, t, J=7.2 Hz), 2.55(1H, m), 3.85 (1H, m), 5.31-5.45(2H, m), 6.14(1H, d, J=7.2 Hz), 7.13(1H, d, J=3.9 Hz), 7.30 (1H, dd, J=1.2 and 5.1 Hz), 7.36(1H, dd, J=3.0 and 5.1 Hz), 7.45-7.46 (2H, m). IR(CHCl3): 3511, 3445, 3428, 3109, 1708, 1642, 1523, 1499, 1456 cm−1. [α]D25+82.9±1.20(c=1.006, MeOH) Anal. (C23H27NO3S2.0.1H2O) Calcd.(%): C, 64.04; H, 6.36; N, 3.25; S, 14.86. Found(%): C, 63.99; H, 6.52; N, 3.23; S, 14.85.

[0374] Compound Number I-43

[0375] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.22-1.31(2H, m), 1.46-1.51(2H, m), 1.60-1.80(4H, m), 2.03-2.22(5H, m), 2.37(2H, t, J=7.2 Hz), 2.55(1H, m), 3.85 (1H, m), 5.32-5.45(2H, m), 6.07(1H, d, J=7.5 Hz), 7.04(1H, dd, J=3.6 and 5.4 Hz), 7.11(1H, d, J=3.9 Hz), 7.24(1H, dd, J=1.2 and 3.6 Hz), 7.28(1H, dd, J=1.2 and 5.4 Hz), 7.42(1H, d J=3.9 Hz). IR(CHCl3): 3511, 3445, 3428, 3113, 3073, 2667, 1708, 1643, 1521, 1498, 1455 cm−1. [α]D25+89.5±1.30°(c=1.005, MeOH) Anal. (C23H27NO3S2.0.1H2O) Calcd.(%): C, 64.04; H, 6.36; N, 3.25; S, 14.86. Found(%): C, 63.93; H, 6.39; N, 3.46; S, 14.61.

[0376] Compound Number I-44

[0377] mp.146-147° C.; 1H-NMR(CDCl3) δ: 1.10(1H, m), 1.24-1.31(2H, m), 1.46-1.51(2H, m), 1.61-1.82(4H, m), 2.00-2.24(5H, m), 2.37(2H, t, J=7.2 Hz), 2.37(3H, s), 2.56(1H, m), 3.85(1H, m), 5.31-5.45(2H, m), 6.06(1H, d, J=6.9 Hz), 7.20 and 7.51(each 2H, each d, each J=9.0 Hz), 7.21 and 7.48(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3517, 3445, 3428, 1740, 1708, 1642, 1542, 1518, 1498, 1451 cm−1. [α]D26+89.3±1.3°(c=1.009, MeOH) Anal. (C26H31NO3S) Calcd.(%): C, 71.36; H, 7.14; N, 3.20; S, 7.33. Found(%): C, 71.51; H, 7.10; N, 3.20; S, 7.33.

[0378] Compound Number I-45

[0379] mp.110-116° C. 1H-NMR(CDCl3) δ: 1.10(1H, m), 1.24-1.31(2H, m), 1.46-1.51(2H, m), 1.61-1..83(4H, m), 2.00-2.25(5H, m), 2.37(2H, t, J=7.2 Hz), 2.56(1H, m), 3.84(3H, s), 3.85(1H, m), 5.31-5.45(2H, m), 6.04(1H, d, J=7.5 Hz), 6.93 and 7.55(each 2H, each d, each J=8.7 Hz), 7.15 and 7.46 (each 2H, each d, each J=4.2 Hz). IR(CHCl3): 3515, 3445, 3428, 1740, 1708, 1640, 1608, 1541, 1499, 1453, 1178 cm−1. [α]D26+88.0±1.3°(c=1.010, MeOH) Anal. (C26H31NO4S) Calcd.(%): C, 68.85; H, 6.89; N, 3.09; S, 7.07. Found(%): C, 68.87; H, 6.82; N, 3.11; S, 7.19.

[0380] Compound Number I-46

[0381] mp.124-125° C.,; 1H-NMR(CDCl3) δ: 1.10(1H, m), 1.24-1.32(2H, m), 1.46-1.51(2H, m), 1.61-1.82(4H, m), 2.00-2.24(5H, m), 2.37(2H, t, J=7.2 Hz), 2.56 (1H, m), 3.85(1H, m), 5.32-5.45(2H, m), 6.06(1H, d, J=7.2 Hz), 7.10 (2H, t, J=8.7 Hz), 6.19 and 7.47(each 1H, each d, each J=3.6 Hz), 7.56-5.60 (2H, m). IR(CHCl3): 3516, 3445, 3428, 2672, 1740, 1708, 1643, 1542, 1519, 1498, 1452 cm−1. [α]D26+83.3±1.2°(c=1.005, MeOH) Anal. (C25H28FNO,3S) Calcd.(%): C, 68.00; H, 6.39; N, 3.17; F, 4.30; S, 7.26. Found(%): C, 67.90; H, 6.34; N, 3.25; F, 4.31; S, 7.20.

[0382] Compound Number I-47

[0383] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.18-1.32(2H, m), 1.38-1.48(2H, m), 1.56-1.76(4H, m), 2.00-2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m), 3.81 (1H, m), 5.31-5.43(2H, m), 6.32(1H, d, J=7.5 Hz), 7.11(1H, dd, J=3.9 and 5.1 Hz), 7.4 and 7.62(each 1H, each d, each J=3.9 Hz), 7.70(1H, dd, J=1.5 and 5.1 Hz), 7.74(1H, dd, J=1.5 and 3.9 Hz). IR(CHCl3): 3516, 3442, 3378, 1708, 1655, 1530, 1504, 1336, 1153 cm−1. [α]D25+74.3±1.1°(c=1.000, MeOH) Anal. (C23H27NO5S3.0.1H2O) Calcd.(%): C, 55.76; H, 5.53; N, 2.83; S, 19.41. Found(%): C, 55.49; H, 5.64; N, 3.09; S, 19.32.

[0384] Compound Number I-48

[0385] mp.112-115° C. 1H-NMR(CDCl3) δ: 1.13-1.30(3H, m), 1.34-1.45 (2H, m), 1.50-1.82(4H, m), 1.94-2.27(5H, m), 2.34(2H, t, J=7.2 Hz), 2.56 (1H, m), 3.74(1H, m), 5.22(2H, s), 5.31-5.50(2H, m), 6.64(1H, d, J=6.6 Hz), 6.84 (1H, (1, J=3.9 Hz), 6.93 and 7.05(each 1H, each s), 7.47(1H, d, J=3.9 Hz), 7.66(1H, s). IR(Nujol): 3339, 3102, 2464, 1691, 1635, 1622, 1551, 1288 cm−1. [α]D25+71.2±1.1°(c=1.005, MeOH) Anal. (C23H29N3O3S) Calcd.(%): C, 64.61; H, 6.84; N, 9.83; S, 7.50. Found(%): C, 64.54; H, 6.85; N, 9.78; S, 7.42.

[0386] Compound Number I-49

[0387] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.16-1.30(2H, m), 1.38-1.47(2H, m), 1.54-1.77(4H, m), 1.98-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.52(1H, m), 3.79 (1H, m), 5.30-5.42(2H, m), 5.47(2H, s), 6.16(1H, d, J=6.9 Hz), 6.30(1H, t, J=2.1 Hz) 6.94 and 7.41(each 1H, each d, each J=3.6 Hz), 7.47 and 7.57 (each 1H, each d, each J=2.1 Hz). IR(CHCl3): 3510, 3444, 3426, 1709, 1646, 1546, 1512 cm−1. [α]D25+68.6±1.1°(c=1.011, MeOH) Anal. (C23H29N3O3S.0.1H2O) Calcd.(%): C, 64.34; H, 6.85; N, 9.79; S, 7.47. Found(%): C, 64.10; H, 6.93; N, 9.90; S, 7.52.

[0388] Compound Number I-50

[0389] mp.126-128° C.; 1H-NMR(CDCl3) δ: 1.12(1H, m), 1.18-1.33(2H, m), 1.40-1.50(2H, m), 1.55-1.78(4H, m), 2.00-2.21(5H, m), 2.54(1H, m), 3.87(1H, m), 5.30-5.44(2H, m), 6.43(1H, d, J=6.6 Hz), 7.48-7.62(3H, m), 7.83-7.95(5H, m). IR(Nujol): 3284, 3058, 2669, 1701, 1641, 1546, 1326, 1294, 1160 cm−1. [α]hd D25+77.2±1.2°(c=1.007, MeOH) Anal. (C27H31NO5S) Calcd.(%): C, 67.34; H, 6.49; N, 2.91; S, 6.66. Found(%): C, 67.20; H, 6.38; N, 2.88; S, 6.58.

[0390] Compound Number I-51

[0391] mp.103-107° C. 1H-NMR(CDCl3) δ: 1.14(1H, m), 1.18-1.33(2H, m), 1.40-1.50(2H, m), 1.54-1.77(4H, m), 2.00-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.54(1H, m), 3.85(3H, s), 3.86(1H, m), 5.30-5.45(2H, m), 6.48(1H, d, J=6.9 Hz), 6.96(2H, m), 7.81-7.91(6H, m). IR(Nujol): 3273, 3067, 2669, 1702, 1639, 1560, 1548, 1323, 1301, 1274, 1156 cm−1. [α]D25+75.4±1.2°(c=1.002, MeOH) Anal. (C28H33NO6S) Calcd.(%): C, 65.73; H, 6.50; N, 2.74; S, 6.27. Found(%): C, 65.50; H, 6.46; N, 2.82; S, 6.25.

[0392] Compound Number I-52

[0393] 1 H-NMR(CDCl3) δ: 1.17(1H, m), 1.26-1.34(2H, m), 1.47-1.53(2H, m), 1.60-1.76(4H, m), 2.04-2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.60(1H, m), 3.91(1H, m), 5.32-5.47(2H, m), 6.46(1H, d, J=8.4 Hz), 7.17(1H, dd, J=3.9 and 5.1 Hz), 7.61(1H, dd, J=1.2 and 3.9 Hz), 7.76(1H, dd, J=1.2 and 5.1 Hz), 7.87(4H, s-like). IR(CHCl3): 3518, 3444, 2663, 1708, 1638, 1517, 1494, 1414 cm−1. [α]D25+86.6±1.3°(c=1.008, MeOH) Anal. (C26H29NO4S) Calcd.(%): C, 69.15; H, 6.47; N, 3.10; S, 7.10. Found(%): C, 68.86; H, 6.70; N, 3.15; S, 6.95.

[0394] Compound Number I-53

[0395] mp.144-145° C.; 1H-NMR(CDCl3) δ: 1.20-2.54(16H, m), 2.62(1H, m), 3.69 (3H, s), 5.35-5.56(2H, m), 6.36 and 7.17(each 2H, each t, each J=2.4 Hz), 6.66(1H, d, J=6.3 Hz), 8.05 and 8.07(each 1H, each d, each J=1.5 Hz). IR(Nujol): 3509, 3406, 3146, 3110, 1728, 1708, 1653, 1535, 1375, 1189, 1166 cm−1. [α]D25+67.9±1.1°(c=1.007, MeOH) Anal. (C23H28N2O5S2) Calcd.(%): C, 57.96; H, 5.92; N, 5.88; S, 13.45. Found(%): C, 58.19; H, 5.95; N, 5.75; S, 13.09.

[0396] Compound Number I-54

[0397] 1 H-NMR(CDCl3) δ: 1.22-2.57(16H, m), 2.68(1H, m), 3.66(3H, s), 5.37-5.63 (2H, m), 6.20, 6.35, 6.74 and 6.87(each 2H, each t, each J=2.4 Hz), 6.92 (1H, d, J=5.4 Hz), 8.27(1H, s). IR(CHCl3): 3402, 3143, 3108, 1725, 1710, 1650, 1516, 1375 cm−1. [α]D26+70.0±1.1°(c=1.006, MeOH) Anal. (C27H31N3O5S2.0.3H2O) Calcd.(%): C, 59.28; H, 5.82; N, 7.68; S, 11.72. Found(%): C, 59.28; H, 5.77; N, 5.58; S, 11.68.

[0398] Compound Number I-55

[0399] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.18-1.31(2H, m), 1.40-1.45(2H, m), 1.57-1.74(4H, m), 2.00-2.10(5H, m), 2.35(2H, t, J=7.2 Hz), 2.38(3H, s), 2.52 (1H, m), 3.80(1H, m), 5.31-5.43(2H, m), 5.99(1H, m), 6.20(1H, t, J=3.3 Hz), 6.30(1H, d, J=6.91 Hz), 7.18(1H, dd, J=1.8 and 3.3 Hz), 7.40 and 7.53(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3513, 3442, 3149, 3100, 1708, 1657, 1530, 1504, 1375, 1183, 1161 cm−1. [α]D27+70.3±1.5°(c=0.730, MeOH) Anal. (C24H30N2O5S2.0.4H2O) Calcd.(%): C, 57.90; H, 6.24; N, 5.63; S, 12.88. Found(%): C, 58.08; H, 6.28; N, 5.77; S, 12.54.

[0400] Compound Number I-56

[0401] 1 H-NMR((d6-DMSO) δ: 1.06-1.59(9H, m), 1.93-2.07(5H, m), 2.21(2H, t, J=7.2 Hz), 2.35(1H, m), 3.65(1H, m), 5.30-5.41(2H, m), 6.90 and 7.69 (each 1H, each d, each J=4.2 Hz), 7.55-7.64(3H, m), 7.99-8.04(3H, m), 11.73 (1H, s), 12.01(1H, brs). IR (KBr): 3562, 1708, 1616, 1564, 1523, 1454, 1295 cm−1. [α]D27+71.2±1.1°(c=1.000, MeOH) Anal. (C26H30N2O4S.0.2H2O) Calcd.(%): C, 66.42; H, 6.52; N, 5.96; S, 6.82. Found(%): C, 66.43; H, 6.32; N, 6.17; S, 6.75.

[0402] Compound Number I-57

[0403] 1 H-NMR(d6-DMSO) δ: 1.05-1.56(9H, m), 1.91-2.05(5H, m), 2.19(2H, t, J=7.2 Hz), 2.29(1H, m), 3.56(1H, m), 5.28-5.38(2H, m), 6.54 and 7.56(each 1H, each d, each J=4.2 Hz), 7.59-7.62(3H, m), 7.76-7.79(2H, m), 8.06(1H, d, J=6.9 Hz), 11.10(1H, s), 11.99(1H, brs). IR(KBr): 3384, 3084, 1707, 1616, 1553, 1523, 1459, 1350, 1322, 1161 cm−1. [α]D27+62.4±1.0°(c=1.005, MeOH) Anal. (C25H30N2O5S2.0.2H2O) Calcd.(%): C, 59.31; H, 6.05; N, 5.53; S, 12.66. Found(%): C, 59.36; H, 5.75; N, 5.55; S, 12.38.

[0404] Compound Number I-58

[0405] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.17-1.33(2H, m), 1.36-1.50(2H, m), 1.54-1.75(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.45(3H, s), 2.52 (1H, m), 3.80(1H, m), 5.31-5.43(2H, m), 6.12(1H, d, J=7.5 Hz), 6.32 and 7.18(each 2H, each t, each J=2.4 Hz), 7.22(1H, s). IR(CHCl3): 3316, 3442, 3145, 2668, 1708, 1657, 1545, 1509, 1455, 1375, 1190, 1165, 1057 cm−1. [α]D26+75.8±1.2°(c=1.002, MeOH) Anal. (C24H30N2O5S2.0.1H2O) Calcd.(%): C, 58.54; H, 6.18; N, 5.69; S, 13.02. Found(%): C, 58.35; H, 6.29; N, 5.74; S, 12.92.

[0406] Compound Number I-59

[0407] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.16-1.30(2H, m), 1.38-1.48(2H, m), 1.53-1.79(4H, m), 1.98-2.17(5H, m), 2.34(2H, t, J=7.2 Hz), 2.50(1H, m), 3.79(1H, m), 5.30-5.42(2H, m), 6.00(1H, d, J=7.5 Hz), 7.01(1H, dd, J=3.6 and 5.4 Hz), 7.03(1H, d, J=3.9 Hz), 7.29(1H, dd, J=1.2 and 3.6 Hz), 7.33(1H, d, J=3.9) 7.43(1H, dd, J=1.2 and 5.4 Hz). IR(CHCl3): 3517, 3444, 3426, 2670, 1708, 1645, 1530, 1499, 1421, 1318 cm−1. [α]D26+70.8±1.1°(c=1.018, MeOH) Anal. (C23H27NO3S3) Calcd.(%): C, 59.84; H, 5.89; N, 3.03; S, 20.84. Found(%): C, 59.73; H, 5.99; N, 3.15; S, 20.70.

[0408] Compound Number I-60

[0409] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.17-1.32(2H, m), 1.40-1.50(2H, m), 1.56-1.80(4H, m), 1.99-2.21(5H, m), 2.34(2H, t, J=7.2 Hz), 2.54(1H, m), 3.85 (1H, m), 5.29-5.42(2H, m), 6.20(1H, d, J=6.9 Hz), 7.23-7.45(7H, m), 7.55 (2H, d, J=8.1 Hz). IR(CHCl3): 3516, 3447, 2667, 1708, 1651, 1596, 1514, 1481 cm−1. [α]D26+89.1±1.3°(c=1.006, MeOH) Anal. (C27H31NO3S.0.2H2O) Calcd.(%): C, 71.56; H, 6.98; N, 3.09; S, 7.07. Found(%): C, 71.39; H, 6.97; N, 3.16; S, 6.94.

[0410] Compound Number I-61

[0411] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.18-1.31(2H, m), 1.41-1.50(2H, m), 1.55-1.80(4H, m), 1.99-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.82(1H, m), 5.31-5.43(2H, m), 5.97(1H, d, J=6.6 Hz), 6.45(1H, d, J=4.2 Hz), 7.11-7.20(3H, m), 7.28(1H, d, J=4.2 Hz), 7.33-7.40(2H, m). IR(CHCl3): 3515, 3445, 3427, 2667, 1740, 1708, 1640, 1506, 1475 cm−1. [α]D27+71.3±1.1°(c=1.002, MeOH) Anal. (C25H29NO4S) Calcd.(%): C, 68.31; H, 6.65; N, 3.19; S, 7.29. Found(%): C, 68.41; H, 6.87; N, 3.22; S, 7.35.

[0412] Compound Number I-62

[0413] 1 H-NMR(CDCl3) δ: 1.14(1H, m), 1.20-1.35(2H, m), 1.42-1.54(2H, m), 1.57-1.77(4H, m), 2.00-2.23(5H, m), 2.35(2H, t, J=7.2 Hz), 2.58(1H, m), 3.88(1H, m), 5.32-5.46(2H, m), 6.31 and 7.19(each 2H, each t, each J=2.4 Hz), 6.33(1H, d, J=7.5 Hz), 7.77(1H, dd, J=1.8 and 8.4 Hz), 7.77(1H, s), 7.87(1H, d, J=8.4 Hz), 8.38(1H, d, J=1.8 Hz). IR(CHCl3): 3514, 3442, 3422, 3144, 2670, 1708, 1654, 1525, 1375, 1193, 1171 cm−1. [α]D26+89.8±1.3°(c=1.000, MeOH) Anal. (C27H3N2O5S2) Calcd.(%): C, 61.58; H, 5.74; N, 5.32; S, 12.17. Found(%): C, 61.42; H, 5.86; N, 5.57; S, 11.98.

[0414] Compound Number I-63

[0415] mp.180-181° C.; 1H-NMR(CDCl3) δ: 1.04(1H, m), 1.22-1.30(2H, m), 1.41-1.46 (2H, m), 1.59-1.82(4H, m), 1.94-2.16(3H, m), 2.25-2.37(2H, m), 2.42 (2H, t, J=6.9 Hz), 2.52(1H, m), 2.52(3H, s), 3.79(1H, m), 5.41-5.59(2H, m), 5.73(1H, d, J=6.6 Hz), 7.48-7.53(2H, m), 7.60(1H, m), 8.07-8.10(2H, m). IR(Nujol): 3372, 3173, 3053, 2544, 1690, 1672, 1632, 1559, 1496, 1362, 1317 cm−1. [α]D28+77.7±1.2°(c=1.007, MeOH) Anal. (C26H31N3O4S) Calcd.(%): C, 64.84; H, 6.49; N, 8.72; S, 6.66. Found(%): C, 64.66; H, 6.31; N, 8.73; S, 6.65.

[0416] Compound Number I-64

[0417] 1 H-NMR(d6-DMSO) δ: 1.07(1H, m), 1.28-1.58(8H, m), 1.91-2.08(5H, m), 2.20(2H, t, J=7.2 Hz), 2.31(3H, s), 2.32(1H, s), 3.96(1H, m), 5.28-5.40(2H, m), 7.52-7.62(3H, m), 7.80-7.83(2H, m), 7.94(1H, d, J=6.9 Hz). IR(Nujol): 3316, 3161, 3106, 2677, 1709, 1629, 1531, 1284, 1142 cm−1. [α]D27+76.2±1.2°(c=1.002, MeOH) Anal. (C25H31N3O5S2.0.1H2O) Calcd.(%): C, 57.80; H, 6.05; N, 8.09; S, 12.34. Found(%): C, 57.59; H, 6.15; N, 8.10; S, 12.57.

[0418] Compound Number I-65

[0419] 1 H-NMR(CDCl3) δ: 1.28-1.31(2H, m), 1.47(2H, brs), 1.56-1.84(4H, m), 1.94-2.30(5H, m), 2.39(2H, t, J=6.9 Hz), 2.62(1H, s), 2.63(3H, s), 3.77(1H, m), 5.35-5.67(2H, m), 6.42(1H, d, J=6.3 Hz), 7.29-7.43(3H, m), 7.46(1H, s), 7.72(2H, d, J=7.2 Hz). IR(CHCl3): 3517, 3421, 3350, 3150, 2538, 1708, 1651, 1590, 1512, 1474, 1442, 1164 cm−1. [α]D28+100.8±1.4°(c=1.002, MeOH) Anal. (C27H31N3O3S.0.5H2O) Calcd.(%): C, 66.64; H, 6.63; N, 8.63; S, 6.59. Found(%): C, 66.55; H, 6.59; N, 8.68; S, 6.76.

[0420] Compound Number I-66

[0421] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.19-1.33(2H, m), 1.42-1.50(2H, m), 1.58-1.79(4H, m), 2.01-2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.55(1H, m), 3.86(1H, m), 4.37(2H, s), 5.30-5.43(2H, m), 6.19(1H, d, J=7.5 Hz), 6.90(1H, dd, J=3.6 and 5.1 Hz), 6.93(1H, m), 7.17(1H, dd, J=1.2 and 5.1 Hz), 7.33 and 7.65(each 2H, each d, J=8.4 Hz). IR(CHCl3): 3518, 3447, 2665, 1708, 1651, 1596, 1515, 1484 cm−1. [α]D26+82.4±1.4°(c=0.900, MeOH) Anal. (C26H31NO3S2.0.1H2O) Calcd.(%): C, 66.24; H, 6.67; N, 2.97; S, 13.60. Found(%): C, 66.14; H, 6.72; N, 2.96; S, 13.53.

[0422] Compound Number I-67

[0423] 1 H-NMR(CDCl3) δ: 1.16(1H, m), 1.21-1.34(2H, m), 1.43-1.52(2H, m), 1.57-1.76(4H, m), 2.04-2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.56(1H, m), 3.89 (1H, m), 4.53(2H, s), 5.33-5.48(2H, m), 6.58(1H, d, J=6.9 Hz), 6.83(1H, dd, J=1.2 and 3.9 Hz), 6.93(1H, dd, J=3.9 and 5.1 Hz), 7.28(1H, dd, J=1.2 and 5.1 Hz), 7.65 and 7.81(each 2H, each d, J=8.4 Hz). IR(CHCl3): 3518, 3442, 3373, 2666, 1708, 1658, 1516, 1483, 1323, 1153 m−1. [α]D26+69.6±1.1°(c=1.003, MeOH) Anal. (C26H31NO5S2.0.5H2O) Calcd.(%): C, 61.15; H, 6.32; N, 2.74; S, 12.56. Found(%): C, 66.16; H, 6.25; N, 2.90; S, 12.57.

[0424] Compound Number I-68

[0425] 1 H-NMR(CDCl3) δ: 1.13(1H, m), 1.20-1.32(2H, m), 1.38-1.50(2H, m), 1.54-1.77(4H, m), 1.98-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m), 3.80 (1H, m), 5.31-5.46(2H, m), 6.47(1H, d, J=7.5 Hz), 6.87(1H, dd, J=1.5 and 3.6 Hz), 3.84(1H, dd, J=3.6 and 5.4 Hz), 7.03(1H, dd, J=1.5 and 5.4 Hz), 7.33 and 7.38(each 1H, each d, each J=3.9 Hz), 7.90(1H, br). IR(CHCl3): 3510, 3440, 3358, 3109, 1708, 1647, 1533, 1505, 1364, 1331, 1161 cm−1. [α]43629+151.3±1.9°(c=1.010, MeOH) Anal. (C23H28N2O5S3.0.1H2O) Calcd.(%): C, 54.12; H, 5.57; N, 5.49; S, 18.84. Found(%): C, 53.84; H, 5.46; N, 5.38; S, 18.62.

[0426] Compound Number I-69

[0427] 1 H-NMR(CDCl3) δ: 1.20(1H, m), 1.26-1.38(2H, m), 1.42-1.52(2H, m), 1.57-1.76(4H, m), 2.00-2.24(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m), 3.88 (1H, m), 5.31-5.49(2H, m), 6.63(1H, dd, J=1.2 and 3.9 Hz), 6.69(1H, d, J=7.5 Hz), 6.77(1H, dd, J=3.9 and 5.4 Hz), 6.98(1H, dd, J=1.2 and 5.4 Hz), 7.66 and 7.76(each 2H, each d, each J=8.4 Hz). IR(CHCl3): 3509, 3439, 3363, 3111, 1707, 1651, 1520, 1328, 1167 cm−1. [α]43629+155.7±2.0°(c=1.003, MeOH) Anal. (C25H30N2O5S3.0.3H2O) Calcd.(%): C, 59.10; H, 6.07; N, 5.51; S, 12.62. Found(%): C, 59.00; H, 5.95; N, 5.51; S, 12.46.

[0428] Compound Number I-70

[0429] mp.187-188° C.; 1H-NMR(d6-DMSO) δ: 1.16-1.62(9H, m), 1.90-2.14(5H, m), 2.21(2H, t, J=7.2 Hz), 2.38(1H, m), 3.66(1H, m), 5.27-5.41(2H, m), 7.10-7.15 (1H, m), 7.34-7.39(2H, m), 7.42-7.75(2H, m), 7.91 and 7.99(each 1H, each d, each J=3.9 Hz), 8.04(1H, d, J=6.6 Hz), 10.32(1H, s), 12.02(1H, s). IR(Nujol): 3316, 3075, 2678, 1704, 1635, 1614, 1544, 1323 cm−1. [α]D28+83.3±1.2°(c=1.003, MeOH) Anal. (C26H30N2O4S) Calcd.(%): C, 66.93; H, 6.48; N, 6.00; S, 6.87. Found(%): C, 67.04; H, 6.45; N, 5.98; S, 6.96.

[0430] Compound Number I-71

[0431] mp.192-194° C.; 1H-NMR(d6-DMSO) δ: 1.16-1.62(9H, m), 1.90-2.14(5H, m), 2.21(2H, t, J=7.2 Hz), 2.37(1H, m), 3.65(1H, m), 5.29-5.41(2H, m), 7.18-7.24 (2H, m), 7.33-7.78(2H, m), 7.91 and 7.97(each 1H, each d, each J=3.9 Hz), 8.04(1H, d, J=6.9 Hz), 10.38(1H, s), 12.01(1H, s). IR(Nujol): 3322, 3278, 3150, 3098, 3077, 2678, 1704, 1635, 1615, 1546, 1521, 1508, 1322 cm−1. [α]D2+83.3±1.2°(c=1.000, MeOH) Anal. (C26H29FN2O4S) Calcd.(%): C, 64.44; H, 6.03; N, 5.78; F, 3.92; S, 6.62. Found(%): C, 64.36; H, 6.00; N, 5.81; F, 3.94; S, 6.46.

[0432] Compound Number I-72

[0433] mp.192-193° C.; 1H-NMR(d6-DMSO) δ: 1.16-1.62(9H, m), 1.92-2.14 (5H, m), 2.21(2H, t, J=7.2 Hz), 2.37(1H, m), 3.66(1H, m), 3.75(3H, s), 5.30-5.41(2H, m), 6.94 and 7.63(each 2H, each d-like), 7.89 and 7.94(each 1H, each d, each J=3.9 Hz), 8.38(1H, d, J=6.9 Hz), 10.21(1H, s), 12.01(1H, s). IR(Nujol): 3316, 3075, 2678, 1704, 1635, 1614, 1544, 1323 cm−1. [α]D27+81.6±1.2°(c=1.000, MeOH) Anal. (C27H132N2O5S) Calcd.(%): C, 65.30; H, 6.49; N, 5.64; S, 6.46. Found(%): C, 65.19; H, 6.49; N, 5.45; S, 6.31.

[0434] Compound Number I-73

[0435] 1 H-NMR(CDCl3) δ: 1.14(1H, m), 1.18-1.32(2H, m), 1.40-1.78(6H, m), 1.94-2.20 (5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80(1H, m), 3.81(6H, s), 3.82(3H, s), 5.30-5.44(2H, m), 6.56(1H, d, J=7.2 Hz), 6.97(2H, s), 7.47 and 7.58(each 1H, each d, each J=3.9 Hz), 8.43(1H, s). IR(CHCl3): 3515, 3438, 3317, 1708, 1650, 1607, 1537, 1508, 1454, 1412, 1131 cm−1. [α]D27+75.8±1.2°(c=1.009, MeOH) Anal. (C29H36N2O7S.0.4H2O) Calcd.(%): C, 61.77; H, 6.58; N, 4.97; S, 5.69. Found(%): C, 61.74; H, 6.64; N, 4.89; S, 5.89.

[0436] Compound Number I-74

[0437] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.20-1.33(2H, m), 1.43-1.52(2H, m), 1.57-1.78(4H, m), 2.00-2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.55(1H, m), 3.85(1H, m), 5.32-5.45(2H, m), 6.09(1H, d, J=6.9 Hz), 6.32 and 7.00(each 2H, each t, each J=2.1 Hz), 6.81 and 7.34(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3515, 3445, 3109, 2678, 1 740, 1708, 1642, 1507, 1489 cm−1. [α]D26+83.5±1.2°(c=1.007, MeOH) Anal. (C23H28N2O3S) Calcd.(%): C, 66.96; H, 6.84; N, 6.79; S, 7.77. Found(%): C, 66.66; H, 6.74; N, 6.74; S, 7.61.

[0438] Compound Number I-75

[0439] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.20-1.32(2H, m), 1.39-1.49(2H, m), 1.57-1.66(4H, m), 2.01-2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.56(1H, m), 3.88(1H, m), 3.95(2H, s), 5.30-5.44(2H, m), 6.27(1H, d, J=7.5 Hz), 6.89-6.91(2H, m), 7.32(1H, dd, J=2.4 and 3.9 Hz), 7.19 and 7.66(each 2H, each d, J=8.4 Hz). IR(CHCl3): 3516, 3447, 2670, 1708, 1651, 1523, 1496 m−1. [α]D26+71.8±1.1°(c=1.016, MeOH) Anal. (C26H3NO3S2.0.1H2O) Calcd.(%): C, 66.24; H, 6.67; N, 2.97; S, 13.60. Found(%): C, 66.36; H, 6.67; N, 3.27; S, 13.62.

[0440] Compound Number I-76

[0441] mp.135-136° C.; 1H-NMR(CDCl3) δ: 1.12(1H, m), 1.22-1.33(2H, m), 1.43-1.51(2H, m), 1.59-1.78(4H, m), 2.03-2.22(5H, m), 2.35(2H, t, J=;7.2 Hz), 2.56 (1H, m), 3.87(1H, m), 4.44(2H, s), 5.31-5.45(2H, m), 6.30(1H, d, J=7.2 Hz), 7.08(1H, dd, J=3.9 and 5.1 Hz), 7.23(2H, d, J=8.4 Hz), 7.40(1H, dd, J=1.5 and 3.9 Hz), 7.69-7.71(3H, m). IR(CHCl3): 3516, 3445, 3096, 2665, 1708, 1655, 1523, 1496, 1403, 1327, 1152, 1127 m−1. [α]D26+65.0±1.1°(c=1.000, MeOH) Anal. (C26H31NO5S2.0.2H2O) Calcd.(%): C, 61.81; H, 6.26; N, 2.77; S, 12.69. Found(%): C, 61.76; H, 6.20; N, 2.90; S, 12.57.

[0442] Compound Number I-77

[0443] mp.215-217° C. 1H-NMR(d6-DMSO) δ: 1.16-1.62(9H, m), 1.90-2.14 (5H, m), 2.21(2H, t, J=7.2 Hz), 2.38(1H, m), 3.66(1H, m), 5.29-5.41 (2H, m), 6.91-6.94(2H, m), 7.05(1H, dd, J=2.4 and 4.2 Hz), 7.93 and 7.96 (each 1H, each d, each J=4.2 Hz), 8.43(1H, d, J=6.6 Hz), 10.67(1H, br), 12.01 (1H, br). IR(Nujol): 3315, 3222, 3097, 3049, 2672, 1705, 1621, 1548, 1504, 1311 cm−1. [α]D27+88.2±1.3°(c=1.009, MeOH) Anal. (C24H28N2O4S2) Calcd.(%): C, 60.99; H, 5.97; N, 5.93; S, 13.57. Found(%): C, 60.94; H, 5.74; N, 5.91; S, 13.61.

[0444] Compound Number I-78

[0445] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.18-1.31(2H, m), 1.40-1.47(2H, m), 1.57-1.73(4H, m), 2.00-2.12(5H, m), 2.31(2H, t, J=7.2 Hz), 2.56(1H, m), 3.79 (1H, m), 4.70(2H, s), 5.30-5.45(2H, m), 6.26-6.30(2H, m), 6.34(1H, d, J=6.9 Hz), 7.22(1H, dd, J=1.8 and 3.3 Hz), 7.41 and 7.62(each 1H, each d, each J=4.2 Hz). IR(CHCl3): 3589, 3516, 3441, 3355, 3100, 1708, 1656, 1530, 1504, 1377, 1180, 1147 cm−1. [α]D26.5+70.8±1.1°(c=1.009, MeOH) Anal. (C24H30N2O6S2.0.2H2O) Calcd.(%): C, 56.50; H, 6.01; N, 5.49; S, 12.57. Found(%): C, 56.43; H, 6.02; N, 5.61; S, 12.47.

[0446] Compound Number I-79

[0447] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.16-1.30(2H, m), 1.38-1.50(2H, m), 1.54-1.77(4H, m), 1.98-2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80(1H, m), 5.30-5.42(2H, m), 6.03(1H, d, J=7.2 Hz), 7.04-7.06(2H, m), 7.32-7.35(2H, m), 7.37(1H, d, J=3.6 Hz). IR(CHCl3): 3509, 3444, 3426, 3110, 2667, 1708, 1645, 1530, 1499, 1421 cm−1. [α]D26.5+69.5±1.1°(c=1.001, MeOH) Anal. (C23H27NO3S3.0.1H2O) Calcd.(%): C, 59.61; H, 5.92; N, 3.02; S, 20.76. Found(%): C, 59.66; H, 5.90; N, 3.15; S, 20.52.

[0448] Compound Number I-80

[0449] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.17-1.32(2H, m), 1.38-1.48(2H, m), 1.54-1.77(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m), 3.81(1H, m), 5.31-5.43(2H, m), 6.31(1H, d, J=7.2 Hz), 7.37-7.44(3H, m), 7.61(1H, d, J=3.9 Hz), 8.15(1H, dd, J=1.2 and 3.0 Hz). IR(CHCl3): 3517, 3441, 3371, 3114, 1708, 1655, 1530, 1504, 1331, 1152 cm−1. [α]D26.5+73.9±1.1°(c=1.001, MeOH) Anal. (C23H27NO5S3.0.3H2O) Calcd.(%): C, 55.35; H, 5.57; N, 2.81; S, 19.28 Found(%): C, 55.47; H, 5.50; N, 2.80; S, 19.09.

[0450] Compound Number I-81

[0451] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.16-1.30(2H, m), 1.38-1.48(2H, m), 1.54-1.77 (4H, m), 1.98-2.17(5H, m), 2.34(2H, t, J=7.2 Hz), 2.46(3H, d, J=0.9 Hz), 2.50(1H, m), 3.79(1H, m), 5.29-5.41(2H, m), 5.99(1H, d, J=7.2 Hz), 6.67(1H, m), 6.99, 7.10 and 7.32(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3517, 3445, 3426, 2668, 1708, 1644, 1530, 1499, 1420, cm−1. [α]D26.5+66.1±1.1°(c=1.002, MeOH) Anal. (C24H29NO3S3.0.1H2O) Calcd.(%): C, 60.37; H, 6.16; N, 2.93; S, 20.15. Found(%): C, 60.21; H, 6.10; N, 2.90; S, 20.45.

[0452] Compound Number I-82

[0453] 1 H-NMR(CDCl3) δ: 1.11(1H, m), 1.18-1.32(2H, m), 1.38-1.50(2H, m), 1.54-1.74. (4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(4H, d and m, J=0.6 Hz), 3.80(1H, m), 5.31-5.43(2H, m), 6.34(1H, d, J=6.6 Hz), 6.77 (1H, m), 7.41, 7.55 and 7.58(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3511, 3442, 3373, 3096, 1708, 1655, 1530, 1504, 1436, 1335, 1152 cm−1. [α]D26.5+73.0±1.1°(c=1.002, MeOH) Anal. (C24H29NO5S3.0.3H2O) Calcd.(%): C, 56.18; H, 5.81; N, 2.73; S, 18.75. Found(%): C, 56.26; H, 5.74; N, 2.65; S, 18.50.

[0454] Compound Number I-83

[0455] 1 H-NMR(CDCl3) δ: 1.17(1H, m), 1.24-1.36(2H, m), 1.37-1.82(6H, m), 2.01-2.23 (5H, m), 2.36(2H, t, J=7.2 Hz), 2.51(1H, m), 3.83(1H, m), 5.31-5.45 (2H, m, 7.17(1H, dd, J=3.9 and 5.4 Hz), 7.36(1H, d, J=7.8 Hz), 7.47 (1H, dd, J=1.5 and 3.9 Hz), 7.66(1H, dd, J=1.5 and 5.4 Hz). IR(CHCl3): 3514, 3404, 3121, 1709, 1657, 1544, 1488, 1425 cm−1. [α]D25+73.2±2.2°(c=0.518, MeOH) Anal. (C22H26N2O3S3.0.2H2O) Calcd.(%): C, 56.67; H, 5.71; N, 6.01; S, 20.63. Found(%): C, 56.55; H, 5.71; N, 6.03; S, 20.93.

[0456] Compound Number I-84

[0457] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.20-1.32(2H, m), 1.43-1.48(2H, m), 1.57-1.82(4H, m), 2.02(1H, d, J=3.3 Hz), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.55(1H, m), 3.86(1H, m), 4.01(2H, s), 5.29-5.43(2H, m), 6.17(1H, d, J=7.2 Hz), 7.15-7.31(7H, m), 7.67(2H, d, J=8.1 Hz). IR(CHCl3): 3517, 3447, 2669, 1708, 1651, 1523, 1495 cm−1. [α]D25+77.9±1.2°(c=1.016, MeOH) Anal. (C28H33NO3) Calcd.(%): C, 77.93; H, 7.71; N, 3.25. Found(%): C, 77.65; H, 7.93; N, 3.32.

[0458] Compound Number I-85

[0459] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.21-1.31(2H, m), 1.44-1.49(2H, m), 1.58-1.82(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.56(1H, m), 3.87(1H, m), 4.1.9(2H, s), 5.30-5.43(2H, m), 6.19(1H, d, J=7.2 Hz), 6.80(1H, m), 6.93(1H, dd, J=2.6 and 5.1 Hz), 7.16(1H, dd, J=1.5 and 5.1 Hz), 7.30 and 8.69(each 2H, each d, each J=8.1 Hz). IR(CHCl3): 3510, 3446, 2664, 1708, 1651, 1523, 1496 cm−1. [α]D25+73.2±1.1°(c=1.009, MeOH) Anal. (C26H31NO3S) Calcd.(%): C, 71.36; H, 7.14; N, 3.20; S, 7.33. Found(%): C, 71.48; H, 7.05; N, 3.29; S, 7.13.

[0460] Compound Number I-86

[0461] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.31(2H, m), 1.43-1.48(2H, m), 1.58-1.81(4H, m), 2.00-2.17(5H, m), 2.34(2H, t, J=7.2 Hz), 2.55(1H, m), 3.87(1H, m), 3.98(2H, s), 5.30-5.43(2H, m), 6.19(1H, d, J=7.2 Hz), 6.93-7.00(2H, m), 7.09-7.13(2H, m), 7.22 and 7.70(each 2H, each d, each J=8.4 Hz). IR(CHCl3): 3516, 3447, 2664, 1709, 1651, 1612, 1522, 1509, 1496, cm−1. [α]D25+71.6±1.1°(c=1.019, MeOH) Anal. (C28H32FNO3) Calcd.(%): C, 74.81; H, 7.17; N, 3.12; F. 4.23. Found(%): C, 74.66; H, 7.19; N, 3.13; F, 4.10.

[0462] Compound Number I-87

[0463] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.20-1.31(2H, m), 1.44-1.49(2H, m), 1.58-1.82(4H, m), 2.00-2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.56(1H, m), 3.87 (1H, m), 4.02(2H, s), 5.30-5.43(2H, m), 6.18(1H, d, J=7.2 Hz), 6.88(1H, dd, J=1.5 and 4.8 Hz), 6.92(1H, m), 7.25-7.28(3H, m), 7.68(2H, d, J=8.1 Hz). IR(CHCl3): 3516, 3446, 2668, 1709, 1651, 1612, 1523, 1496 cm−1. [α]D25+72.7±1.1°(c=1.014, MeOH) Anal. (C26H31NO3S.0.1H2O) Calcd.(%): C, 71.07; H, 7.16; N, 3.18; S, 7.30. Found(%): C, 70.90; H, 7.08; N, 3.21; S, 7.46.

[0464] Compound Number I-88

[0465] mp.103-105° C.; 1H-NMR(CDCl3) δ: 1.05(1H, m), 1.19-1.29(2H, m), 1.42-1.47(2H, m), 1.58-1.81(4H, m), 2.00-2.15(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.82(1H, m), 4.16(2H, s), 5.30-5.43(2H, m), 5.97(1H, d, J=7.5 Hz), 6.79(1H, dt, J=0.9 and 3.9 Hz), 6.96(1H, dd, J=1.5 and 4.8 Hz), 7.05 (1H, m), 7.28(1H, dd, J=3.0 and 4.8 Hz), 7.37(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3445, 3427, 2670, 1708, 1642, 1544, 1507 cm−1. [α]D25+67.3±1.1°(c=1.002, MeOH) Anal. (C24H29NO3S2.0.3H2O) Calcd.(%): C, 64.20; H, 6.64; N, 3.12; S, 14.28. Found(%): C, 64.29; H, 6.49; N, 3.10; S, 14.11.

[0466] Compound Number I-89

[0467] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.20-1.29(2H, m), 1.40-1.49(2H, m), 1.56-1.89(4H, m), 2.00-2.25(6H, m), 2.32-2.38(2H, m), 2.51(1H, m), 3.80 (1H, m), 5.04(2H, s), 5.27-5.41(2H, m), 5.90(1H, d, J=6.6 Hz), 6.38(1H, m), 6.63(1H, t, J=2.4 Hz), 7.14-7.17(2H, m), 7.29-7.35(4H, m). IR(CHCl3): 3510, 3448, 2663, 1736, 1709, 1636, 1555, 1497 cm−1. [α]D25+60.8±1.0°(c=1.003, MeOH) Anal. (C26H32N2O3.0.3H2O) Calcd.(%): C, 73.62; H, 7.70; N, 6.60. Found(%): C, 73.68; H, 7.62; N, 6.73.

[0468] Compound Number I-90

[0469] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.20-1.29(2H, m), 1.40-1.48(2H, m), 1.56-1.87(4H, m), 2.00-2.24(5H, m), 2.32-2.38(2H, m), 2.50(1H, m), 3.80 (1H, m), 5.19(2H, s), 5.27-5.41(2H, m), 5.90(1H, d, J=7.5 Hz), 6.37(1H, dd, J=2.1 and 3.0 Hz), 6.67(1H, t, J=2.4 Hz), 6.95-6.98(2H, m), 7.27(1H, dd, J=1.8 and 4.5 Hz), 7.31(1H, dd, J=1.8 and 2.1 Hz). IR(CHCl3): 3513, 3448, 2661, 1709, 1637, 1555, 1497 cm−1. [α]D25+59.4±1.0°(c=1.011, MeOH) Anal. (C24H30N2O3S.0.2H2O) Calcd.(%): C, 67.01; H, 7.12; N, 6.51; S, 7.45. Found(%): C, 67.07; H, 7.03; N, 6.62; S, 7.55.

[0470] Compound Number I-91

[0471] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.23-1.26(2H, m), 1.39-1.48(2H, m), 1.57-1.82(4H, m), 2.00-2.16(5H, m), 2.34(2H, t, J=7.2 Hz), 2.50(1H, m), 3.82(1H, m), 5.03(2H, s), 5.27-5.42(2H, m), 5.98(1H, brs), 6.40(1H, m), 6.91(1H, dd, J=1.2 and 4.8 Hz), 7.08(1H, brs), 7.28-7.31(2H, m). IR(CHCl3): 3516, 3448, 3108, 2663, 1736, 1709, 1636, 1555, 1497 cm−1. [α]D25+59.8±1.0°(C=1.008, MeOH) Anal. (C24H30N2O3S.0.2H2O) Calcd.(%): C, 67.01; H, 7.12; N, 6.51; S, 7.45. Found(%): C, 67.26; H, 7.06; N, 6.61; S, 7.55.

[0472] Compound Number I-92

[0473] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.18-1.28(2H, m), 1.38-1.43(2H, m), 1.54-1.78(4H, m), 1.96-2.23(5H, m), 2.36(2H, dt, J=1.8 and 6.9 Hz), 2.52 (1H, m) 3.77(1H, m), 5.30-5.45(2H, m), 6.07(1H, d, J=6.9 Hz), 6.58(1H, dd, J=1.5 and 3.3 Hz), 7.14(1H, dd, J=2.1 and 3.3 Hz), 7.51-7.57(2H, m), 7.65 (1H, m), 7.77(1H, t, J=2.1 Hz), 7.88-7.92(2H, m). IR(CHCl3): 3510, 3444, 3144, 1732, 1708, 1651, 1570, 1509, 1382, 1176 cm−1. [α]D24+55.9±0.9°(c=1.013, MeOH) Anal. (C25H30N2O5S.0.3H2O) Calcd.(%): C, 63.08; H, 6.48; N, 5.88; S, 6.74. Found(%): C, 63.24; H, 6.27; N, 6.03; S, 6.74.

[0474] Compound Number I-93

[0475] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.18-1.29(2H, m), 1.39-1.47(2H, m), 1.56-1.78 (4H, m), 1.98-2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81(1H, m), 4.33(2H, s), 5.29-5.42(2H, m), 6.03(1H, d, J=7.5 Hz), 6.84(1H, d, J=3.9 Hz), 6.90(1H, m), 6.95(1H, dd, J=3.6 and 5.1 Hz), 7.19(1H, dd, J=1.2 and 5.1 Hz), 7.38(1H, d, J=3.9 Hz). IR(CHCl3): 3510, 3554, 3427, 1708, 1643, 1544, 1507 m−1. [α]D27+70.1±1°(c=1.010, MeOH) Anal. (C24H29NO29NO3S2.0.1H2O) Calcd.(%): C, 64.72; H, 6.61; N, 3.14; S, 14.40. Found(%): C, 64.83; H, 6.60; N, 3.31; S, 14.46.

[0476] Compound Number I-94

[0477] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.20-1.27(2H, m), 1.40-1.44(2H, m), 1.56-1.78(4H, m), 2.00-2.19(5H, m), 2.36(2H, d, J=7.2 Hz), 2.51(1H, m), 3.78 (1H, m), 5.30-5.44(2H, m), 6.13(1H, d, J=6.9 Hz), 6.59(1H, dd, J=1.5 and 3.3 Hz), 7.10(1H, dd, J=3.6 and 5.1 Hz), 7.16(1H, dd, J=2.1 and 3.3 Hz), 7.69-7.76(3H, m). IR(CHCl3): 3510, 3444, 3143, 1708, 1651, 1571, 1508, 1387, 1179 cm−1. [α]D24+56.0±1.0°(c=1.005, MeOH) Anal. (C23H28N2O5S2.0.2H2O) Calcd.(%): C, 57.53; H, 5.96; N, 5.83; S, 13.35. Found(%): C, 57.54; H, 6.07; N, 5.93; S, 12.91.

[0478] Compound Number I-95

[0479] 1 H-NMR(CDCl3) δ: 1.16(1H, m), 1.26-1.37(2H, m), 1.40-1.81(6H, m), 2.04-2.25(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m), 3.87(1H, m), 5.32-5.46 (2H, m), 6.37(2H, t, J=2.1 Hz), 7.31(1H, d, J=7.5 Hz), 7.33(2H, t, J=2.1 Hz), 7.82(1H, m). IR(CHCl3): 3512, 3408, 3127, 1708, 1658, 1540, 1525, 1493, 1341 m−1. [α]D25+88.2±1.3°(c=1.003, MeOH) Anal. (C22H27N3O3S.0.1H2O) Calcd.(%): C, 63.62; H, 6.60; N, 10.12; S, 7.72. Found(%): C, 63.72; H, 6.45; N, 9.99; S, 7.75.

[0480] Compound Number I-96

[0481] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.18-1.30(2H, m), 1.39-1.48(2H, m), 1.57-1.78(4H, m), 2.01-2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.80(1H, m), 5.30-5.43(2H, m), 6.11(1H, m), 6.98(1H, dd, J=3.6 and 5.4 Hz), 7.24(1H, dd, J=1.2 and 3.6 Hz), 7.38(1H, dd, J=1.2 and 5.4 Hz), 7.43 (1H, d, J=1.5 Hz), 7.85(1H, d, J=1.5 Hz). IR(CHCl3): 3510, 3445, 3108, 1708, 1650, 1535, 1498 m−1. [α]D25+70.7±1.1°(c=1.004, MeOH) Anal. (C23H27NO3S3.0.3H2O) Calcd.(%): C, 59.15; H, 5.96; N, 3.00; S, 20.60. Found(%): C, 59.06; H, 5.66; N, 3.07; S, 20.87.

[0482] Compound Number I-97

[0483] 1 H-NMR(CDCl3) δ: 1.20-2.52(16H, m), 2.61(1H, m), 3.72(1H, m), 5.34-5.55 (2H, m), 6.66(1H, d, J=6.3 Hz), 71.2(1H, m), 7.71(1H, m), 7.75(1H, m), 8.29(1H, m), 8.37(1H, brs). IR(CHCl3): 3512, 3405, 3096, 1726, 1710, 1653, 1542, 1505, 1402, 1329, 1152 m−1. [α]D25+65.4±1.1°(c=1.005, MeOH) Anal. (C23H27NO5S3.0.2H2O) Calcd.(%): C, 55.55; H, 5.55; N, 2.82; S, 19.35. Found(%): C, 55.47; H, 5.54; N, 3.09; S, 19.21.

[0484] Compound Number I-98

[0485] mp.103-104° C.; 1H-NMR(CDCl3) δ: 1.09(1H, m), 1.23-1.31(2H, m), 1.45-1.50(2H, m), 1.60-1.80(4H, m), 2.00-2.23(5H, m), 2.37(2H, t, J=7.2 Hz), 2.55 (1H, m), 3.85(1H, m), 5.31-5.45(2H, m), 6.05(1H, d, J=7.5 Hz), 6.98 and 7.04(each 1H, each d, each J=16.2 Hz), 6.97(1H, d, J=3.9 Hz), 7.25-7.33 (3H, m), 7.41(1H, d, J=3.9 Hz). IR(CHCl3): 3511, 3445, 3428, 2665, 1708, 1641, 1538, 1519, 1499 cm−1. [α]D24+77.8±1.2°(c=1.007, MeOH) Anal. (C25H29NO3S2.0.25AcOEt) Calcd.(%): C, 65.38; H, 6.54; N, 2.93; S, 13.43. Found(%): C, 65.64; H, 6.62; N, 2.95; S, 13.26.

[0486] Compound Number I-99

[0487] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.20-1.30(2H, m), 1.41-1.46(2H, m), 1.59-1.80(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.80(1H, m), 5.30-5.43(2H, m), 5.94(1H, d, J=6.9 Hz), 6.57(2H, s), 6.94(1H, d, J=3.9 Hz), 7.03(1H, dd, J=1.5 and 4.5 Hz), 7.29(1H, s), 7.30(1H, m), 7.34 (1H, d, J=3.91 Hz). IR(CHCl3): 3511, 3445, 3427, 2670, 1708, 1642, 1536, 1518, 1500 cm−1. [α]D24+62.8±1.0°(c=1.003, MeOH) Anal. (C25H29NO3S2.0.2AcOEt) Calcd.(%): C, 65.48; H, 6.52; N, 2.96; S, 13.55. Found(%): C, 65.36; H, 6.47; N, 2.13; S, 13.58.

[0488] Compound Number I-100

[0489] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.17-1.32(2H, m), 1.38-1.50(2H, m), 1.56-1.80 (4H, m), 1.98-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.44(3H, d, J=0.9 Hz), 2.52(1H, m), 3.80(1H, m), 5.30-5.43(2H, m), 5.99(1H, d, J=7.5 Hz), 5.99(1H, d, J=7.5. Hz), 6.70(1H, m), 7.03(1H, d, J=3.9 Hz), 7.10(1H, d, J=1.5 Hz), 7.36(1H, d, J=3.9 Hz). IR(CHCl3): 3510, 3445, 3426, 2671, 1708, 1644, 1530, 1499, 1420, 1318 cm−1. [α]D25+69.1±1.1°(c=1.018, MeOH) Anal. (C24H29NO3S3) Calcd.(%): C, 60.60; H, 6.14; N, 2.94; S, 20.22. Found(%): C, 60.49; H, 6.26; N, 2.98; S, 20.25.

[0490] Compound Number I-101

[0491] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.18-1.32(2H, m), 1.38-1.50(2H, m), 1.54-1.77 (4H, m), 2.00-2.20(5H, m), 2.36(2H, t, J=7.2 Hz), 2.47(3H, d, J=0.9 Hz), 2.53(1H, m), 3.81(1H, m), 5.31-5.44(2H, m), 6.30(1H, d, J=7.2 Hz), 7.03(1H, m), 7.42 and 7.59(each 1H, each d, each J=3.9 Hz), 7.90(1H, d, J=1.5 Hz). IR(CHCl3): 3517, 3441, 3370, 3115, 2671, 1708. 1655, 1530, 1504, 1442, 1328, 1156, 1142 cm−1. [α]D24+71.6±1.1°(c=1.018, MeOH) Anal. (C24H29NO5S3.0.2H2O) Calcd.(%): C, 56.38; H, 5.80; N, 2.74; S, 18.81. Found(%): C, 56.28; H, 5.74; N, 2.79; S, 18.92.

[0492] Compound Number I-102

[0493] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.21-1.28(2H, m), 1.42-1.47(2H, m), 1.57-1.74(4H, m), 2.00-2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m), 3.82 (1H, m), 5.30-5.43(2H, m), 6.15(1H, d, J=7.5 Hz), 6.51 and 6.68(each 1H, each d, J=11.7 Hz), 6.98(1H, dd, J=3.6 and 5.1 Hz), 7.06(1H, dd, J=0.9 and 3.9 Hz), 7.13(1H, dt, J=0.9 and 3.6 Hz), 7.25(1H, dd, J=0.9 and 5.1 Hz), 7.41(1H, d, J=3.9 Hz). IR(CHCl3): 3510, 3445, 3427, 2665, 1708, 1643, 1535, 1501 cm−1. [α]D24+68.6±1.1°(c=1.006, MeOH) Anal. (C25H29NO3S2.0.2H2O) Calcd.(%): C, 65.45; H, 6.45; N, 3.05; S, 13.98. Found(%): C, 65.44; H, 6.37; N, 3.28; S, 13.82.

[0494] Compound Number I-103

[0495] mp.107-108° C.; 1H-NMR(CDCl3) δ: 1.09(1H, m), 1.26-1.32(2H, m), 1.45-1.50 (2H, m), 1.60-1.81(4H, m), 2.01-2.23(5H, m), 2.37(2H, t, J=7.2 Hz), 2.55 (1H, m, 3.84(1H, m), 5.31-5.45(2H, m), 6.03(1H, d, J=7.5 Hz), 6.97 and 7.14(each 1H, each d, J=15.9 Hz), 6.97(1H, d, J=3.9 Hz), 7.01(1H, dd, J=3.6 and 5.4 Hz), 7.08(1H, d, J=3.6 Hz), 7.23(1H, d, J=5.4 Hz), 7.40(1H, d, J=3.9 Hz). IR(CHCl3): 3517, 3445, 3428, 2670, 1708, 1641, 1536, 1518, 1500 cm−1. [α]D24+85.0±1.2°(c=1.009, MeOH) Anal. (C25H29NO3S2.0.15AcOEt) Calcd.(%): C, 65.58; H, 6.49; N, 2.99; S, 13.68. Found(%): C, 65.88; H, 6.74; N, 2.98; S, 13.35.

[0496] Compound Number I-104

[0497] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.30(2H, m), 1.42-1.50(2H, m), 1.57-1.79(4H, m), 2.01-2.24(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m), 3.82 (1H, m), 4.10(sH, s), 5.31-5.44(2H, m), 6.03(1H, d, J=7.2 Hz), 6.70(1H, d, J=3.6 Hz), 6.95(1H, dd, J=3.6 and 5.4 Hz), 7.03(1H, dd, J=1.5 and 3.6 Hz), 7.30(1H, d, J=3.6 Hz), 7.36(1H, dd, J=1.5 and 5.4 Hz). IR(CHCl3): 3518, 3445, 3427, 1708, 1644, 1542, 1507 cm−1. [α]D24.5+65.0±1.0°(c=1.008, MeOH) Anal. (C24H29NO3S3.0.4H2O) Calcd.(%): C, 59.69; H, 6.22; N, 2.90; S, 19.92. Found(%): C, 59.40; H, 5.98; N, 2.95; S, 20.06.

[0498] Compound Number I-105

[0499] 1 H-NMR(CDCl3) δ: 1.11(1H, m), 1.21-1.31(2H, m), 1.42-1.49(2H, m), 1.58-1.76(4H, m), 2.01-2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m), 3.81 (1H, m), 4.60(sH, s), 5.32-5.45(2H, m), 6.18(1H, d, J=7.2 Hz), 6.91(1H, d, J=3.9 Hz), 7.12(1H, dd, J=3.9 and 5.1 Hz), 7.40(1H, d, J=3.9 Hz), 7.52 (1H, dd, J=1.2 and 3.9 Hz), 7.72(1H, dd, J=1.2 and 5.1 Hz). IR(CHCl3): 3517, 3444, 3425, 3097, 1708, 1648, 1524, 1508, 1402, 1328, 1147 cm−1. [α]D24.5+61.5±1.0°(c=1.008, MeOH) Anal. (C24H29NO5S2.0.4H2O) Calcd.(%): C, 55.98; H, 5.83; N, 2.72; S, 18.68. Found(%): C, 55.77; H, 5.71; N, 2.84; S, 18.73.

[0500] Compound Number I-106

[0501] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.31(2H, m), 1.41-1.49(2H, m), 1.57-1.78(4H, m), 2.00-2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m), 3.81 (1H, m), 4.23(sH, s), 5.31-5.44(2H, m), 6.00(1H, d, J=7.2 Hz), 6.82(1H, m), 6.88(1H, dd, J=3.6 and 5.1 Hz), 6.92(1H, d, J=3.6 Hz), 7.21(1H, dd, J=1.2 and 5.1 Hz), 7.33(1H, d, J=3.6 Hz). IR(CHCl3): 3514, 3444, 3427, 2665, 1709, 1645, 1529, 1498, 1421, 1317 cm−1. [α]D24+67.1±1.1°(c=1.006, MeOH) Anal. (C24H29NO3S3.0.1H2O) Calcd.(%): C, 60.37; H, 6.16; N, 2.90; S, 20.15. Found(%): C, 60.46; H, 6.14; N, 2.96; S, 20.02.

[0502] Compound Number I-107

[0503] 1 H-NMR(CDCl3) δ: 1.09-1.32(3H, m), 1.38-1.48(2H, m), 1.53-1.79(4H, m), 1.96-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.54(4H, d and m, J=0.6 Hz), 3.79 (1H, m), 5.30-5.45(2H, m), 6.48 and 6.51(total 1H, each d, J=7.8 and 7.5 Hz), 7.12 (1H, dd, J=3.9 and 5.1 Hz), 7.42 and 7.43(total 1H, each d, each J=3.9 Hz), 7.52 and 7.53(total 1H, each d, each J=3.9 Hz), 7.58(1H, m), 7.69 (1H, dd, J=1.2 and 5.1 Hz). IR(CHCl3): 3509, 3443, 3425, 3092, 2666, 1708, 1650, 1532, 1503, 1403, 1322 cm−1. [α]D23+70.4±1.1°(c=1.007, MeOH) Anal. (C23H27NO4S3.0.4H2O) Calcd.(%): C, 56.97; H, 5.78; N, 2.89; S, 19.84. Found(%): C, 57.03; H, 5.67; N, 3.19; S, 19.73.

[0504] Compound Number I-108

[0505] 1 H-NMR(CDCl3) δ: 1.09-1.32(3H, m), 1.39-1.50(2H, m), 1.54-1.77(4H,m), 1.97-2.20(5H ,m), 2.35(2H, t, J=7.2 Hz), 2.52 and 2.53(total 3H, each s), 2.54(1H, m), 3.79(1H, m), 5.31-5.45(2H, m), 6.43 and 6.47(total 1H, each d, J=7.5 and 6.6 Hz), 6.76(1H, m), 7.39(1H, t-like), 7.40(1H, dd, J=2.1 and 3.6 Hz), 7.52(1H, dd, J=2.1 and 4.2 Hz). IR(CHCl3): 3510, 3443, 3425, 3092, 1708, 1650, 1531, 1503, 1437, 1237 cm−1. [α]D2368.6±1.1°(c=1.011, MeOH) Anal. (C24H29NO4S3.0.2H2O) Calcd.(%): C, 58.20; H, 5.98; N, 2.83; S, 19.42. Found(%): C, 58.18; H, 5.67; N, 2.90; S, 19.11.

[0506] Compound Number I-109

[0507] 1 H-NMR(CDCl3) δ: 1.13(1H, m), 1.21-1.34(2H, m), 1.45-1.52(2H, m), 1.59-1.78(4H, m), 2.03-2.23(5H, m), 2.37(2H, t, J=7.2 Hz), 2.58(1H, m), 3.86(1H, m), 5.32-5.46(2H, m), 6.28(1H, d, J=6.6 Hz), 7.20(1H, dd, J=3.9 and 5.1 Hz), 7.59(1H, d, J=3.9 Hz), 7.75(1H, dd, J=1.2 and 5.1 Hz), 7.81(1H, d, J=3.9 Hz), 7.92(1H, dd, J=1.2 and 3.9 Hz). IR(CHCl3): 3518, 3442, 3425, 3109, 1709, 1651, 1622, 1529, 1508, 1442, 1414, 1356, 1286, 1267 cm−1. [α]D23+89.2±1.3°(c=1.002, MeOH) Anal. (C24H27NO4S2.0.2H2O) Calcd.(%): C, 62.50; H, 5.99; N, 3.04; S, 13.90. Found(%): C, 62.63; H, 6.07; N, 2.97; S, 13.60.

[0508] Compound Number I-110

[0509] 1 H-NMR(CDCl3) δ: 1.12(1H, m), 1.22-1.33(2H, m), 1.44-1.52(2H, m), 1.59-1.79 (4H, m), 2.03-2.24(5H, m), 2.37(2H, t, J=7.2 Hz), 2.57(1H, m), 3.87(1H, m), 4.14(3H, s), 5.32-5.47(2H, m), 6.14(1H, d, J=7.5 Hz), 7.08(1H, dd, J=3.9 and 5.4 Hz), 7.27(1H, dd, J=1.2 and 3.9 Hz), 7.39(1H, dd, J=1.2 and 5.4 Hz), 7.41(1H, d, J=3.9 Hz), 7.49(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3444, 3425, 2665, 1709, 1649, 1529, 1498, 1049 cm−1. [α]D24+73.3±1.1°(c=1.003, MeOH) Anal. (C25H30N2O4S2.0.6H2O) Calcd.(%): C, 60.36; H, 6.32; N, 5.63; S, 12.89. Found(%): C, 60.30; H, 6.14; N, 5.84; S, 12.95.

[0510] Compound Number I-111

[0511] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.19-1.30(2H, m), 1.40-1.50(2H, m), 1.55-1.82(4H, m), 1.98-2.21(5H ,m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m), 3.83(1H, m), 5.30-5.44(2H, m), 5.96(1H, d, J=7.5 Hz), 6.43(1H, br), 6.52 (1H, d, J=3.9 Hz), 6.90(1H, m), 7.08-7.11(2H, m), 7.26-7.32(3H, m). IR(CHCl3): 3514, 3444, 3419, 1739, 1709, 1633, 1601, 1500, 1456 cm−1. [α]D22+86.6±1.3°(c=1.005, MeOH) Anal. (C25H30N2O3S.0.1H2O) Calcd.(%): C, 68.18; H, 6.91; N, 6.36; S, 7.28. Found(%): C, 68.11; H, 6.95; N, 6.43; S, 7.31.

[0512] Compound Number I-112

[0513] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.30(2H, m), 1.39-1.48(2H, m), 1.54-1.83(4H, m), 1.98-2.21(5H ,m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m), 3.38 (3H, s), 3.80(1H, m), 5.29-5.42(2H, m), 5.82(1H, d, J=6.0 Hz), 6.15(1H, d, J=4.2 Hz), 7.11-7.39(6H, m). IR(CHCl3): 3514, 3446, 3425, 1741, 1709, 1628, 1597, 1477, 1415 cm−1. [α]D22+83.2±1.2°(c=1.001, MeOH) Anal. (C26H32N2O3S) Calcd.(%): C, 69.00; H, 7.13; N, 6.19; S, 7.08. Found(%): C, 68.74; H, 7.08; N, 6.15; S, 7.01.

[0514] Compound Number I-113

[0515] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.18-1.31(2H, m), 1.40-1.49(2H, m), 1.55-1.75(4H, m), 1.99-2.16(5H, m), 2.31(3H, s), 2.35(2H, t, J=7.2 Hz), 2.52 (1H, m), 3.82(1H, m), 5.31-5.43(2H, m), 6.06(1H, d, J=7.5 Hz), 7.03-7.20 (5H, m), 7.44(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3444, 3425, 2671, 1709, 1647, 1529, 1498, 1421, 1317 cm−1. [α]D23+70.2±1.1°(c=1.001, MeOH) Anal. (C26H31NO3S2) Calcd.(%): C, 66.49; H, 6.65; N, 2.98; S, 13.65. Found(%): C, 66.34; H, 6.74; N, 2.94; S, 13.78.

[0516] Compound Number I-114

[0517] mp.114-116° C.; 1H-NMR(CDCl3) δ: 1.09(1H, m), 1.18-1.32(2H, m), 1.37-1.47 (2H, m), 1.55-1.75(4H, m), 2.00-2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.42 (3H, s), 2.52(1H, m), 3.80(1H, m), 5.30-5.43(2H, m), 6.23(1H, d, J=7.5 Hz), 7.41(3H, m), 7.59(1H, d, J=3.9 Hz), 7.78(2H, m). IR(CHCl3): 3514, 3442, 3371, 2669, 1707, 1655, 1529, 1504, 1329, 1151 cm−1. [α]D23+72.4±1.1°(c=1.004, MeOH) Anal. (C26H31NO5S2) Calcd.(%): C, 62.25; H, 6.23; N, 2.79; S, 12.78. Found(%): C, 61.83; H, 6.39; N, 2.73; S, 12.78.

[0518] Compound Number I-115

[0519] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.18-1.31(2H, m), 1.40-1.50(2H, m), 1.56-1.78(4H, m), 1.99-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m), 3.77(3H, s), 3.82(1H, m), 5.31-5.43(2H, m), 6.06(1H, d, J=7.2 Hz), 6.74-6.89(3H, m), 7.16-7.23(2H, m), 7.45(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3444, 3425, 2665, 1709, 1647, 1591, 1529, 1498, 1477, 1423 cm−1. [α]D23+68.7±1.1°(c=1.014, MeOH) Anal. (C26H31NO4S2) Calcd.(%): C, 64.30; H, 6.43; N, 2.88; S, 13.20. Found(%): C, 64.04; H, 6.56; N, 2.87; S, 13.43.

[0520] Compound Number I-116

[0521] mp.67-70° C.; 1H-NMR(CDCl3) δ: 1.09(1H, m), 1.17-1.32(2H, m), 1.39-1.47 (2H, m), 1.55-1.75(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52 (1H, m), 3.80(1H, m), 3.86(3H, s), 5.30-5.43(2H, m), 6.26(1H, d, J=7.2 Hz), 7.12 (1H, m), 7.40-7.47(2H, m), 7.55(1H, m), 7.59(1H, d, J=3.9 Hz). IR (CHCl3): 3514, 3442, 3373, 1707, 1655, 1599, 1529, 1504, 1481, 1327, 1151 cm−1. [α]D23+70.0±1.1°(c=1.008, MeOH) Anal. (C26H31NO6S2.0.7H2O) Calcd.(%): C, 58.89; H, 6.16; N, 2.64; S, 12.09. Found(%): C, 58.87; H, 6.15; N, 2.74; S, 12.10.

[0522] Compound Number I-117

[0523] 1 H-NMR(CDCl3) δ: 1.10-1.32(3H, m), 1.37-1.46(2H, m), 1.55-1.73(4H, m), 1.94-2.18(5H, m), 2.34(2H, t, J=7.2 Hz), 2.55(1H, m), 3.78(1H, m), 5.29-5.45(2H, m), 6.56(1H, d, J=6.6 Hz), 7.09(1H, m), 7.37(1H, t, J=8.1 Hz), 7.45 (1H, d, J=3.9 Hz), 7.47-7.53(2H, m), 7.55(1H, (d, J=3.9 Hz). IR(KBr): 3365, 3095, 1707, 1628, 1543, 1448, 1306, 1147 cm−1. [α]D23+70.8±1.1°(c=1.003, MeOH) Anal. (C25H29NO6S2.0.3H2O) Calcd.(%): C, 58.99; H, 5.86; N, 2.75; S, 12.60. Found(%): C, 58.85; H, 5.85; N, 2.67; S, 12.77.

[0524] Compound Number I-118

[0525] mp.133-134° C.; 1H-NMR(CDCl3) δ: 1.08(1H, m), 1.18-1.32(2H, m), 1.40-1.49 (2H, m), 1.55-1.78(4H, m), 1.96-2.24(5H, m), 2.34(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81(1H, m), 5.31-5.46(2H, m), 6.14(1H, d, J=6.6 Hz), 6.71 (2H, m), 6.86(1H, m), 7.14(2H, m), 7.42(1H, d, J=3.9 Hz). IR(Nujol): 3336, 3091, 2656, 1703, 1603, 1581, 1545 cm−1. [α]D23+73.2±1.1°(c=1.007, MeOH) Anal. (C25H29NO4S2) Calcd.(%): C, 63.67; H, 6.20; N, 2.97; S, 13.60. Found(%): C, 63.78; H, 6.17; N, 3.10; S, 13.73.

[0526] Compound Number I-119

[0527] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.17-1.30(2H, m), 1.38-1.48(2H, m), 1.54-1.80 (4H, m), 1.98-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.79 (3H, s), 3.81(1H, m), 4.10(2H, s), 5.29-5.42(2H, m), 5.97(1H, d, J=7.5 Hz), 6.77-6.84(4H, m), 7.23(2H, m), 7.37(1H, d, J=3.9 Hz). IR (CHCl3): 3514, 3446, 3427, 1741, 1709, 1641, 1543, 1506, 1456 cm−1. [α]D22+64.3±1.0°(c=1.005, MeOH) Anal. (C27H33NO4S.0.1H2O) Calcd.(%): C, 69.08; H, 7.13; N, 2.98; S, 6.83. Found(%): C, 69.03; H, 7.25; N, 3.06; S, 7.00.

[0528] Compound Number I-120

[0529] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.16-1.28(2H, m), 1.36-1.46(2H, m), 1.52-1.78 (4H, m), 1.96-2.17(5H, m), 2.32(2H, t, J=7.2 Hz), 2.50(1H, m), 3.80(1H, m), 4.02(2H, s), 5.28-5.42(2H, m), 6.16(1H, d, J=7.5 Hz), 6.72-6.77(4H, m), 1H, m), 7.36(1H, d, J=3.9 Hz). IR(CHCl3): 3595, 3423, 3207, 1707, 1635, 1599, 1545, 1508, 1456 cm−1. [α]D23+66.8±1.1°(c=1.009, MeOH) Anal. (C26H31NO4S.0.4H2O) Calcd.(%): C, 67.77; H, 6.96; N, 3.04; S, 6.96. Found(%): C, 67.83; H, 6.92; N, 3.18; S, 7.14.

[0530] Compound Number I-121

[0531] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.8-1.31(2H, m), 1.40-1.48(2H, m), 1.55-1.82(4H, m), 1.98-2.22(5H, m), 2.29(3H, s), 2.35(2H, t, J=7.2 Hz), 2.52 (1H, m), 3.80(1H, m), 4.14(2H, s), 5.29-5.43(2H, m), 5.97(1H, d, J=7.5 Hz), 6.78 (1H, m), 6.94-7.00(2H, m), 7.10(1H, m), 7.33(1H, m), 7.36(1H, d, J=3.9 Hz). IR(CHCl3): 3514, 3446, 3427, 2669, 1763, 1745, 1709, 1643, 1545, 1506, 1371 cm−1. [α]D23+61.3±1.0°(c=1.019, MeOH) Anal. (C28H33NO5S.0.1H2O) Calcd.(%): C, 67.61; H, 6.73; N, 2.82; S, 6.45. Found(%): C, 67.52; H, 6.77; N, 2.99; S, 6.48.

[0532] Compound Number I-122

[0533] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.18-1.30(2H, m), 1.40-1.48(2H, m), 1.56-1.76(4H, m), 1.99-2.17(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81(1H, m), 4.25(2H, s), 5.30-5.43(2H, m), 6.00(1H, d, J=7.5 Hz), 6.81(1H, d, J=3.9 Hz), 7.20-7.36(6H, m). IR(CHCl3): 3516, 3446, 3427, 2667, 1709, 1643, 1543, 1506 cm1. [α]D23+65.0±1.0°(c=1.008, MeOH) Anal. (C26H31NO3S2.0.1H2O) Calcd.(%): C, 66.24; H, 6.67; N, 2.97; S, 13.60. Found(%): C, 66.14; H, 6.63; N, 3.05; S, 13.49.

[0534] Compound Number I-123

[0535] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.20-1.32(2H, m), 1.40-1.50 (2H, m), 1.56-1.80 (4H, m), 2.00-2.20(5H, m), 2.36(2H, t, J=7.2 Hz), 2.54 (1H, m), 3.84 (1H, m), 5.20(2H, s), 5.31-5.44(2H, m), 6.06(1H, d, J=7.5 Hz), 6.94-7.05 (4H, m), 7.27-7.33(2H, m), 7.42(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3444, 3427, 2669, 1709, 1645, 1599, 1545, 1508, 1497 cm−1. [α]D24+65.4±1.1°(c=1.003, MeOH) Anal. (C26H31NO4S.0.2H2O) Calcd.(%): C, 68.30; H, 6.92; N, 3.06; S, 7.01. Found(%): C, 68.32; H, 6.83; N, 3.08; S, 6.99.

[0536] Compound Number I-124

[0537] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.18-1.32(2Hl, m), 1.40-1.50(2H, m), 1.55-1.80(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81(1H, m), 4.51(2H, d, J=0.9 Hz), 5.30-5.43(2H, m), 6.01(1H, d, J=7.5 Hz), 6.65-6.97(3H, m), 6.96(1H, d, J=3.9 Hz), 7.16-7.21(1H, m), 7.41(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3444, 3427, 1709, 1643, 1603, 1545, 1504, 1309, 1260 cm−1. [α]D22+65.7±1.0°(c=1.014, MeOH) Anal. (C26H32N2O3S.0.2H2O) Calcd.(%): C, 68.45; H, 7.16; N, 6.14; S, 7.03. Found(%): C, 68.43; H, 7.18; N, 6.27; S, 6.94.

[0538] Compound Number I-125

[0539] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.27(2H, m), 1.40-1.45(2H, m), 1.56-1.77(4H, m), 2.00-2.13(5H, m), 2.28(3H, s), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 3.80(1H, m), 4.12(2H, s), 5.29-5.41(2H, m), 5.98(1H, d, J=7.2 Hz), 6.69(1H, d, J=3.6 Hz), 7.18(4H, s), 7.36(1H, d, J=3.6 Hz). IR (CHCl3): 3518, 3446, 3426, 1741, 1709, 1641, 1543, 1506, 1458 cm−1. [α]D22.5+66.8±1.1°(c=1.003, MeOH) Anal. (C27H33NO3S.H2O) Calcd.(%): C, 69.05; H, 7.51; N, 2.98; S, 6.83. Found(%): C, 69.07; H, 7.11; N, 3.23; S, 7.04.

[0540] Compound Number I-126

[0541] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.17-1.28(2H, m), 1.41-1.46(2H, m), 1.55-1.77(4H, m), 2.00-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80(1H, m), 4.12(2H, s), 5.29-5.41(2H, m), 5.91(1H, d, J=7.2 Hz), 6.77(1H, d, J=3.3 Hz), 6.86-6.90(2H, m), 7.15(1H, dd, J=1.8 and 7.5 Hz), 7.20-7.26 (1H, m), 7.34(1H, d, J=3.6 Hz). IR(CHCl3): 3519, 3446, 3427, 2669, 1741, 1709, 1641, 1543, 1504, 1458, 1248 cm−1. [α]D22.5+64.2±1.0°(c=1.005, MeOH) Anal. (C27H33NO4S.0.1H2O) Calcd.(%): C, 69.08; H, 7.13; N, 2.98; S, 6.83. Found(%): C, 68.97; H, 6.90; N, 3.09; S, 6.77.

[0542] Compound Number I-127

[0543] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18 (3H, t, J=7.7 Hz), 1.15-1.29 (2H, m), 1.41-1.46 (2H, m), 1.56-1.80 (4H, m), 2.00-2.15 (5H, m), 2.35 (2H, t, J=7.2 Hz), 2.51 (1H, s), 2.64 (2H, q, J=7.7 Hz), 3.80 (1H, m), 4.16 (2H, s), 5.29-5.41 (2H, m), 5.91 (1H, d, J=7.5 Hz), 6.69 (1H, d, J=3.6 Hz), 7.16-7.25 (4H, m), 7.35 (1H, d, J=3.6 Hz). IR (CHCl3): 3516, 3447, 3427, 2669, 1709, 1641, 1543, 1506, 1456 cm−1. [α]D21+65.8±1.1°(c=1.011, MeOH). Anal. (C28H35NO3S.0.2H2O) Calcd.(%): C, 71.67; H, 7.60; N, 2.98; S, 6.83. Found(%): C, 71.83; H, 7.49; N, 3.12; S, 6.89.

[0544] Compound Number I-128

[0545] 1 H-NMR(CDCl3) δ: 1.04 (1H, m), 1.18-1.29 (2H, m), 1.41-1.46 (2H, m), 1.56-1.80 (4H, m), 2.00-2.20 (5H, m), 2.24 and 2.31 (each 3H, each s), 2.35 (2H, t, J=7.4 Hz), 2.51 (1H, s), 3.80 (1H, m), 4.19 (2H, s), 5.29-5.41 (2H, m), 5.91 (1H, d, J=7.2 Hz), 6.70 (1H, d, J=3.6 Hz), 6.99 (1H, d, J=7.5 Hz), 7.00 (1H, s), 7.07 (1H, d, J=7.5 Hz), 7.35 (1H, d, J=3.6 Hz). IR (CHCl3): 3514, 3446, 3426, 1741, 1709, 1641, 1543, 1506, 1456 cm−1. [α]D21+65.2±1.0°(c=1.014, MeOH) Anal. (C28H35NO3S.0.2H2O) Calcd.(%): C, 71.67; H, 7.60; N, 2.98; S, 6.83. Found(%): C, 71.53; H, 7.49; N, 3.31; S, 6.90.

[0546] Compound Number I-129

[0547] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.29(2H, m), 1.42-1.47(2H, m), 1.56-1.78(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.5 Hz), 2.43(3H, s), 2.52 (1H, s),3.81(1H, m), 4.24(2H, s), 5.30-5.42(2H, m), 5.97(1H, d, J=7.5 Hz), 6.57(1H, m), 6.67(1H, d, J=3.3 Hz), 6.83(1H, d, J=3.9 Hz), 7.37 (1H, d, J=3.9 Hz). IR(CHCl3): 3514, 3446, 3427, 1709, 1643, 1545, 1506, 1456 cm−1. [α]D22+67.1±1.1°(c=1.002, MeOH) Anal. (C25H31NO3S2) Calcd.(%): C, 65.61; H, 6.83; N, 3.06; S, 14.01. Found(%): C, 65.42; H, 6.76; N, 3.20; S, 13.73.

[0548] Compound Number I-130

[0549] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.28(2H, m), 1.41-1.45(2H, m), 1.55-1.78 (4H, m), 1.99-2.16(5H, m), 2.34(2H, t, J=7.2 Hz), 2.38(3H, s), 2.51 (1H, m), 3.80(1H, m), 4.09(2H, s), 5.29-5.41(2H, m), 5.96(1H, d, J=6.9 Hz), 6.76(1H, d, J=3.6 Hz), 7.12(4H, s), 7.37(1H, d, J=3.6 Hz). IR (CHCl3): 3510, 3446, 3427, 1741, 1709, 1641, 1543, 1508, 1458 cm−1. [α]D22+67.0±1.1°(c=1.014, MeOH) Anal. (C27H33NO3S) Calcd.(%): C, 71.81; H, 7.36; N, 3.10; S, 7.10. Found(%): C, 71.53; H, 7.24; N, 3.21; S, 7.36.

[0550] Compound Number I-131

[0551] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.28(2H, m), 1.41-1.46(2H, m), 1.56-1.78(4H, m), 1.99-2.19(5H, m), 2.33(3H, s), 2.34(2H, t, J=7.5 Hz), 2.51 (1H, m), 3.81(1H, m), 4.09(2H, s), 5.29-5.42(2H, m), 5.96(1H, d, J=7.2 Hz), 6.77 (1H, d, J=3.6 Hz), 7.02-7.07(3H, m), 7.21(1H, m), 7.37(1H, d, J=3.6 Hz). IR (CHCl3): 3516, 3446, 3427, 1741, 1709, 1641, 1543, 1506, 1458 cm−1. [α]D23+66.1±1.1°(c=1.006, MeOH) Anal. (C27H33NO3S.0.2H2O) Calcd.(%): C, 71.24; H, 7.40; N, 3.08; S, 7.04. Found(%): C, 71.26; H, 7.20; N, 3.19; S, 7.12.

[0552] Compound Number I-132

[0553] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.19-1.30(2H, m), 1.41-1.49(2H, m), 1.57-1.78(4H, m), 2.00-2.21(5H, m), 2.30(3H, s), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81(1H, m), 4.25(2H, s), 5.30-5.43(2H, m), 6.01(1H, d, J=6.9 Hz), 6.82(1H, d, J=3.9 Hz), 7.02(1H, m), 7.10-7.19(3H, m), 7.31(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3446, 3427, 2671, 1739, 1709, 1643, 1543, 1506, 1475, 1456 cm−1. [α]D23+63.2±1.0°(c=1.007, MeOH) Anal. (C27H33NO3S2.0.2H2O) Calcd.(%): C, 66,55; H, 6.91; N, 2.87; S, 13.16. Found(%): C, 66.44; H, 6.87; N, 2.99; S, 13.11.

[0554] Compound Number I-133

[0555] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.20-1.30(2H, m), 1.45-1.51(2H, m), 1.56-1.82(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.82 (1H, m), 4.16(2H, s), 5.30-5.43(2H, m), 5.98(1H, d, J=7.2 Hz), 6.13 (1H, dd, J=3.3 and 0.9 Hz), 6.32(1H, dd, J=3.3 and 1.8 Hz), 6.84(1H, d, J=3.6 Hz), 7.35(1H, dd, J=1.8 and 0.9 Hz), 7.37(1H, d, J=3.6 Hz). IR (CHCl3): 3512, 3446, 3427, 2669, 1709, 1.643, 1545, 1506 cm−1. [α]D22+69.6±1.1°(c=1.015, MeOH) Anal. (C24H29NO4S.0.2H2O) Calcd.(%): C, 66.86; H, 6.87; N, 3.25; S, 7.44. Found(%): C, 66.75; H, 6.63; N, 3.32; S, 7.50.

[0556] Compound Number I-134

[0557] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.29(2H, m), 1.45-1.60(2H, m), 1.61-1.80(4H, m), 2.00-2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81(1H, m), 3.96(2H, s), 5.29-5.42(2H, m), 5.96(1H, d, J=6.9 Hz), 6.30 (1H, m), 6.80(1H, m), 7.32(1H, m), 7.35-7.39(2H, m). IR(CHCl3): 3516, 3446, 3427, 2663, 1709, 1643, 1545, 1506 cm−1. [α]D21+70.2±1.1°(c=1.007, MeOH) Anal. (C24H29NO4S) Calcd.(%): C, 67.42; H, 6.84; N, 3.28; S, 7.50. Found(%): C, 67.13; H, 6.57; N, 3.40; S, 7.40.

[0558] Compound Number I-135

[0559] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.20-1.29(2H, m), 1.42-1.47(2H, m), 1.58-1.82(4H, m), 2.00-2.15(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81 (1H, m), 4.41(2H, s), 5.29-5.41(2H, m), 5.96(1H, d, J=7.2 Hz), 6.91 (1H, d, J=3.6 Hz), 7.11(1H, s), 7.25-7.35(3H, m), 7.39(1H, d, J=3.6 Hz), 7.76 (1H, d, J=7.8 Hz). IR(CHCl3): 3510, 3444, 3427, 2667, 1709, 1643, 1543, 1508 cm−1. [α]D24+66.5±1.1°(c=1.012, MeOH) Anal. (C28H31NO3S2.0.5H2O) Calcd.(%): C, 66.90; H, 6.42; N, 2.79; S, 12.76. Found(%): C, 66.99; H, 6.12; N, 2.81; S, 12.48.

[0560] Compound Number I-136

[0561] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.20-1.42(2H, m), 1.44-1.49(2H, m), 1.55-1.80(4H, m), 2.00-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81 (1H, m), 4.30(2H, s), 5.29-5.41(2H, m), 5.98(1H, d, J=7.8 Hz), 6.51 (1H, d, J=0.6 Hz), 6.92(1H, d, J=3.9 Hz), 7.17-7.25(2H, m), 7.38-7.51 (3H, m). IR (CHCl3): 3514, 3444, 3427, 2669, 1709, 1643, 1545, 1508, 1454 cm−1. [α]D23+63.8±1.0°(c=1.004, MeOH) Anal. (C28H31NO4S.0.3H2O) Calcd.(%): C, 69.62; H, 6.59; N, 2.90; S, 6.64. Found(%): C, 69.51; H, 6.52; N, 2.92; S, 6.63.

[0562] Compound Number I-137

[0563] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.29(2H, m), 1.40-1.48(2H, m), 1.55-1.78(4H, m), 1.98-2.18(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.81(1H, m), 4.17(2H, s), 5.29-5.42(2H, m), 5.98(1H, d, J=7.5 Hz), 6.81 (1H, d, J=3.6 Hz), 7.29-7.46(6H, m), 7.52-7.60(41H, m). IR(CHCl3): 3510, 3446, 3427, 1741, 1709, 1643, 1543, 1506, 1489 cm−1. [α]D23+59.4±1.0°(c=1.007, MeOH) Anal. (C32H35NO3S.0.2H2O) Calcd.(%): C, 74.30; H, 6.90; N, 2.71; S, 6.20. Found(%): C, 74.24; H, 6.78; N, 2.97; S, 6.16.

[0564] Compound Number I-138

[0565] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.17-1.29(2H, m), 1.39-1.47(2H, m), 1.54-1.76(4H, m), 1.97-2.38(5H, m), 2.33(2H, t, J=7.5 Hz), 2.51(1H, m), 3.80 (1H, m), 4.19(2H, s), 5.28-5.41(2H, m), 5.98(1H, d, J=7.5 Hz), 6.79 (1H, d, J=3.6 Hz), 7.21(1H, d, J=7.8 Hz), 7.31-7.49(7H, m), 7.56(2H, m). IR (CHCl3): 3512, 3446, 3427, 2669, 1741, 1709, 1643, 1543, 1506, 1479, 1456 cm−1. [α]D24+59.2±1.0°(c=1.006 MeOH) Anal. (C32H35NO3S.0.2H2) Calcd.(%): C, 74.30; H, 6.90; N, 2.71; S, 6.20. Found(%): C, 74.26; H, 6.92; N, 3.00; S, 6.20.

[0566] Compound Number I-139

[0567] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.17-1.32(2H, m), 1.43-1.48(2H, m), 1.58-1.80(4H, m), 2.02-2.24(5H, m), 2.34(2H, t, J=7.2 Hz), 2.58(1H, s), 3.91(1H, m),4.11(2H, s), 5.30-5.44(2H, m), 6.11(1H, d, J=7.2 Hz), 7.18-7.30(6H, m), 7.75(1H, d, J=8.4 Hz), 7.86(1H, s), 8.16(1H, s). IR(CHCl3): 3516, 3430, 2665, 1741, 1709, 1651, 1513, 1494, 1454, 1435 cm−1. [α]D24+45.6±0.9°(c=1.004, MeOH) Anal. (CO30H33NO3S.0.1H2O) Calcd.(%): C, 73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.57; H, 6.71; N, 3.07; S, 6.30.

[0568] Compound Number I-140

[0569] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.20-1.32(2H, m), 1.46-1.51(2H, m), 1.58-1.78(4H, m), 2.02-2.24(5H, m), 2.35(2H, t, J=7.41 Hz), 2.60(1H, s), 3.92(1H, m),4.10(2H, s), 5.32-5.46(2H, m), 6.14(1H, d, J=7.2 Hz), 7.19-7.32(6H, m), 7.64(1H, s), 7.81(1H, s), 8.20(1H, d, J=8.4 Hz). IR(CHCl3): 3516, 3438, 2669, 1709, 1651, 1516, 1494, 1406 cm−1. [α]D24+53.0±0.9°(c=1.002, MeOH) Anal. (C30H33NO3S) Calcd.(%): C, 73.89; H, 6.82; N, 2.87; S, 6.58. Found(%): C, 73.57; H, 7.05; N, 3.08; S, 6.63.

[0570] Compound Number I-141

[0571] mp.54-56° C.; 1-NMR(CDCl3) δ: 0.97(1H, m), 1.10-1.43(4H, m), 1.53-1.72 (4H, m), 1.97-2.15(5H, m), 2.31(2H, t, J=7.4 Hz), 2.45(1H, s), 3.83(1H, m), 4.39 and 4.52(each 1H, each d, J=16.5 Hz), 5.25-5.40(2H, m), 5.98 (1H, d, J=7.5 Hz), 7.00-7.31(7H, m), 7.57(1H, s), 7.73(1H, d, J=7.5 Hz). IR (CHCl3): 3514, 3433, 2671, 1709, 1655, 1512, 1454 cm−1. [α]D25+76.7±1.2°(c=1.005, MeOH) Anal. (C30H33NO3S.0.1H2O) Calcd.(%): C, 73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.45; H, 6.91; N, 3.21; S, 6.34.

[0572] Compound Number I-142

[0573] mp.118-119° C.; 1H-NMR(CDCl3) δ: 1.07(1H, m), 1.20-1.27(2H, m), 1.42-1.46(2H, m), 1.55-1.73(4H, m), 1.99-2.12(5H, m), 2.33(2H, t, J=7.5 Hz), 2.52(1H, s), 3.82(1H, m),3.93(2H, s), 5.29-5.42(2H, m), 6.10 (1H, d, J=7.2 Hz), 7.05(1H, d, J=0.9 Hz), 7.16-7.32(6H, m). IR(CHCl3): 3516, 3444, 3429, 2669, 1739, 1709, 1665, 1549, 1508, 1454 cm−1. [α]D24+72.7±0.1.1°(c=1.001, MeOH) Anal. (C26H31NO3S) Calcd.(%): C, 71.36; H, 7.14; N, 3.20; S, 7.33. Found(%): C, 71.31; H, 7.27; N, 3.36; S, 7.31.

[0574] Compound Number I-143

[0575] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.19-1.32(2H, m), 1.46-1.51(2H, m), 1.58-1.78(4H, m), 2.02-2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.60(1H, s), 3.92(1H, m),4.24(2H, s), 5.32-5.47(2H, m), 6.14(1H, d, J=7.5 Hz), 7.18-7.30(6H, m), 7.43(1H, t, J=7.8 Hz), 7.83(1H, s), 8.17(1H, d, J=7.8 Hz). IR(CHCl3): 3516, 3438, 2671, 1709, 1651, 1518, 1495, 1454 cm−1. [α]D25+62.8±1.0°(c=1.011, MeOH) Anal. (C30H33NO3S.0.1H2O) Calcd.(%): C, 73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.52; H, 6.87; N, 3.13; S, 6.47.

[0576] Compound Number I-144

[0577] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.23-1.29(2H, m), 1.41-1.49(2H, m), 1.58-1.77(4H, m), 2.00-2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81 (1H, m), 4.05(2H, s), 5.12(2H, s), 5.29-5.42(2H, m), 5.94(1H, d, J=7.8 Hz), 6.76(1H, d, J=3.9 Hz), 6.90-6.98(31H, m), 7.32-7.45 (6H, m). IR (CHCl3): 3516, 3446, 3427, 1741, 1709, 1643, 1543, 1510, 1456, 1273 cm−1. [α]D23+53.7±0.9°(c=1.006, MeOH) Anal. (C33H36FNO4S.0.2H2O) Calcd.(%): C, 70.11; H, 6.49; N, 2.48; S, 5.67; F,3.36. Found(%): C, 70.00; H, 6.44; N, 2.50; S, 5.75; F,3.32.

[0578] Compound Number I-145

[0579] mp.136-137° C.; 1H-NMR(CDCl3) δ: 1.06(1H, m), 1.23-1.29(2H, m), 1.41-1.49(2H, m), 1.58-1.77(4H, m), 2.00-2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.78(1H, m), 4.05(2H, s), 5.29-5.42(2H, m), 5.93 (1H, d, J=10.8 Hz), 6.77(1H, d, J=3.6 Hz), 6.88-6.98(3H, m), 7.36 (1H, d, J=3.6 Hz). IR (Nujol): 3377, 3101, 2752, 1703, 1618, 1601, 1550, 1518 cm−1. [α]D23+64.2±1.0°(c=1.009, MeOH) Anal. (C26H30FNO4S) Calcd.(%): C, 66.23; H, 6.41; N, 2.97; S, 6.80; F, 4.03. Found(%): C, 66.15; H, 6.38; N, 2.94; S, 6.76; F, 3.94.

[0580] Compound Number I-146

[0581] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.20-1.29(2H, m), 1.41-1.46(2H, m), 1.61-1.81(4H, m), 2.00-2.16(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m), 3.79 (1H, m), 4.03(2H, s), 5.08(2H, s), 5.29-5.40(2H, m), 5.63(1H, brs), 5.93 (1H, d, J=7.5 Hz), 6.70(1H, dd, J=2.1 and 8.4 Hz), 6.77 (1H, d, J=3.9 Hz), 6.83 (1H, d, J=5.7 Hz). 6.86(1H, d, J=8.4 Hz), 7.36-7.41(6H, m). IR(CHCl3): 3539, 3446, 3425, 1741, 1709, 1641, 1543, 1508, 1475, 1273 cm−1. [α]D23+53.8±0.9°(c=1.003, MeOH) Anal. (C33H37NO5S.0.5H2O) Calcd.(%): C, 69.69; H, 6.73; N, 2.46; S, 5.64. Found(%): C, 69.68; H, 6.85; N, 2.68; S, 5.76.

[0582] Compound Number I-147

[0583] mp.150-151° C.; 1H-NMR(CDCl3) δ: 1.06(1H, m), 1.20-1.29(2H, m), 1.41-1.46(2H, m), 1.58-1.79(4H, m), 2.00-2.16(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m), 3.79(1H, m), 3.86(3H, s), 4.06(2H, s), 5.29-5.41 (2H, m), 5.56 (1H, brs), 5.93(1H, d, J=8.4 Hz), 6.72-6.77(3H, m), 6.87 (1H, d, J=8.1 Hz), 7.37(1H, d, J=3.6 Hz). IR(Nujol): 3452, 3361, 3130, 1.743, 1707, 1620, 1599, 1550, 1522, 1286 cm−1. [α]D23+62.6±1.0°(c=1.002, MeOH) Anal. (C27H33NO5S) Calcd.(%): C, 67.05; H, 6.88; N, 2.90; S, 6.63. Found(%): C, 67.20; H, 7.04; N, 2.98; S, 6.58.

[0584] Compound Number I-148

[0585] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.31(2H, m), 1.41-1.50(2H, m), 1.56-1.81 (4H, m), 1.99-2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m), 2.95-3.00 (2H, m), 3.10-3.15(2H, m),3.83(1H, m), 5.31-5.44(2H, m), 6.02 (1H, d, J=7.2 Hz), 6.70(1H, d, J=3.9 Hz), 7.15-7.32(5H, m), 7.33(1H, d, J=3.9 Hz). IR(CHCl3): 3510, 3446, 3429, 2671, 1741, 1709, 1641, 1543, 1506, 1456 cm−1. [α]D23+68.4±1.1°(c=1.004, MeOH) Anal. (C27H33NO3S.0.1H2O) Calcd.(%): C, 71.52; H, 7.38; N, 3.09; S, 7.07. Found(%): C, 71.35; H, 7.37; N, 3.19; S, 7.19.

[0586] Compound Number I-149

[0587] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.32(2H, m), 1.41-1.50(2H, m), 1.56-1.81 (4H, m), 1.99-2.23(5H, m), 2.36(2H, t, J=7.2 Hz), 2.43(3H, s), 2.53 (1H, m), 3.05-3.19(4H, m), 3.83(1H, m), 5.31-5.44(2H, m), 6.00(1H, d, J=6.9 Hz), 6.23-6.56(2H, m), 6.75 and 7.34(each 1H, each d, each J=3.6 Hz). IR (CHCl3): 3510, 3446, 3429, 2669, 1709, 1641, 1543, 1506, 1458 cm−1. [α]D23+64.6±1.0°(c=1.014, MeOH) Anal. (C26H33NO3S2.0.1H2O) Calcd.(%): C, 65.96; H, 7.07; N, 2.96; S, 13.54. Found(%): C, 65.87; H, 7.03; N, 3.02; S, 13.50.

[0588] Compound Number I-150

[0589] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.31(2H, m), 1.41-1.50(2H, m), 1.56-1.80(4H, m), 1.99-2.20(5H, m), 2.35(2H, t, J=7.5 Hz), 2.53(1H, m), 3.18(3H, s), 3.83(1H, m), 5.31-5.44(2H, m), 6.05(1H, d, J=7.2 Hz), 6.74 (1H, d, J=3.6 Hz), 6.79(1H, m), 6.91(1H, dd, J=3.6 and 5.4 Hz), 7.13(1H, dd, J=1.2 and 5.4 Hz), 7.34(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 34446, 3429, 2669, 1709, 1641, 1543, 1506 cm−1. [α]D2430 66.1±1.0°(c=1.019, MeOH) Anal. (C25H31NO3S2) Calcd.(%): C, 65.61; HL, 6.83; N, 3.06; S,14.01. Found(%): C, 65.47; H, 6.89; N, 3.12; S, 13.82.

[0590] Compound Number I-151

[0591] 1 H-NMR(CDCl3) δ: 1.09(1H, m), 1.20-1.32(2H, m), 1.42-1.51(2H, m), 1.57-1.81(4H, m), 2.00-2.22(5H, m), 2.33(2H, t, J=7.5 Hz), 2.56(1H, m), 2.99-3.05(2H, m), 3.11-3.17(2H, m), 3.88(1H, m), 5.30-5.44(2H, m), 6.22 (1H, d, J=7.2 Hz), 6.74(1H, m), 6.89(1H, dd, J=3.3 and 5.1 Hz), 7.11(1H, dd, J=1.2 and 5.1 Hz), 7.23 and 7.67(each 2H, each d, each J=8.1 Hz). IR (CHCl3): 3516, 3448, 2665, 1709, 1651, 1523, 1496 cm−1. [α]D24+71.8±1.1°(c=1.009, MeOH) Anal. (C27H33NO3S) Calcd.(%): C, 71.81; H, 7.37; N, 3.10; S, 7.10. Found(%): C, 71.68; H, 7.40; N, 3.18; S, 6.96.

[0592] Compound Number I-152

[0593] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.31(2H, m), 1.42-1.50(2H, m), 1.56-1.81(4H, m), 2.00-2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m), 2.92-2.97(2H, m), 3.07-3.12(2H, m), 3.83(1H, m), 5.31-5.44(2H, m), 5.99 (1H, d, J=7.2 Hz), 6.68(1H, d, J=3.6 Hz), 6.92-7.00(2H, m), 7.08-7.15(2H, m), 7.32(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3446, 3429, 1741, 1709, 1641, 1543, 1510, 1458 cm−1. [α]D23+64.1±1.0°(c=1.012, MeOH) Anal. (C27H32FNO3S) Calcd.(%): C, 69.06; H, 6.87; N, 2.98; S, 6.83; F, 4.05. Found(%): C, 68.92; H, 6.90; N, 3.03; S, 6.81; F, 4.02.

[0594] Compound Number I-153

[0595] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.19-1.29(2H, m), 1.41-1.46(2H, m), 1.56-1.78(4H, m), 2.00-2.19(5H, m), 2.29(6H, s), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 3.81(1H, m), 4.05(2H, s), 5.29-5.42(2H, m), 5.96(1H, d, J=7.5 Hz), 6.77(1H, td, J=0.9 and 3.6 Hz), 6.85(2H, s), 6.88(1H, s), 7.37 (1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3446, 3427, 1739, 1709, 1641, 1606, 1543, 1506, 1458 cm−1. [α]D23+64.6±1.0°(c=1.004, MeOH) Anal. (C28H35NO3S.0.1H2O) Calcd.(%): C, 71.94; H, 7.59; N, 3.00; S, 6.86. Found(%): C, 71.87; H, 7.52; N, 3.31; S, 6.94.

[0596] Compound Number I-154

[0597] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.29(2H, m), 1.41-1.46(2H, m), 1.56-1.78 (4H, m), 2.00-2.19(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 3.81(1H, m), 4.10(2H, s), 5.29-5.42(2H, m), 5.98(1H, d, J=7.2 Hz), 6.75 (1H, td, J=0.9 and 3.9 Hz), 6.97-7.03(2H, m), 7.17-7.22(2H, m), 7.36(1H, d, J=3.9 Hz). IR(CHCl3): 3512, 3446, 3427, 1741, 1709, 1643, 1543, 1508 cm−1. [α]D24+66.1±1.1°(c=1.008, MeOH) Anal. (C26H30FNO3S) Calcd.(%): C, 68.54; H, 6.64; N, 3.07; S, 7.04; F,4.17. Found(%): C, 68.41; H, 6.70; N, 3.19; S, 6.90; F,3.98.

[0598] Compound Number I-155

[0599] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.19-1.29(2H, m), 1.42-1.46(2H, m), 1.58-1.78(4H, m), 2.00-2.17(5H, m), 2.35(2H, t, J=7.5 Hz), 2.52(1H, m), 3.81 (1H, m), 4.19(2H, s), 5.29-5.42(2H, m), 5.97(1H, d, J=7.8 Hz), 6.75 (1H, td, J=0.9 and 3.6 Hz), 7.34-7.37(3H, m), 7.56-7.59(2H, m). IR (CHCl3): 3512, 3444, 3427, 1741, 1709, 1643, 1543, 1506, 1325, 1167, 1130, 1066 cm−1. [α]D24+60.3±1.0°(c=1.001, MeOH) Anal. (C27H30F3NO3S) Calcd.(%): C, 64.14; H, 5.98; N, 2.77; S, 6.34; F,11.27. Found(%): C, 64.16; H, 6.04; N, 3.02; S, 6.19; F,11.17.

[0600] Compound Number I-156

[0601] mp.66-70° C.; 1H-NMR(CDCl3) δ: 1.11(1H, m), 1.22-1.30(2H, m), 1.43-1.50(2H, m), 1.60-1.78(4H, m), 2.03-2.22(5H, m), 2.36(2H, t, J=7.5 Hz), 2.54(1H, m), 3.87(1H, m), 4.08(2H, s), 5.31-5.45(2H, m), 6.21 (1H, d, J=7.2 Hz), 7.18-7.32(6H, m), 7.60(1H, d, J=0.9 Hz), 7.70(1H, d, J=0.6 Hz), 7,74 (1H, d, J=8.1 Hz). IR(KBr): 3338, 1707, 1616, 1556, 1537 cm−1. [α]D23+97.2±1.4°(c=1.016, MeOH) Anal. (C30H33NO3S.0.3H2O) Calcd.(%): C, 73.08; H, 6.87; N, 2.84; S, 6.50. Found(%): C, 73.19; H, 7.11; N, 2.98; S, 6.32.

[0602] Compound Number I-157

[0603] 1 H-NMR(CDCl3) δ: 1.03(1H, m), 1.17-1.29(2H, m), 1.38-1.47(2H, m), 1.55-1.76(4H, m), 1.97-2.18(5H, m), 2.33(2H, t, J=7.5 Hz), 2.50(1H, m), 3.80 (1H, m), 4.29(2H, s), 5.28-5.40(2H, m), 5.94(1H, d, J=7.5 Hz), 6.81 (1H, d, J=3.9 Hz), 7.32-7.39(2H, m), 7.42-7.50(2H, m), 7.69(1H, s), 7.77-7.83 (3H, m). IR(CHCl3): 3516, 3446, 3427, 2665, 1739, 1709, 1643, 1543, 1506, 1458 cm−1. [α]D23+62.8±1.0°(c=1.005, MeOH) Anal. (C30H12NO3S.0.2H2O) Calcd.(%): C, 73.35; H, 6.85; N, 2.85; S, 6.53. Found(%): C, 73.36; H, 6.84; N, 3.19; S, 6.55.

[0604] Compound Number I-158

[0605] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.20-1.32(2H, m), 1.42-1.50(2H, m), 1.57-1.84 (4H, m), 2.00-2.23(5H, m), 2.36(2H, t, J=7.5 Hz), 2.53(1H, m), 2.95-3.00(2H, m), 3.06-3.12(2H, m), 3.82(1H, m),3.83(3H, s), 5.30-5.43 (2H, m), 5.95(1H, d, J=6.9 Hz), 6.73(1H, d, J=3.6 Hz), 6.84-6.89(2H, m), 7.09 (1H, dd, J=1.5 and 7.5 Hz), 7.20(1H, dt, J=1.5 and 7.5 Hz), 7.34(1H, d, J=3.6 Hz). IR(Nujol): 3367, 3221, 3186, 3091, 3055, 2654, 1711, 1631, 1566, 1541, 1321 cm−1. [α]D25+61.3±1.020 (c=1.003, MeOH) Anal. (C28H35NO4S) Calcd.(%): C, 69.82; H, 7.32; N, 2.91; S, 6.66. Found(%): C, 69.93; H, 7.48; N, 3.09; S, 6.54.

[0606] Compound Number I-159

[0607] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.18-1.30(2H, m), 1.40-1.50(2H, m), 1.54-1.78(4H, m), 1.98-2.21(5H, m), 2.33(2H, t, J=7.2 Hz), 2.53(1H, m), 2.94-3.03 (2H, m), 3.06-3.15(2H, m), 3.83(1H, m), 5.29-5.43(2H, m), 6.12 (1H, d, J=7.5 Hz), 6.72(1H, d, J=3.6 Hz), 6.77-6.83(2H, m), 7.04-7.08(2H, m), 7.36(1H, d, J=3.6 Hz). IR(CHCl3): 3599, 3444, 3425, 3195, 1709, 1635, 1543, 1508, 1456 cm−1. [α]D25+64.8±1.0°(c=1.006, MeOH) Anal. (C27H33NO4S.0.2H2O) Calcd.(%): C, 68.82; H, 7.14; N, 2.97; S, 6.80. Found(%): C, 68.81; H, 7.10; N, 3.03; S, 6.88.

[0608] Compound Number I-160

[0609] mp.139-141° C.; 1H-NMR(CDCl3) δ: 1.12(1H, m), 1.25-1.31(2H, m), 1.45-1.51(2H, m), 1.60-1.78(4H, m), 2.02-2.22(5H, m), 2.35(2H, t, J=7.5 Hz), 2.57 (1H, m), 3.87(1H, m), 4.09(2H, s), 5.31-5.45(2H, m), 6.22 (1H, d, J=7.2 Hz), 7.19-7.33(6H, m), 7.63(1H, m), 7.71(1H, d, J=8.7 Hz), 7,73(1H, s). IR (KBr): 3338, 1705, 1616, 1560, 1537 cm−1. [α]D25+92.1±1.3°(c=1.006, MeOH) Anal. (C30H33NO3S) Calcd.(%): C, 73.89; H, 6.82; N, 2.87; S, 6.58. Found(%): C, 73.69; H, 6.75; N, 2.91; S, 6.58.

[0610] Compound Number I-161

[0611] 1 H-NMR(CDCl3) δ: 1.12(1H, m), 1.25-1.31(2H, m), 1.47-1.51(2H, m), 1.60-1.76(4H, m), 2.03-2.20(5H, m), 2.36(2H, t, J=7.2 Hz), 2.57(1H, m), 3.87 (1H, m), 4.08(2H, s), 5.31-5.45(2H, m), 6.22(1H, d, J=7.5 Hz), 6.90 (1H, dd, J=1.2 and 4.8 Hz), 6.93(1H, m), 7.25-7.29(2H, m), 7.61 and 7.71 (each 1H, each s), 7.75(1H, d, J=8.4 Hz). IR(CHCl3): 3512, 3444, 3423, 2671, 1709, 1649, 1531, 1502 cm−1. [α]D25+96.1±1.4°(c=1.005, MeOH) Anal. (C28H31NO3S2) Calcd.(%): C, 68.12; H, 6.33; N, 2.84; S, 12.99. Found(%): C, 67.89; H, 6.32; N, 2.88; S, 12.88.

[0612] Compound Number I-162

[0613] 1 H-NMR(CDCl3) δ: 1.12(1H, m), 1.24-1.31(2H, m), 1.45-1.51(2H, m), 1.60-1.78(4H, m), 2.03-2.22(5H, m), 2.36(2H, t, J=7.2 Hz), 2.57(1H, m), 3.87(1H, m), 4.25(2H, s), 5.31-5.45(2H, m), 6.25(1H, d, J=7.2 Hz), 6.81 (1H, m), 6.93(1H, dd, J=3.3 and 5.4 Hz), 7.15(1H, dd, J=1.5 and 5.4 Hz), 7.31 (1H, dd, J=1.5 and 8.1 Hz), 7.65 and 7.71(each 1H, each s), 7.76(1H, d, J=8.1 Hz). IR(CHCl3): 3516, 3444, 3423, 1741, 1709, 1649, 1531, 1502 cm−1. [α]D25+98.5±1.4°(c=1.007, MeOH) Anal. (C28H31NO3S2.0.1H2O) Calcd.(%): C, 67.87; H, 6.35; N, 2.83; S, 12.94. Found(%): C, 67.83; H, 6.29; N, 3.00; S, 12.99.

[0614] Compound Number I-163

[0615] mp.114-115° C.; 1NMR(CDCl3) δ: 1.09(1H, m), 1.20-1.30(2H, m), 1.40-1.49 (2H, m), 1.55-1.77(4H, m), 1.99-2.19(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m, 3.83(1H, m), 4.12(2H, s), 5.30-5.43(2H, m), 6.14 (1H, d, J=7.5 Hz), 6.81 and 6.93(each 1H, each m), 7.14-7.17(2H, m), 7.37(1H, d, J=1.8 Hz). IR (CHCl3): 3516, 3444, 3428, 2671, 1709, 1645, 1550, 1508, 1435 cm−1. [α]D25+71.6±1.1°(c=1.002, MeOH) Anal. (C24H29NO3S2.0.1H2O) Calcd.(%): C, 64.72; H, 6.61; N, 3.14; S, 14.40. Found(%): C, 64.50; H, 6.54; N, 3.24; S, 14.45.

[0616] Compound Number I-164

[0617] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.20-1.31(2H, m), 1.41-1.49(2H, m), 1.56-1.77(4H, m), 1.99-2.19(5H, m), 2.34(2H, t, J=7.211 Hz), 2.53(1H, m), 3.83(1H, 3.94(2H, s), 5.30-5.43(2H, m), 6.08(1H, d, J=6.9 Hz), 6.91 and 6.95 (each 1H, each m), 7.08(1H, d, J=1.5 Hz), 7.27(1H, m), 7.34(1H, d, J=1.5 Hz). IR(CHCl3): 3512. 3444, 3429, 1739, 1709, 1644, 1550, 1508 cm−1. [α]D25+69.7±1.1°(c=1.000, MeOH) Anal. (C24H29NO3S2.0.2H2O) Calcd.(%): C, 64.45; H, 6.63; N, 3.13; S, 14.34. Found(%): C, 64.37; H, 6.49; N, 3.16; S, 14.41.

[0618] Compound Number I-165

[0619] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.19-1.31(2H, m), 1.41-1.51(2H, m), 1.55-1.74(4H, m), 1.99-2.16(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m), 3.73(2H, s), 3.83(1H, m), 5.30-5.42(2H, m), 6.15(1H, d, J=6.6 Hz), 6.25, 7.10 and 7.24(each 1H, each s), 7.35-7.38(2H, m). IR(CHCl3): 3510, 3444, 3429, 2669, 1709, 1645, 1550, 1508 cm−1. [α]D25+71.635 1.1°(c=1.008, MeOH) Anal. (C24H29NO4S.0.2H2O) Calcd.(%): C, 66.85; H, 6.78; N, 3.25; S, 7.44. Found(%): C, 66.94; H, 6.81; N, 3.26; S, 7.38.

[0620] Compound Number I-166

[0621] 1 H-NMR(CDCl3) δ: 1.02(1H, m), 1.15-1.27(2H, m), 1.36-1.45(2H, m), 1.53-1.76(4H, m), 1.96-2.14(5H, m), 2.32(2H, t, J=7.2 Hz), 2.49(1H, m), 3.78 (1H, m), 4.58(2H, s), 5.27-5.39(2H, m), 5.92(1H, d, J=7.2 Hz), 6.73 and 7.32(each 1H, each d, each J=3.9 Hz), 7.37-7.51(4H, m), 7.80(1H, d, J=7.5 Hz), 7.87 and 7.97(each 1H, each m). IR(CHCl3): 3516, 3446, 3427, 2669, 1739, 1709, 1641, 1543, 1508, 1458 cm−1. [α]D25.5+62.8±1.0°(c=1.012, MeOH) Anal. (C30H33NO3S.0.1H2O) Calcd.(%): C, 73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.35; H, 6.54; N, 3.06; S, 6.51.

[0622] Compound Number I-167

[0623] mp.129-130° C.; 1H-NMR(CDCl3) δ: 1.04(1H, m), 1.16-1.28(2H, m), 1.38-1.46(2H, m), 1.54-1.73(4H, m), 1.97-2.15(5H, m), 2.31(2H, t, J=7.2 Hz), 2.51(1H, m), 3.81(1H, m), 4.37(2H, s), 5.28-5.41(2H, m), 6.04 (1H, d, J=7.5 Hz), 6.97(1H, s), 7.30-7.50(5H, m), 7.77(1H, d, J=8.1 Hz), 7.86 and 7.94(each 1H, each m). IR(CHCl3): 3514, 3444, 3427, 1739, 1709, 1645, 1549, 1508 cm−1. [α]D24+59.4±1.0°(c=1.011, MeOH) Anal. (C30H33NO3S) Calcd.(%): C, 73.89; H, 6.82; N, 2.87; S, 6.58. Found(%): C, 73.85; H, 6.90; N, 2.85; S, 6.81.

[0624] Compound Number I-168

[0625] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.21-1.33(2H, m), 1.47-1.52(2H, m), 1.59-1.80 (4H, m), 2.04-2.27(5H, m), 2.36(2H, t, J=7.5 Hz), 2.61(1H, m), 3.93(1H, m), 4.42(2H, s), 5.33-5.47(2H, m), 6.13(1H, d, J=7.5 Hz), 6.88 (1H, m), 6.92(1H, m), 7.15(1H, dd, J=1.2 and 5.1 Hz), 7.28(1H, d, J=7.5 Hz), 7.43 (1H, d, J=8.1 Hz), 7.84(1H, s), 8.20(1H, d, J=8.1 Hz). IR(CHCl3): 3512, 3438, 1709, 1651, 1518, 1495 cm−1. [α]D25+61.6±1.0°(c=1.003, MeOH) Anal. (C28H31NO3S2) Calcd.(%): C, 68.12; H, 6.33; N, 2.84; S, 12.99. Found(%): C, 67.83; H, 6.28; N, 2.96; S, 12.76.

[0626] Compound Number I-169

[0627] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.22-1.32(2H, m), 1.46-1.51(2H, m), 1.58-1.76(4H, m), 2.02-2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.60(1H, m), 3.92 (1H, m), 4.23(2H, s), 5.32-5.47(2H, m), 6.18(1H, d, J=8.1 Hz), 6.92 (1H, dd, J=1.2 and 4.8 Hz), 7.01(1H, m), 7.20-7.25(2H, m), 7.41(1H, t, J=8.1 Hz), 7.84(1H, s), 8.18(1H, d, J=7.5 Hz). IR (CHCl3): 3510, 3438, 2667, 1709, 1651, 1518, 1495 cm−1. [α]D25+61.3±1.0°(c=1.006, MeOH) Anal. (C28H31NO3S2) Calcd.(%): C, 68.12; H, 6.33; N, 2.84; S, 12.99. Found(%): C, 67.94; H, 6.30; N, 2.97; S, 12.87.

[0628] Compound Number I-170

[0629] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.21-1.33(2H, m), 1.47-1.52(2H, m), 1.59-1.79(4H, m), 2.03-2.27(5H, m), 2.36(2H, t, J=7.5 Hz), 2.61(1H, m), 3.93 (1H, m), 4.03(2H, s), 5.33-5.48(2H, m), 6.15(1H, d, J=7.2 Hz), 7.23 (1H, d, J=7.2 Hz), 7.29(1H, m), 7.35(1H, t, J=1.5 Hz), 7.42(1H, t, J=7.8 Hz), 7.85 (1H, s), 8.18(1H, (c, J=7.8 Hz). IR (CHCl3): 3518, 3438, 2663, 1739, 1709, 1651, 1518, 1496 cm−1. [α]D25+60.3±1.0®(c=1.002, MeOH) Anal. (C28H31NO4S.0.1H2O) Calcd.(%): C, 70.15; H, 6.56; N, 2.92; S, 6.69. Found(%): C, 70.03; H, 6.49; N, 2.92; S, 6.69.

[0630] Compound Number I-171

[0631] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.28(2H, m), 1.41-1.46(2H, m), 1.56-1.79(4H, m), 2.00-2.15(5H, m), 2.34(2H, t, J=7.2 Hz), 2.45(3H, s), 2.50(1H, m), 3.80(1H, m), 4.25(2H, s), 5.29-5.42(2H, m), 5,95(1H, d, J=7.5 Hz), 6.78(1H, d, J=3.6 Hz), 7.11-7.27(4H, m), 7.36(1H, d, J=3.6 Hz). IR(CHCl3): 3512, 3446, 3427, 2669, 1739, 1709, 1643, 1543, 1506 cm−1. [α]D23.5+62.8±1.0°(c=1.005, MeOH) Anal. (C27H33NO3S2) Calcd.(%): C, 67.05; H, 6.88; N, 2.90; S, 13.26. Found(%): C, 66.94; H, 7.05; N, 3.00; S, 13.14.

[0632] Compound Number I-172

[0633] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.29(2H, m), 1.41-1.46(2H, m), 1.57-1.78(4H, m), 2.01-2.19(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 2.90(3H, s), 3.80(1H, m), 4.68(2H, s), 5.29-5.43(2H, m), 6.02(1H, d, J=7.5 Hz), 6.84(1H, td, J=0.9 and 3.9 Hz), 7.37(1H,d, J=3.9 Hz), 7.42-7.51 (2H, m), 7.62(1H, dt, J=1.5 and 7.5 Hz), 8.08(1H, dd, J=1,5 and 7.5 Hz). IR(CHCl3): 3518, 3444, 3427, 1709, 1643, 1543, 1508, 1311, 1153 cm−1. [α]D23.5+59.3±1.0°(c=1.007, MeOH) Anal. (C27H33NO5S2.0.2H2O) Calcd.(%): C, 62.45; H, 6.48; N, 2.70; S, 12.35. Found(%): C, 62.47; H, 6.60; N, 2.73; S, 12.36.

[0634] Compound Number I-173

[0635] 1 H-NMR(CDCl3) δ: 1.13(1H, m), 1.23-1.36(2H, m), 1.43-1.80(6H, m), 2.03-2.24(5H, m), 2.36(2H, t, J=7.2 Hz), 2.60(1H, m), 3.91(1H, m), 3.93 (2H, s), 5.31-5.46(2H, m), 6.31(1H, d, J=7.2 Hz), 7.32-7.42(2H, m), 7.57 (1H, d, J=6.9 Hz), 7.73-7.82(3H, m), 7.94(1H, s). IR(CHCl3): 3516, 3446, 2665, 1709, 1649, 1616, 1514, 1481, 1468 cm−1. [α]D24+100.7±1.4°(c=1.008, MeOH) Anal. (C28H31NO3.0.2H2O) Calcd.(%): C, 77.64; H, 7.31; N, 3.23. Found(%): C, 77.64; H, 7.57; N, 3.29.

[0636] Compound Number I-174

[0637] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.19-1.28(2H, m), 1.40-1.47(2H, m), 1.57-1.78(4H, m), 1.99-2.18(5H, m), 2.35(2H, t, J=7.4 Hz), 2.51(1H, s), 3.21(2H, t, J=8.7 Hz), 3.81(1H, m), 4.01(2H, s), 4.58(2H, t, J=8.7 Hz), 5.29-5.42 (2H, m), 6.02(1H, d, J=7.5 Hz), 6.80(1H, d, J=3.9 Hz), 7.06(1H, d, J=1.8 Hz), 7.18(1H, d, J=1.8 Hz), 7.36(1H, d, J=3.9 Hz). IR (CHCl3): 3512, 3446, 3427, 2669, 1709, 1641, 1543, 1506, 1477, 1460, 1173 cm−1. [α]D25+53.8±0.9°(c=1.007, MeOH) Anal. (C28H32BrNO4S.0.1H2O) Calcd.(%): C, 60.02; H, 5.79; Br, 14.26; N, 2.50; S, 5.72. Found(%): C, 59.87; H, 5.68; Br, 14.13; N, 2.59; S, 5.71.

[0638] Compound Number I-175

[0639] 1 H-NMR(CDCl3) δ: 1.12(1H, m), 1.23-1.31(2H, m), 1.44-1.51(2H, m), 1.60-1.78(4H, m), 2.03-2.28(5H, m), 2.36(2H, t, J=7.4 Hz), 2.56(1H, s), 3.87(1H, m),4.21(2H, s), 5.31-5.45(2H, m), 6.21(1H, d, J=7.2 Hz), 7.18-7.37(7H, m), 7.70(1H, d, J=7.2 Hz), 7.80(1H, s). IR(CHCl3): 3514, 3444, 3423, 2667, 1709, 1649, 1537, 1502, 1454 cm−1. [α]D25+78.2±1.2°(c=1.002, MeOH) Anal. (C30H33BrNO3S.0.1H2O) Calcd.(%): C, 73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.49; H, 6.88; N, 2.89; S, 6.57.

[0640] Compound Number I-176

[0641] 1 H-NMR(CDCl3) δ: 1.12(1H, m), 1.23-1.32(2H, m), 1.44-1.51(2H, m), 1.61-1.78(4H, m), 2.03-2.28(5H, m), 2.36(2H, t, J=7.4 Hz), 2.57(1H, s), 3.88 (1H, m),4.21(2H, s), 5.31-5.45(2H, m), 6.22(1H, d, J=7.2 Hz), 6.94 (1H, dd, J=1.5 and 4.8 Hz), 7.04(1H, m), 7.21-7.25(2H, m), 7.35(1H, dd, J=7.2 and 7.8 Hz), 7.71(1H, d, J=7.2 Hz), 7.80(1H, s). IR(CHCl3): 3512, 3444, 3423, 2669, 1709, 1647, 1539, 1504 cm−1. [α]D25+77.1±1.2°(c=1.002, MeOH) Anal. (C28H31NO3S2.0.2H2O) Calcd.(%): C, 67.63; H, 6.36; N, 2.82; S, 12.90. Found(%): C, 67.57; H, 6.34; N, 2.97; S, 12.98.

[0642] Compound Number I-177

[0643] 1 H-NMR(CDCl3) δ: 1.12(1H, m), 1.25-1.32(2H, m), 1.44-1.51(2H, m), 1.60-1.78(4H, m), 2.03-2.28(5H, m), 2.31(3H, s), 2.36(2H, t, J=7.2 Hz), 2.56 (1H, s),3.87(1H, m),4.17(2H, s), 5.31-5.45(2H, m), 6.22(1H, d, J=7.2 Hz), 7.09 and 7.15(each 2H, each d, J=8.1 Hz), 7.19(1H, d, J=7.2 Hz), 7.34(1H, dd, J=7.2 and 7.8 Hz), 7.69(1H, d, J=7.8 Hz), 7.79(1H, s). IR (CHCl3): 3510, 3444, 3423, 2669, 1709, 1647, 1537, 1504 cm−1. [α]D25+75.9±1.2°(c=1.004, MeOH) Anal. (C31H35NO3S) Calcd.(%): C, 74.22; H, 7.03; N, 2.79; S, 6.39. Found(%): C, 73.93; H, 7.13; N, 2.91; S, 6.38.

[0644] Compound Number I-178

[0645] 1 H-NMR(CDCl3) δ: 1.13(1H, m), 1.24-1.31(2H, m), 1.44-1.51(2H, m), 1.60-1.77(4H, m), 2.03-2.22(5H, m), 2.36(2H, t, J=7.2 Hz), 2.56(1H, s), 3.88(1H, m),4.39(2H, s), 5.31-5.45(2H, m), 6.26(1H, d, J=7.2 Hz), 6.90-6.94(2H, m), 7.15(1H, dd, J=1.5 and 5.1 Hz), 7.27(1H, d, J=7.5 Hz), 7.36 (1H, t, J=7.5 Hz), 7.71(1H, d, J=7.5 Hz), 7.80(1H, s). IR(CHCl3): 3510, 3444, 3423, 2667, 1709, 1649, 1537, 1504 cm−1. [α]D25+76.6±1.2°(c=1.003, MeOH) Anal. (C23H31NO3S2) Calcd.(%): C, 68.12; H, 6.33; N, 2.84; S, 12.99. Found(%): C, 67.83; H, 6.45; N, 3.04; S, 13.03.

[0646] Compound Number I-179

[0647] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.28(2H, m), 1.39-1.47(2H, m), 1.56-1.78(4H, m), 1.98-2.18(5H, m), 2.34(2H, t, J=7.2 Hz), 2.50(1H, m), 3.8(1H, m), 4.08(2H, s), 5.29-5.41(2H, m), 5.95(1H, d, J=7.2 Hz), 6.53 (1H, d, J=3.6 Hz), 7.23-7.41(10H, m). IR(CHCl3): 3516, 3446, 3427, 1741, 1709, 1641, 1543, 1506, 1479, 1456 cm−1. [α]D24.5+57.6±1.0°(c=1.007, MeOH) Anal. (C32H35NO3S.0.2H2O) Calcd.(%): C, 74.30; H, 6.90; N, 2.71; S, 6.20. Found(%): C, 74.24; H, 6.89; N, 2.88; S, 6.47.

[0648] Compound Number I-180

[0649] 1 H-NMR(CDCl3) δ: 1.17(1H, m), 1.24-1.35(2H, m), 1.48-1.55(2H, m), 1.61-1.79(4H, m), 2.06-2.26(5H, m), 2.37(2H, t, J=7.2 Hz), 2.61(1H, m), 3.90 (1H, m), 5.33-5.48(2H, m), 6.44(1H, d, J=7.2 Hz), 7.31(1H, m), 7.47-7.65 (5H, m), 7.90(1H, s). IR(CHCl3): 3516, 3440, 1714, 1655, 1604, 1514, 1473, 1446 cm−1. [α]D25+92.1±1.3°(c=1.001, MeOH) Anal. (C28H29NO4.0.3H2O) Calcd.(%): C, 74.91; H, 6.65; N, 3.12. Found(%): C, 74.81; H, 6.51; N, 3.29.

[0650] Compound Number I-181

[0651] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.28(2H, m), 1.41-1.46(2H, m), 1.55-1.77(4H, m), 1.99-2.16(5H, m), 2.34(2H, t, J=7.4 Hz), 2.51(1H, s), 3.79(3H, s),3.80(1H, m), 4.08(2H, s), 5.29-5.42(2H, m), 5.97(1H, d, J=7.2 Hz), 6.75(1H, d, J=3.9 Hz), 6.85 and 7.15(each 2H, each d, J=8.4 Hz), 7.37(1H, d, J=3.9 Hz). IR(CHCl3): 3518, 3446, 3427, 1741, 1709, 1641, 1612, 1543, 1510, 1458 cm−1. [α]D25+63.6±1.0°(c=1.000, MeOH) Anal. (C27H33NO4S.0.2H2O) Calcd.(%): C, 68.88; H, 7.14; N, 2.97; S, 6.80. Found(%): C, 68.92; H, 7.02; N, 3.12; S, 6.96.

[0652] Compound Number I-182

[0653] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.27(2H, m), 1.40-1.45(2H, m), 1.59-1.78(4H, m), 1.99-2.14(5H, m), 2.34(2H, t, J=7.4 Hz), 2.51(1H, s), 3.80 (1H, m),4.37(2H, s), 5.29-5.41(2H, m), 5.97(1H, d, J=7.2 Hz), 6.82 (1H, d, J=3.6 Hz), 7.20(1H, s), 7.34-7.37(3H, m), 7.69(1H, m), 7.86(1H, m). IR (CHCl3): 3512, 3444 3427, 2669, 1709, 1643, 1543, 1508, 1458, 1431 cm−1. [α]D25+60.7±1.0°(c=1.008, MeOH) Anal. (C28H31NO3S2.0.3H2O) Calcd.(%): C, 67.39; H, 6.38; N, 2.81; S, 12.85. Found(%): C, 67.44; H, 6.30; N, 3.15; S, 12.81.

[0654] Compound Number I-183

[0655] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.26(2H, m), 1.39-44(2H, m), 1.54-1.75(4H, m), 1.99-2.15(5H, m), 2.32(2H, t, J=7.4 Hz), 2.50(1H, s), 3.80 (1H, m),4.12(2H, s), 5.28-5.42(2H, m), 6.05(1H, d, J=7.5 Hz), 6.78 (1H, d, J=3.9 Hz), 6.82-6.87(2H, m), 7.07-7.14(2H, m), 7.35(1H, d, J=3.9 Hz). IR (CHCl3): 3508, 3444, 3197, 1707, 1635, 1543, 1508, 1456 cm−1. [α]D25+64.7±1.0°((c=1.004, MeOH) Anal. (C26H31NO4S.0.2H2O) Calcd.(%): C, 68.30; H, 6.92; N, 3.06; S, 7.01. Found(%): C, 68.21; H, 6.96; N, 3.09; S, 6.93.

[0656] Compound Number I-184

[0657] 1 H-NMR(CDCl3) δ: 1.15(1H, m), 1.26-1.35(2H, m), 1.47-1.56(2H, m), 1.62-1.82(4H, m), 2.05-2.26(5H, m), 2.37(2H, t, J=7.2 Hz), 2.61(1H, m), 3.92(1H, m), 3.93(2H, s), 5.32-5.47(2H, m), 6.34(1H, d, J=6.9 Hz), 7.31-7.43 (2H, m), 7.53-7.59(2H, m), 7.67(1H, m), 7.5(1H, d, J=6.9 Hz), 8.17 (1H, s). IR(CHCl3): 3514, 3444, 2667, 1709, 1651, 1572, 1516, 1481, 1452 cm−1. [α]D24+81.2±1.2°(c=1.002, MeOH) Anal. (C28H31NO3.0.2H2O) Calcd.(%): C, 77.64; H, 7.31; N, 3.23. Found(%): C, 77.59; H, 7.15; N, 3.44.

[0658] Compound Number I-185

[0659] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.21-1.28(2H, m), 1.41-1.46(2H, m), 1.58-1.78(4H, m), 2.00-2.16(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m), 3.79 (1H, m), 4.16(2H, s), 5.31-5.40(2H, m), 5.93(1H, d, J=7.8 Hz), 6.80 (1H, d, J=3.6 Hz), 7.03-7.12(2H, m), 7.20-7.28(2H, m), 7.35(1H, d, J=3.6 Hz). IR (CHCl3): 3518, 3444, 3427, 1741, 1709, 1643, 1543, 1506, 1456 cm−1. [α]D24+56.2±0.9°(c=1.03, CHCl3) Anal. (C26H30FNO3S.0.4H2O) Calcd.(%): C, 67.48; H, 6.71; N, 3.03; S, 6.93; F, 4.11. Found(%): C, 67.49; H, 6.72; N, 3.09; S, 6.93; F, 4.11.

[0660] Compound Number I-186

[0661] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.19-1.29(2H, m), 1.41-1.46(2H, m), 1.58-1.82(4H, m), 2.00-2.16(5H, m), 2.34(2H, t, J=7.4 Hz), 2.51(1H, s), 3.80(1H, m),4.17(2H, s), 5.08(2H, s), 5.28-5.41(2H, m), 5.90(1H, d, J=7.5 Hz), 6.76(1H, d, J=3.9 Hz), 6.90-6.95(2H, m), 7.18-7.25(2H, m), 7.31-7.38 (6H, m). IR(CHCl3): 3516, 3446, 3427, 1741, 1709, 1641, 1601, 1543, 1502, 1454 cm−1. [α]D24+53.9±0.9°(c=1.005, MeOH) Anal. (C33H37NO4S) Calcd.(%): C, 72.90; H, 6.86; N, 2.58; S, 5.90. Found(%): C, 72.64; H, 6.92; N, 2.52; S, 5.74.

[0662] Compound Number I-187

[0663] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.28(2H, m), 1.41-1.46(2H, m), 1.57-1.78(4H, m), 1.99-2.15(5H, m), 2.34(2H, t, J=7.4 Hz), 2.51(1H, s), 3.80 (1H, m),4.16(2H, s), 4.54-4.57(2H, m), 5.24-5.41(4H, m), 5.94(1H, d, J=7.5 Hz), 6.04(1H, m), 6.79(1H, d, J=3.9 Hz), 6.85-6.93(2H, m), 7.15-7.24 (2H, m), 7.34(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3446, 3427, 1739, 1709, 1641, 1543, 1506, 1477 cm−1. [α]D24+59.0±1.0°(c=1.007, MeOH) Anal. (C29H35NO4S.0.2H2O) Calcd.(%): C, 70.05; H, 7.18; N, 2.82; S, 6.45. Found(%): C, 69.97; H, 7.16; N, 2.80; S, 6.52.

[0664] Compound Number I-188

[0665] mp.84-85° C.; 1-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.29(2H, m), 1.41-1.46 (2H, m), 1.56-1.81(4H, m), 2.00-2.17(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51 (1H, s), 3.80(1H, m),4.07(2H, s), 5.05(2H, s), 5.29-5.42(2H, m), 5.93 (1H, d, J=7.5 Hz), 6.75(1H, d, J=3.9 Hz), 6.92 and 7.15(each 2H, each d, J=8.7 Hz), 7.31-7.44( 6H, m). IR(CHCl3): 3521, 3446, 3427, 1741, 1709, 1643, 1612, 1543, 1510, 1456 cm−1. [α]D24+56.1±1.0°(c=1.002, MeOH) Anal. (C33H37NO4S) Calcd.(%): C, 72.90; H, 6.86; N, 2.58; S, 5.90. Found(%): C, 72.78; H, 6.88; N, 2.74; S, 5.84.

[0666] Compound Number I-189

[0667] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.19-1.29(2H, m), 1.41-1.46(2H, m), 1.56-1.79(4H, m), 2.00-2.15(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, s), 3.80 (1H, m),4.07(2H, s), 4.51-4.53(2H, m), 5.26-5.44(4H, m), 5.94(1H, d, J=7.5 Hz), 6.05(1H, m), 6.76(1H, d, J=3.9 Hz), 6.87 and 7.14(each 2H, each d, J=8.7 Hz), 7.36(1H, d, J=3.9 Hz). IR(CHCl3): 3512, 3446, 3427, 1741, 1709, 1643, 1612, 1543, 1508, 1458 cm−1. [α]D24+61.6±1.0°(c=1.004, MeOH) Anal. (C29H35NO4S.0.4H2O) Calcd.(%): C, 69.54; H, 7.20; N, 2.78; S, 6.40. Found(%): C, 69.47; H, 7.22; N, 2.84; S, 6.51.

[0668] Compound Number I-190

[0669] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.32(2H, m), 1.39-1.48(2H, m), 1.54-1.80(4H, m), 1.98-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.81(1H, m), 4.04(2H, s), 5.29-5.42(2H, m), 5.93(1H, d, J=7.5 Hz), 6.68-6.78(2H, m), 7.36(1H, d, J=3.6 Hz). IR(CHCl3): 3517, 3446, 3427, 1741, 1709, 1643, 1543, 1504, 1489, 1444, 1250, 1041 cm−1. [α]D24+59.4±1.0°(c=1.0111, MeOH) Anal. (C27H31NO5S) Calcd.(%): C, 67.34; H, 6.49; N, 2.91; S, 6.66. Found(%): C, 67.27; H, 6.45; N, 3.04; S, 6.63.

[0670] Compound Number I-191

[0671] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.18-1.32(2H, m), 1.39-1.48(2H, m), 1.54-1.80(4H, m), 1.98-2.20(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 3.81 (1H, m), 4.12(2H, s), 5.30-5.42(2H, m), 6.04(1H, d, J=7.2 Hz), 6.77 (1H, d, J=3.6 Hz), 6.89-7.04(3H, m), 7.28(1H, m), 7.38(1H, d, J=3.6 Hz). IR(CHCl3): 3518, 3446, 3427, 1739, 1709, 1643, 1545, 1506 cm−1. [α]D25+62.6±1.0°(c=1.009, MeOH) Anal. (C26H30FNO3S) Calcd.(%): C, 68.54; H, 6.64; N, 3.07; S, 7.04; F,4.17. Found(%): C, 68.25; H, 6.37; N, 3.19; S, 7.12; F,4.12.

[0672] Compound Number I-192

[0673] 1 H-NMR(CDCl3), : 1.06(1H, m), 1.18-1.32(2H, m), 1.40-1.48(2H, m), 1.54-1.80(4H, m), 1.98-2.20(5H, m), 2.35(2H, t, J=7.5 Hz), 2.52(1H, m), 3.81(1H, m), 4.19(2H, s), 5.30-5.42(2H, m), 5.99(1H, d, J=7.2 Hz), 6.78 and 7.37(each 1H, each d, each J=3.6 Hz), 7.40-7.54(4H, m). IR(CHCl3): 3516, 3446, 3427, 1740, 1709, 1643, 1545, 1506, 1450, 1330, 1167, 1130, 1074 cm−1. [α]D25+55.4±0.9°(c=1.029, MeOH) Anal. (C27H30F3NO3S) Calcd.(%): C, 64.14; H, 5.98; N, 2.77; S, 6.34; F,11.27. Found(%): C, 63.95; H, 5.99; N, 2.90; S, 6.36; F, 10.98.

[0674] Compound Number I-193

[0675] 1 H-NMR(CDCl3)) δ: 1.05(1H, m), 1.24-1.28(2H, m), 1.42-1.46(2H, m), 1.58-1.79(4H, m), 2.01-2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80 (1H, m), 4.26(2H, s), 5.33-5.38(2H, m), 5.94(1H, (c, J=7.2 Hz), 6.79 (1H, d, J=3.9 Hz), 7.21-7.28(3H, m), 7.35-7.40(2H, m). IR(CHCl3): 3518, 3446, 3427, 1743, 1709, 1643, 1543, 1506 cm−1. [α]D25+55.5±0.9°(c=1.06, CHCl3) Anal. (C26H30ClNO3S.0.3H2O) Calcd.(%): C, 65.41; H, 6.46; N, 2.93; S, 6.72; Cl, 7.43. Found(%): C, 65.41; H, 6.40; N, 3.08; S, 6.75; Cl, 7.31.

[0676] Compound Number I-194

[0677] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.28(2H, m), 1.39-1.46(2H, m), 1.56-1.78 (4H, m), 1.98-2.16(5H, m), 2.30(6H, s), 2.34(2H, t, J=7.2 Hz), 2.50 (1H, m), 3.80(1H, m), 4.16(2H, s), 5.28-5.41(2H, m), 5.93(1H, d, J=6.9 Hz), 6.78(1H, d, J=3.9 Hz), 7.03-7.14(3H, m), 7.77(1H, d, J=3.9 Hz). IR (CHCl3): 3516, 3446, 3427, 2669, 1709, 1641, 1543, 1506, 1456 cm−1. [α]D24+66.6±1.0°(c=1.009, MeOH) Anal. (C28H35NO3S.0.2H2O) Calcd.(%): C, 71.67; H, 7.60; N, 2.98; S, 6.83. Found(%): C, 71.71; H, 7.54; N, 3.15; S, 6.81.

[0678] Compound Number I-195

[0679] 1 H-NMR(CDCl3)) δ: 1.05(1H, m), 1.22-1.28(2H, m), 1.42-1.47(2H, m), 1.59-1.78(4H, m), 2.01-2.17(5H, m), 2.35(2H, t, J=7.2 Hz), 2.50(1H, m), 3.82(1H, m), 4.32(2H, s), 5.35-5.37(2H, m), 5.94(1H, d, J=6.9 Hz), 6.76 (1H, d, J=3.9 Hz), 7.33-7.39(3H, m), 7.50 (1H, m), 7.69(1H, d, J=3.9 Hz). IR (CHCl3): 3316, 3446, 3427, 1743, 1709, 1643, 1543, 1506, 1456, 1163, 1126 cm−1. [α]D25+54.5±1.0°(c=1.00, CHCl3) Anal. (C27H30F3NO3S.0.2H2O) Calcd.(%): C, 63.93; H, 6.02; N, 2.75; S, 6.30. Found(%): C, 63.92; H, 5.85; N, 2.94; S, 6.38.

[0680] Compound Number I-196

[0681] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.22-1.28(2H, m), 1.42-1.46.(2H, m), 1.58-1.80 (4H, m), 2.01-2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81 (1H, m), 3.88(3H, s), 4.06(2H, s), 5.33-5.38(2H, m), 5.94(1H, d, J=10.2 Hz), 6.70(1H, d, J=3.6 Hz), 6.87-6.97(3H, m), 7.36(1, d, J=3.6 Hz). IR (CHCl3): 3517, 3446, 3427, 2673, 1741, 1709, 1643, 1543, 1516, 1274 1030 cm−1. [α]D25+54.2±0.9°(c=1.00, CHCl3) Anal. (C27H32FNO4S.0.3H2O) Calcd.(%): C, 66.04; Ft, 6.69; N, 2.85; S, 6.53; F, 3.87. Found(%): C, 66.16; H, 6.61; N, 2.82; S, 6.34; F, 3.66.

[0682] Compound Number I-197

[0683] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.27(2H, m), 1.41-1.45(2H, m), 1.56-1.77(4H, m), 1.98-2.13(5H, m), 2.34(2H, t, J=7.5 Hz), 2.50(1H, s), 3.21 (2H, t, J=8.7 Hz), 3.80(1H, m), 4.07(2H, s), 4.57(2H, t, J=8.7 Hz), 5.29-5.41 (2H, m), 6.00(1H, d, J=7.5 Hz), 6.79(1H, d, J=3.6 Hz), 6.79(1H, dd, J=7.2 and 7.5 Hz), 6.95(1H, d, J=7.5 Hz), 7.09(1H, d, J=7.2 Hz), 7.36(1H, d, J=3.6 Hz). IR(CHCl3): 3514, 3446, 3427, 2669,.1739, 1709, 1641, 1543, 1506, 1477, 1456, 1441 cm−1. [α]D25+61.1±1.0°(c=1.004, MeOH) Anal. (C28H33NO4S.0.2H2O) Calcd.(%): C, 69.60; H, 6.97; N, 2.90; S, 6.63. Found(%): C, 69.68; H, 6.89; N, 3.19; S, 6.65.

[0684] Compound Number I-198

[0685] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.18-1.27(2H, m), 1.40-1.46(2H, m), 1.56-1.76(4H, m), 1.98-2.13(5H, m), 2.33(2H, t, J=7.5 Hz), 2.50(1H, s), 3.21(2H, t, J=8.7 Hz), 3.80(1H, m), 4.24(2H, s), 5.28-5.40(2H, m), 5.97(1H, d, J=7.2 Hz), 6.79(1H, d, J=3.6 Hz), 7.22(1H, dd, J=1.2 and 8.1 Hz), 7.29 (1H, d, J=5.4 Hz), 7.38(1H, d,J=3.6 Hz), 7.44(1H, d, J=5.4 Hz), 7.68(1H, d, J=1.2 Hz), 7.81(1H, d, J=8.1 Hz). IR(CHCl3): 3516, 3446, 3427, 1741, 1709, 1643, 1543, 1506, 1547 cm−1. [α]D25+62.0±1.0°(c=1.000, MeOH) Anal. (C28H31NO3S2.0.2H2O) Calcd.(%): C, 67.63; H, 6.36; N, 2.82; S, 12.90. Found(%): C, 67.55; H, 6.28; N, 2.97; S, 12.90.

[0686] Compound Number I-199

[0687] 1 H-NMR(CDCl3)) δ: 1.04(1H, m), 1.17-1.27(2H, m), 1.40-1.45(2H, m), 1.54-1.77(4H, m), 1.98-2.15(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, s), 3.80 (1H, m),4.25(2H, s), 5.28-5.41(2H, m), 5.97(1H, d, J=7.2 Hz), 6.79(1H, d, J=3.9 Hz), 7.24(1H, dd, J=1.5 and 8.1 Hz), 7.30(1H, d, J=5.4 Hz), 7.38(1H, d, J=3.6 Hz), 7.41(1H, d, J=5.4 Hz), 7.73(1H, m), 7.76(1H, d, J=8.1 Hz). IR(CHCl3): 3516, 3447, 3427, 1741, 1709, 1643, 1543, 1506, 1458 cm−1. [α]D25+62.1±1.0°(c=1.008, MeOH) Anal. (C28H31NO3S2.0.3H2O) Calcd.(%): C, 67.39; H, 6.38; N, 2.81; S, 12.85. Found(%): C, 67.42; H, 6.29; N, 2.99; S, 12.94.

[0688] Compound Number I-200

[0689] 1 H-NMR(CDCl3) δ: 1.03(1H, m), 1.16-1.22(2H, m), 1.39-1.44(2H, m), 1.53-1.76 (4H, m), 1.97-2.14(5H, m), 2.33(2H, t, J=7.5 Hz), 2.49(1H, s), 3.79 (1H, m),4.39(2H, s), 5.28-5.40(2H, m), 5.98(1H, d, J=7.5 Hz), 6.86(1H, d, J=3.9 Hz), 7.21(1H, d, J=6.9 Hz), 7.35(1H, dd, J=6.9 and 8.1 Hz), 7.36(1H, d, J=5.4 Hz), 7.36(1H, d, J=3.9 Hz), 7.42(1H, d, J=5.4 Hz), 7.74(1H, d, J=8.1 H). IR(CHCl3): 3516, 3446, 3427, 1739, 1709, 1643, 1543, 1506, 1458 cm−1. [α]D25+58.4±1.0°(c=1.003, MeOH) Anal. (C28H31NO3S2.0.2H2O) Calcd.(%): C, 67.63; H, 6.36; N, 2.82; S, 12.90. Found(%): C, 67.62; H, 6.27; N, 3.09; S, 12.92.

[0690] Compound Number I-201

[0691] 1 H-NMR(CDCl3+CD3OD) δ: 1.08(1H, m), 1.22-1.28(2H, m), 1.41-1.46(2H, m), 1.55-1.71(4H, m), 2.01-2.10(5H, m), 2.29(2H, t, J=7.4 Hz), 2.51(1H, s), 3.77(1H, m), 4.29(2H, s), 5.34-5.40(2H, m), 6.80(1H, d, J=3.9 Hz), 6.93(1H, dd, J=1.8 and 8.7 Hz), 7.10(1H, d, J=1.8 Hz), 7.22(1H, s), 7.36(1H, d, J=3.9 Hz), 7.65(1H, d, J=8.7 Hz). IR(CHCl3): 3508, 3423, 3236, 1709, 1633, 1601, 1545, 1510, 1441 cm−1. [α]D25+57.5±1.0°(c=1.006, MeOH) Anal. (C28H31NO4S2.0.2H2O) Calcd.(%): C, 64.84; H, 6.21; N, 2.70; S, 12.36. Found(%): C, 67.57; H, 6.20; N, 2.93; S, 12.38.

[0692] Compound Number I-202

[0693] 1 H-NMR(CDCl3) δ: 1.05(1H, m),, 1.24-1.28(2H, m), 1.41-1.48(2H, m), 1.58-1.79(4H, m), 2.02-2.22(5H, m), 2.33(2H, t, J=7.5 Hz), 2.51(1H, m), 3.78 (1H, m), 4.25(2H, s), 4.70(2H, s), 5.31-5.42(2H, m), 6.00(1H, d, J=7.2 Hz), 6.74(1H, d, J=3.6 Hz), 7.24-7.42(5H, m). IR(CHCl3): 3518, 3444, 3427, 1709, 1643, 1543, 1506, 1456 cm−1. [α]D26+51.9±0.9°(c=1.04, CHCl3) Anal. (C27H33FNO4S.0.7H2O) Calcd.(%): C, 67.53; H, 7.22; N, 2.92; S, 6.02. Found(%): C, 67.92; H, 7.13; N, 2.88; S, 6.11.

[0694] Compound Number I-203

[0695] 1 H-NMR(CDCl3) δ: 1.02(1H, m), 1.22-1.28(2H, m), 1.40-1.42(2H, m), 1.57-1.72(4H, m), 1.82-1.85(4H, m), 2.01-2.13(5H, m), 2.27(2H, t, J=7.5 Hz), 2.49(1H, m), 2.71-2.73(4H, m), 3.67(1H, d, J=13.2 Hz), 3.76 (1H,m), 3.83(1H, d, J=13.2 Hz), 4.26(1H, d, J=16.5 Hz), 4.34(1H, d, J=16.5 Hz), 5.33-5.45(2H, m), 6.04(1H, d, J=7.2 Hz), 6.70(1H, d, J=3.6 Hz), 7.16-7.33 (4H, m), 7.43((1H, d, J=3.6 Hz). IR(CHCl3): 3518, 3446, 3424, 2472, 1707, 1643, 1545, 1506, 1456 cm−1. [α]D26+41.9.±0.8°(c=1.03, CHCl3) Anal. (C31H40N2O3S.0.6H2O) Calcd.(%): C, 70.05; H, 7.81; N, 5.27; S, 6.03. Found(%): C, 70.01; H, 7.81; N, 5.18; S, 5.86.

[0696] Compound Number I-204

[0697] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.22-1.29(2H, m), 1.41-1.46(2H, m), 1.58-1.72(4H, m), 2.03-2.17(5H, m), 2.31(2H, t, J=7.2 Hz), 2.51(1H, m), 2.60 (6H, s), 3.79(1H, m), 3.94(1H, d, J=13.2 Hz), 3.99(1H, d, J=13.2 Hz), 4.39 (2H,s), 5.30-5.44(2H, m), 6.01(1H, d, J=7.2 Hz), 6.72(1H, d, J=3.9 Hz), 7.26-7.40(4H, m), 7.56(1H, d, J=7.2 Hz). IR(CHCl3): 3519, 3444, 3425, 2455, 1753, 1712, 1643, 1545, 1508, 1458 cm−1. [α]D26+41.2±0.8°(c=1.02, CHCl3) Anal. (C29H38N2O3S.1.7H20.2CHCl3) Calcd.(%): C, 63.86; H, 7.63; N, 5.10; S, 5.84 Cl, 3.87. Found(%): C, 63.88; H, 7.51; N, 4.94; S, 5.63; Cl, 4.22.

[0698] Compound Number I-205

[0699] 1 H-NMR(CDCl3)) δ: 1.14(1H, m), 1.24-1.36(2H, m), 1.45-1.54(2H, m), 1.60-1.79(4H, m), 2.03-2.26(5H, m), 2.36(2H, t, J=7.5 Hz), 2.58(1H, m), 3.19-3.26(4H, m), 3.89(1H, m), 5.32-5.45(2H, m), 6.33(1H, d, J=6.3 Hz), 7.24(1H, d, J=7.2 Hz), 7.34 and 7.46(each 1H, each m), 7.61(1H, dd, J=1.5 and 8.4 Hz), 7.68(1H, d, J=1.5 Hz), 7.98-8.04(2H, m). IR(CHCl3): 3518, 3444, 2667, 1709, 1649, 1597, 1514, 1483, 1450, 1294 cm−1. [α]D25+78.7±1.2°(c=1.003, MeOH) Anal. (C30H33NO4) Calcd.(%): C, 75.54; H, 7.10; N, 2.94. Found(%): C, 75.62; H, 7.05; N, 2.94.

[0700] Compound Number I-206

[0701] 1 H-NMR(CDCl33) δ: 1.10(1H, m), 1.22-1.36(2H, m), 1.40-1.52(2H, m), 1.56-1.81(4H, m), 2.00-2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.50(1H, m), 3.84 (1H, m), 3.99(2H, s), 5.30-5.43(2H, m), 6.05(1H, d, J=3.3 Hz), 6.29(1H, d, J=7.8 Hz), 6.99-7.05(3H, m), 7.17-7.22(2H, m). IR(CHCl3): 3512, 3435, 1739, 1709, 1653, 1606, 1549, 1510 cm−1. [α]D26+71.0±1.1°(c=1.005, MeOH) Anal. (C26H30FNO4O) Calcd.(%): C, 71.05; H, 6.88; N, 3.19; F,4.32. Found(%): C, 70.78; H, 6.97; N, 3.30; F,4.27.

[0702] Compound Number I-207

[0703] 1 H-NMR(CDCl3) δ: 1.10(1H, m), 1.22-1.34(2H, m), 1.40-1.50(2H, m), 1.56-1.81(4H, m), 2.00-2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.50(1H, m), 3.84 (1H, m), 4.02(2H, s), 5.30-5.43(2H, m), 6.07(1H, d, J=3.3 Hz), 6.30(1H, d, J=7.5 Hz), 7.02(1H, d, J=3.3 Hz), 7.22-7.36(5H, m). IR(CHCl3): 3516, 3435, 2669, 1709, 1651, 1606, 1547, 1498 cm−1. [α]D24+76.5±1.2°(c=1.005, MeOH) Anal. (C26H31FNO4.0.1H2O) Calcd.(%): C, 73.77; H, 7.43; N, 3.31. Found(%): C, 73.63; H, 7.27; N, 3.42.

[0704] Compound Number I-208

[0705] 1 H-NMR(CDCl3)) δ: 1.04(1H, m), 1.16-1.26(2H, m), 1.39-1.44(2H, m), 1.55-1.76(4H, m), 1.98-2.18(5H, m), 2.33(2H, t, J=7.2 Hz), 2.50(1H, s), 3.79 (1H, m),4.42(2H, s), 5.28-5.40(2H, m), 5.98(1H, d, J=6.9 Hz), 6.78(1H, d, J=2.1 Hz), 6.84(1H, d, J=3.6 Hz), 7.12-7.21(2H, m), 7.36(1H, d, J=3.6 Hz), 7.50(1H, dd, J=1.5 and 7.5 Hz), 7.63(1H, d, J=2.1 Hz). IR(CHCl3): 3516, 3446, 3427, 2665, 1741, 1709, 1643, 1523, 1506, 1458, 1427 cm−1. [α]D25+63.4±1.0°(c=1.006, MeOH) Anal. (C28H31NO4S.0.2H2O) Calcd.(%): C, 69.89; H, 6.58; N, 2.91; S, 6.66. Found(%): C, 69.68; H, 6.48; N, 3.10; S, 6.62.

[0706] Compound Number I-209

[0707] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.22-1.29(2H, m), 1.42-1.47(2H, m), 1.59-1.82(4H, m), 2.01-2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 2.94 (3H,s), 3.81(1H, m), 4.19(2H, s), 4.44(2H, s), 5.31-5.38(2H, m), 5.35 (1H,d, J=7.2 Hz), 6.63-6.72(4H, m), 7.16-7.25(6H, m), 7.36(1H, d, J=3.6 Hz). IR (CHCl3): 3514, 3444, 3427, 1741, 1709, 1643, 1599, 1543, 1506, 1456 cm−1. [α]D26+50.8±0.9°(c=1.04, CHCl3) Anal. (C34H40N2O3S.0.7H2O) Calcd.(%): C, 71.72; H, 7.33; N, 4.92; S, 5.63. Found(%): C, 71.81; H, 7.29; N, 4.81; S, 5.54.

[0708] Compound Number I-210

[0709] 1 H-NMR (CHCl3) δ: 1.14-1.68(11H, m), 1.91-2.16(9H, m), 2.21(2H, t, J=7.2 Hz), 2.57(1H, m), 2.98(1H, m), 3.71(1H, m), 3.89(2H, s), 4.28(1H, d, J=16.5 Hz), 4.30(1H, d, J=16.5 Hz), 5.28-5.50(3H, m), 6.56(1H, m), 6.75(1H, m), 7.20-7.33 (2H, m), 7.49-7.55(2H, m). IR(CHCl3): 3518, 3425, 1753, 1711, 1641, 1545, 1508, 1456 cm−1. [α]D26+35.6±0.7°(c=1.03, CHCl3)

[0710] Compound Number I-211

[0711] 1 H-NMR(CDCl3) δ: 1.04(1H, m), 1.17-1.28(2H, m), 1.39-1.46(2H, m), 1.54-1.78(4H, m), 1.98-2.19(5H, m), 2.33(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80(1H, m), 4.29(2H, s), 5.28-5.40(2H, m), 5.95(1H, d, J=7.2 Hz), 6.82(1H, d, J=3.6 Hz), 7.23(1H, dd, J=1.5 and 8.1 Hz), 7.30-7.47(4H, m), 7.55(1H, d, J=8.1 Hz), 7.89(1H, d, J=7.8 Hz), 7.93(1H, dd, J=1.5 and 7.8 Hz). IR (CHCl3): 3510, 3446, 3427, 2671, 1739, 1709, 1641, 1545, 1506, 1458, 1427 cm−1. [α]D24+60.2±1.0°(c=1.006, MeOH) Anal. (C32H33NO4S.0.2H2O) Calcd.(%): C, 72.34; H, 6.34; N, 2.64; S, 6.04. Found(%): C, 72.28; H, 6.25; N, 2.72; S, 5.93.

[0712] Compound Number I-212

[0713] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.30(2H, m), 1.38-1.47(2H, m), 1.54-1.80(4H, m), 1.98-2.20(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 3.78 (3H, s), 3.80(1H, m), 3.86(3H, s), 4.15(2H, s), 5.29-5.42(2H, m), 5.93(1H, d, J=7.5 Hz), 6.78-6.85(3H, m), 7.01(1H, t, J=8.1 Hz), 7.36(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3446, 3425, 2667, 1739, 1709, 1641, 1543, 1506, 1481, 1273, 1076 cm−1. [α]D25+60.8±1.0°(c=1.002, MeOH) Anal. (C28H35NO5S.0.1H2O) Calcd.(%): C, 67.33; H, 7.10; N, 2.80; S, 6.42. Found(%): C, 67.21; H, 7.08; N, 2.92; S, 6.45.

[0714] Compound Number I-213

[0715] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.19-1.30(2H, m), 1.42-1.47(2H, m), 1.58-1.78(4H, m), 2.01-2.16(5H, m), 2.38(2H, t, J=7.2 Hz), 2.39(3H, s), 2.53 (1H, s),3.82(1H, m), 4.15(2H, s), 5.31-5.44(2H, m), 5.87(1H, s), 6.05(1H, d, J=7.2 Hz), 6.86(1H, d, J=3.9 Hz), 7.38(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3444, 3427, 2669, 1709, 1643, 1608, 1545, 1508, 1456 cm−1. [α]D25+64.3±1.0°(c=1.012, MeOH) Anal. (C24H30N2O4S.0.2H2O) Calcd.(%): C, 64.61; H, 6.87; N, 6.28; S, 7.19. Found(%): C, 64.70; H, 6.84; N, 6.34; S, 7.27.

[0716] Compound Number I-214

[0717] 1 H-NMR(CDCl3) δ: 1.06(1H, m), 1.19-1.28(2H, m), 1.41-1.46(2H, m), 1.58-1.79(4H, m), 2.00-2.15(5H, m), 2.33-2.37(5H, m), 2.51(1H, s), 3.81-3.82 (4H,m), 4.08(2H, s), 5.29-5.42(2H, m), 5.93(1H, d, J=6.9 Hz), 6.70(1H, s), 6.72(1H, d, J=7.8 Hz), 6.77(1H, d, J=3.6 Hz), 7.04(1H, d, J=7.8 Hz), 7.34 (1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3446, 3427, 2669, 1741, 1709, 1641, 1614, 1583, 1506, 1458 cm−1. [α]D25+58.9±1.0°(c=1.012, MeOH) Anal. (C28H35N4S.0.2H2O) Calcd.(%): C, 69.31; H, 7.35; N, 2.89; S, 6.61. Found(%): C, 69.21; H, 7.35; N, 3.03; S, 6.65.

[0718] Compound Number I-215

[0719] mp.128-129° C.; 1H-NMR(CDCl3) δ: 1.05 (1H, m), 1.19-1.28 (2H, m), 1.41-1.46 (2H, m), 1.56-1.79(4H, m), 2.00-2.15(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, s), 3.80(1H, m), 3.84(3H, s), 4.33(2H, s), 5.29-5.42 (2H, m), 5.94(1H, d, J=6.9 Hz), 6.83(1H, d, J=3.6 Hz), 7.01(1H, dd, J=2.7 and 9.0 Hz), 7.11(1H, d, J=2.7 Hz), 7.21(1H, s), 7.36(1H, d, J=3.6 Hz), 7.72 (1H, d, J=9.0 Hz). IR(CHCl3): 3516, 3446, 3427, 1739, 1709, 1643, 1601, 1543, 1506, 1458, 1427 cm−1. [α]D25+55.7±1.0°(c=1.008, MeOH) Anal. (C29H33NO4S2) Calcd.(%): C, 66.51; H, 6.35; N, 2.67; S, 12.25. Found(%): C, 66.41; H, 6.30; N, 2.96; S, 12.15.

[0720] Compound Number I-216

[0721] 1 H-NMR(CDCJ3) δ: 1.04(1H, m), 1.16-1.29(2H, m), 1.39-1.46(2H, m), 1.55-1.79 (4H, m), 1.98-2.19(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80 (1H, m), 3.87 and 4.20(each 2H, each s), 5.28-5.40(2H, m), 5.93(1H, d, J=8.1 Hz), 6.81(1H, d, J=3.9 Hz), 7.24-7.39(5H, m), 7.53(1H, d, J=7.2 Hz), 7.71-7.77(2H, m). IR(CHCl3): 3516, 3446, 3427, 1739, 1709, 1643, 1543, 1506, 1456 cm−1. [α]D25+56.7±1.0°(c=1.000, MeOH) Anal. (C33H35NO3S.0.1H2O) Calcd.(%): C, 75.14; H, 6.73; N, 2.66; S, 6.08. Found(%): C, 75.14; H, 6.80; N, 2.74; S, 5.83.

[0722] Compound Number I-217

[0723] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.19-1.32(2H, m), 1.40-1.48(2H, m), 1.56-1.78 (4H, m), 2.00-2.21(5H, m), 2.34(2H, t, J=7.5 Hz), 2.54(1H, m), 3.13-3.24 (4H, m), 3.85(1H, m), 4.13(2H, s), 5.28-5.42(2H, m), 6.17(1H, d, J=7.2 Hz), 7.06-7.17(4H, m), 7.22(1H, d, J=7.8 Hz), 7.44(1H, dd, J=1.8 and 7.8 Hz), 7.53(1H, d, J=1.8 Hz). IR(CHCl3): 3518, 3446, 1739, 1709, 1651, 1570, 1518, 1491, 1456 cm−1. [α]D25+73.3±1.1°(c=1.000, MeOH) Anal. (C30H35NO3.0.2H2O) Calcd.(%): C, 78.13; H, 7.44; N, 3.04. Found(%): C, 78.25; H, 7.76; N, 3.29.

[0724] Compound Number I-218

[0725] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.30(2H, m), 1.39-1.48(2H, m), 1.54-1.81(4H, m), 1.98-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80(1H, m), 3.82, 3.85 and 3.87(each 3H, each s), 4.07(2H, s), 5.29-5.42 (2H, m), 5.94(1H, d, J=7.5 Hz), 6.62(1H, d, J=8.7 Hz), 6.76(1H, d, J=3.6 Hz), 6.85(11H, d, J=8.7 Hz), 7.35(1H, d, J=3.6 Hz). IR(CHCl3): 3514, 3446, 3427, 1739, 1709, 1641, 1603, 1543, 1495, 1468, 1277, 1259, 1097 cm−1. [α]D26+54.8±1.0°(c=1.013, MeOH) Anal. (C29H37NO6S.0.2H2O) Calcd.(%): C, 65.56; H, 7.10; N, 2.64; S, 6.04. Found(%): C, 65.54; H, 6.96; N, 2.74; S, 5.98.

[0726] Compound Number I-219

[0727] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.30(2H, m), 1.39-1.48(2H, m), 1.54-1.81(4H, m), 1.98-2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80 (1H, m), 3.82, 3.85 and 3.87(each 3H, each s), 4.07(2H, s), 5.29-5.42 (2H, m), 5.94(1H, d, J=7.5 Hz), 6.62(1H, d, J=8.7 Hz), 6.76(1H, d, J=3.6 Hz), 6.85(1H, d, J=8.7 Hz), 7.35(1H, d, J=3.6 Hz). IR(CHCl3): 3514, 3446, 3427, 1739, 1709, 1641, 1603, 1543, 1495, 1468, 1277, 1259, 1097 cm−1. [α]D26+54.8±1.0°(c=1.013, MeOH) Anal. (C29H37NO6S.0.2H2O) Calcd.(%): C, 65.56; H, 7.10; N, 2.64; S, 6.04. Found(%): C, 65.54; H, 6.96; N, 2.74; S, 5.98.

[0728] Compound Number I-220

[0729] mp.131-133° C.; 1H-NMR(CDCl3)) δ: 1.06(1H, m), 1.18-1.31(2H, m), 1.40-1.48 (2H, m), 1.56-1.82(4H, m), 2.00-2.21(5H, m), 2.35(2H, t, J=7.5 Hz), 2.52 (1H, m), 3.82(1H, m), 3.83(3H, s), 3.84(6H, s), 4.07(2H, s), 5.30-5.42 (2H, m), 5.95(1H, d, J=7.5 Hz), 6.45(2H, s), 6.79(1H, d, J=3.6 Hz), 7.36(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3446, 3427, 1739, 1709, 1643, 1593, 1543, 1506, 1462, 1421, 1331, 1240, 1130 cm−1. [α]D24+57.5±1.0°(c=1.007, MeOH) Anal. (C29H37NO6S) Calcd.(%): C, 66.01; H, 7.07; N, 2.65; S, 6.08. Found(%): C, 65.84; H, 6.93; N, 2.71; S, 6.06.

[0730] Compound Number I-221

[0731] 1 H-NMR(CDCl3)) δ: 1.05(1H, m), 1.17-1.30(2H, m), 1.39-1.48(2H, m), 1.54-1.80(4H, m), 1.98-2.20(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 3.81 (1H, m), 4.08(2H, s), 5.29-5.42(2H, m), 5.95(2H, s), 5.98(1H, d, J=7.5 Hz), 6.68-6.80(4H, m), 7.35(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3446, 3427, 1741, 1709, 1641, 1543, 1504, 1460, 1252, 1063 cm−1. [α]D24+62.7±1.0°(c=1.006, MeOH) Anal. (C27H31NO5S) Calcd.(%): C, 67.34; H, 6.49; N, 2.91; S, 6.66. Found(%): C, 67.12; H, 6.37; N, 2.98; S, 6.55.

[0732] Compound Number I-222

[0733] 1 H-NMR(CDCl3) δ: 1.08(1H, m), 1.24-1.28(2H, m), 1.41-1.45(2H, m), 1.56-1.78(4H, m), 1.97-2.20(5H, m), 2.14(3H, s), 2.33(2H, t, J=7.2 Hz), 2.51 (1H, m), 3.77(1H, m), 4.06(2H, s), 5.28-5.42(2H, m), 6.16(1H, d, J=7.2 Hz), 6.74 (1H, d, J=3.6 Hz), 6.96(1H, d, J=7.5 Hz), 7.24(1H, t, J=8.7 Hz), 7.35-7.38 (3H, m), 7.74(1H, br s). IR(KBr): 3309, 1707, 1672, 1614, 1547, 1523, 1489, 1441, 1371, 1319 cm−1. [α]D26+57.7±1.0°(c=1.012, MeOH) Anal. (C28H34N2O4S.0.4H2O) Calcd.(%): C, 67.01; H, 6.99; N, 5.58; S, 6.39. Found(%): C, 66.98; H, 6.72, N, 5.47; S, 6.27.

[0734] Compound Number I-223

[0735] 1 H-NMR(CDCl3)) δ: 1.05(1H, m), 1.22-1.28(2H, m), 1.42-1.46(2H, m), 1.55-1.75(4H, m), 2.02-2.22(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 2.99 (3H, s), 3.81(1H, m), 4.11(2H, s), 5.29-5.45(2H, m), 6.04(1H, d, J=7.2 Hz), 6.78 (1H, d, J=3.6 Hz), 7.04-7.06(2H, m), 7.16(1H, m), 7.25(1H, br s), 7.29(1H, t, J=7.8 Hz), 7.36 (1H, d, J=3.6 Hz). IR (CHCl3): 3512, 3444, 3427, 3371, 1709, 1639, 1608, 1545, 1508, 1475, 1458, 1389, 1335, 1151 cm−1. [α]D24+55.0±1.0°(c=1.003, MeOH) Anal. (C27H34N2O5S2.0.2H2O) Calcd.(%): C, 60.69; H, 6.49; N, 5.24; S, 12.00. Found(%): C, 60.70; H, 6.44; N, 5.15; S, 11.56.

[0736] Compound Number I-224

[0737] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.22-1.28(2H, m), 1.42-1.53(2H, m), 1.57-1.74(4H, m), 2.00-2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.81 (1H, m), 4.33(2H, s), 5.29-5.42(2H, m), 5.98(1H, d, J=7.8 Hz), 6.86, 6.88 and 7.14 (each 1H, each d, each J=3.6 Hz), 7.22-7.37(4H, m), 7.53-7.56(2H, m).

[0738] Compound Number I-225

[0739] 1 H-NMR (CDCl3)) δ: 1.05(1H, m), 1.17-1.30(2H, m), 1.39-1.48(2H, m), 1.54-1.81(4H, m), 1.98-2.20(5H, m), 2.35(2H, t, J=7.5 Hz), 2.51(1H, m), 3.81 (1H, m), 4.08(2H, s), 4.23-4.30(4H, m), 5.29-5.42(2H, m), 5.95(1H, d, J=7.2 Hz), 6.71-6.80(4H, m), 7.34(1H, d, J=3.6 Hz). IR(CHCl3): 3514, 3446, 3427, 1739, 1709, 1641, 1603, 1543, 1506, 1475, 1456, 1284, 1090 cm−1. [α]D24.5+58.9±1.0°(c=1.013, MeOH) Anal. (C28H33NO5S) Calcd.(%): C, 67.85; H, 6.71; N, 2.83; S, 6.47. Found(%): C, 68.01; H, 6.72; N, 2.97; S, 6.50.

[0740] Compound Number I-226

[0741] 1 H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.30(2H, m), 1.38-1.47(2H, m), 1.54-1.81 (4H, m), 1.98-2.20(5H, m), 2.31(3H, s), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 3.70(3H, s), 3.80(1H, m), 4.16(2H, s), 5.29-5.42(2H, m), 5.95 (1H, d, J=7.2 Hz), 6.78(1H, d, J=3.6 Hz), 6.96-7.11(3H, m), 7.37(1H, d, J=3.6 Hz). IR(CHCl3): 3514, 3446, 3427, 2669, 1709, 1641, 1543, 1506, 1473, 1458, 1259, 1011 cm−1. [α]D24+62.7±1.0°(c=1.009, MeOH) Anal. (C28H35NO4S) Calcd.(%): C, 69.82; H, 7.32; N, 2.91; S, 6.66. Found(%): C, 69.55; H, 7.27; N, 3.09; S, 6.55.

[0742] Compound Number I-227

[0743] 1 H-NMR(CDCl3) δ: 1.07(1H, m), 1.24-1.28(2H, m), 1.41-1.46(2H, m), 1.56-1.79(4H, m), 2.00-2.17(5H, m), 2.16(3H, s), 2.33(2H, t, J=7.5 Hz), 2.51 (1H, m), 3.79(1H, m), 4.08(2H, s), 5.28-5.42(2H, m), 6.05(1H, d, J=7.5 Hz), 6.75 (1H, d, J=3.6 Hz), 7.16(2H, d, J=8.1 Hz), 7.37(1H, d, J=3.6 Hz), 7.43 (2H, d, J=8.1 Hz), 7.53(1H, br s). IR(CHCl3): 3512, 3437, 1707, 1639, 1543, 1516, 1410 cm−1. [α]D24.5+60.7±1.0°(c=1.012, MeOH) Anal. (C28H34N2O4S.0.5H2O) Calcd.(%): C, 67.77; H, 7.00; N, 5.56; S, 6.37. Found(%): C, 66.84; H, 6.91; N, 5.56; S, 6.26.

[0744] Compound Number I-228

[0745] 1 H-NMR(CDCl3)) δ: 1.06(1H, m), 1.22-1.29(2H, m), 1.41-1.46(2H, m), 1.58-1.76 (4H, m), 2.01-2.17(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m), 2.99 (3H, s), 3.80(1H, m), 4.11(2H, s), 5.29-5.43(2H, m), 6.01(1H, d, J=7.5 Hz), 6.78(1H, d, J=3.6 Hz), 6.86(1H, br s), 7.17-7.23(4H, m), 7.36(1H, d, J=3.6 Hz). IR(CHCl3): 3510, 3444, 3427, 3371, 1709, 1639, 1543, 1510, 1456, 1389, 1338, 1155 cm−1. [α]D24.5+56.5±1.0°(c=0.953, MeOH) Anal. (C27H34N2O5S2.0.1H2O) Calcd.(%): C, 60.90; H, 6.47; N, 5.26; S, 12.04. Found(%): C, 61.06; H, 6.45; N, 5.29; S, 11.52.

[0746] Compound Number I-229

[0747] mp.103-105° C.; 1H-NMR(CDCl3) δ: 1.02 (1H, m), 1.15-1.27 (2H, m), 1.37-1.45(2H, m), 1.53-1.77(4H, m), 1.96-2.18(5H, m), 2.33 (2H, t, J=7.5 Hz), 2.49(1H, m), 3.79(1H, m), 4.40(2H, s), 5.27-5.39 (2H, m), 5.94(1H, d, J=7.8 Hz), 6.89(1H, d, J=3.9 Hz), 7.32-7.37(2H, m), 7.43-7.48 (3H, m), 7.84(1H, m), 8.08(1H, d, J=6.9 Hz), 8.15(1H, m). IR(CHCl3): 3514, 3444, 3427, 2667, 1739, 1709, 1643, 1543, 1506, 1458, 1444 cm−1. [α]D24.5+58.9±1.0°(c=1.006, MeOH) Anal. (C32H33NO3S2) Calcd.(%): C, 70.68; H, 6.12; N, 2.58; S, 11.79. Found(%): C, 70.52; H, 6.11; N, 2.67; S, 11.72.

[0748] Compound Number I-230

[0749] mp.86-87° C.; 1H-NMR(CDCl3) δ: 1.02(1H, m), 1.16-1.28(2H, m), 1.37-1.45 (2H, m), 1.54-1.77(4H, m), 1.97-2.17(5H, m), 2.32(2H, t, J=7.5 Hz), 2.49 (1H, m), 3.78(1H, m), 3.79 and 4.26(each 2H, each s), 5.27-5.39(2H, m), 5.93 (1H, d, J=7.2 Hz), 6.78(1H, d, J=3.9 Hz), 7.18(1H, d, J=7.2 Hz), 7.29 (1H, m), 7.34-7.40(3H, m), 7.52(1H, d, J=7.2 Hz), 7.72(1H, d, J=7.5 Hz), 7.78(1H, d, J=7.2 Hz). IR(CHCl3): 3514, 3446, 3427, 2669, 1709, 1641, 1543, 1506, 1456 cm−1. [α]D24.5+59.2±1.0°(c=1.006, MeOH) Anal. (C33H35NO3S) Calcd.(%): C, 75.40; H, 6.71; N, 2.66; S, 6.10. Found(%): C, 75.33; H, 6.73; N, 2.75; S, 6.06.

[0750] Compound Number I-231

[0751] 1 H-NMR (CHCl3) δ: 1.04(1H, m), 1.16-1.30(2H, m), 1.38-1.46(2H, m), 1.54-1.81(4H, m), 1.98-2.16(5H, m), 2.21 and 2.50(each 3H, each s), 2.34 (2H, t, J=7.2 Hz), 2.51(1H, m), 3.66(3H, s), 3.80(1H, m), 4.13(2H, s), 5.29-5.42 (2H, m), 5.93(1H, d, J=6.9 Hz), 6.78(1H, d, J=3.6 Hz), 6.89 and 6.96 (each 1H, each d, each J=7.5 Hz), 7.36(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3446, 3425, 2669, 1709, 1641, 1545, 1506, 1458, 1263, 1084, 1009 cm−1. [α]D24+61.8±1.0°(c=1.006, MeOH) Anal. (C29H37NO4S.0.2H2O) Calcd.(%): C, 69.76; H, 7.55; N, 2.81; S, 6.42. Found(%): C, 69.80; H, 7.59; N, 2.97; S, 6.34.

[0752] Compound Number I-232

[0753] 1 H-NMR(CDCl3) δ: 1.02(1H, m), 1.16-1.27(2H, m), 1.37-1.45(2H, m), 1.53-1.77(4H, m), 1.96-2.15(5H, m), 2.33(2H, t, J=7.5 Hz), 2.50(1H, m), 3.79 (1H, m), 4.50(2H, s), 5.27-5.40(2H, m), 5.94(1H, d, J=7.5 Hz), 6.88(1H, d, J=3.9 Hz), 7.29-7.38(4H, m), 7.47(1H, m), 7.58(1H, d, J=8.4 Hz), 7.86(1H, m), 7.95(1H, d, J=7.8 Hz). IR(CHCl3): 3512, 3444, 3427, 2669, 1739, 1708, 1641, 1543, 1506, 1475, 1452, 1423 cm−1. [α]D24+58.5±1.0°(c=1.006, MeOH) Anal. (C32H33NO4S.0.2H2O) Calcd.(%): C, 72.34; H, 6.34; N, 2.64; S, 6.04. Found(%): C, 72.36; H, 6.16; N, 2.72; S, 5.94.

[0754] Compound Number I-233

[0755] mp.125-126° C.; 1H-NMR(CDCl3) δ: 1.05(1H, m), 1.18-1.28(2H, m), 1.41-1.45 (2H, m), 1.57-1.78(4H, m), 2.00-2.20 (5H, m), 2.33(2H, t, J=7.4 Hz), 2.51 (1H, s), 3.80(1H, m),4.05 (2H, s), 5.28-5.42 (2H, m), 5.98(1H, d, J=6.6 Hz), 6.76 (1H, d, J=3.6 Hz), 6.80 and 7.09(each 2H, each d, J=8.4 Hz), 7.37(1H, d, J=3.6 Hz). IR(KBr): 3354, 3132, 2688, 1703, 1616, 1599, 1549, 1514, 1458, 1250 cm−1. [α]D25+67.7±1.1°(c=1.001, MeOH) Anal. (C26H31NO4S) Calcd.(%): C, 68.85; H, 6.89; N, 3.09; S, 7.07. Found(%): C, 69.12; H, 6.95; N, 3.10; S, 7.12.

[0756] Compound Number II-1

[0757] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.41(14H, m), 4.20(1H, m), 5.35-5.47(2H, m), 6.16(1H, d, J=8.7 Hz), 6.33 and 7.16(each 2H, each t, each J=2.4 Hz), 7.30 and 7.56 (each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3515, 3446, 3144, 3100, 1708, 1658, 1529, 1504, 1456, 1385, 1167 cm−1. [α]D 26.5+54.1±0.9°(c=1.004, MeOH) Anal. (C25H32N2O5S2.0.2H2O) Calcd.(%): C, 59.08; H, 6.43; N, 5.51; S, 12.62. Found(%): C, 59.12; H, 6.36; N, 5.57; S, 12.59.

[0758] Compound Number II-6

[0759] 1 H-NMR(CDCl3) δ: 0.98(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, each s), 1.54-2.48(14H, m), 4.30(1H, m), 5.35-5.52(2H, m), 6.26 (1H, d, J=8.7 Hz), 6.38 and 7.13 (each 2H, each t, J=2.1 Hz), 7.44 and 7.79 (each 2H, each d, each J=8.4 Hz). IR(CHCl3): 3453, 2662, 1739, 1708, 1652, 1609, 1500, 1333 cm−1. [α]D22+65.2±1.1°(c=1.006, MeOH) Anal. (C27H34N2O3.0.3H2O) Calcd.(%): C, 73.71; H, 7.93; N, 6.37. Found(%): C, 73.85; H, 7.88; N, 6.37.

[0760] Compound Number II-7

[0761] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.22 (each 3H, each s), 1.52-2.42(14H, m), 4.25(1H, m), 5.34-5.51(2H, m), 6.35(1H, d, J=8.7 Hz), 7.07-7.15(3H, m), 7.21-7.26(2H, m), 7.73 and 7.77(each 2H, each d, each J=8.7 Hz). IR(CHCl3): 3518, 3446, 3365, 3249, 2673, 1709, 1655, 1516, 1348, 1167 cm−1. [α]D21.5+56.1±0.9°(c=1.000, MeOH) Anal. (C29H36N2O5S.0.6H2O) Calcd.(%): C, 65.05; H, 7.00; N, 5.23; S, 5.99. Found(%): C, 65.07; H, 6.94; N, 5.37; S, 6.03.

[0762] Compound Number II-8

[0763] 1 H-NMR(CDCl3) δ: 0.89(1H, d, J=10.2 Hz), 1.05 and 1.19(each 3H, each s), 1.50-2.44(14H, m), 4.15(1H, m), 5.31-5.50(2H, m), 6.31 (1H, d, J=8.1 Hz), 7.00(1H, d, J=1.8 Hz), 7.42-7.47(2H, m), 7.54 (1H, d, J=1.8 Hz), 7.56(1H, m), 7.76-7.79(2H, m), 8.29(1H, s). IR (CHCl3): 3509, 3446, 3360, 3108, 1708, 1639, 1515, 1448, 1330, 1164 cm−1. [α]D20+39.0±0.8°(c=1.006, MeOH) Anal. (C27H34N2O5S2.0.2H2O) Calcd.(%): C, 60.09; H, 6.54; N, 5.19; S,11.88. Found(%): C, 60.07; H, 6.48; N, 5.31; S,11.92.

[0764] Compound Number II-9

[0765] 1 H-NMR(CDCl3) δ: 0.73(1H, d, J=10.2 Hz), 1.06 and 1.16(each 3H, each s), 1.43-2.36(14H, m), 4.07(1H, m), 5.28-5.49(2H, m), 6.37 (1H, d, J=8.7 Hz), 7.28 and 7.33(each 1H, each d, each J=1.8 Hz), 7.38-7.43 (2H, m), 7.50(1H, m), 7.96-7.99(2H, m). IR(CHCl3): 3440, 3254, 3096, 3062, 1708, 1643, 1560, 1530, 1298 cm−1. [α]D20+49.0±0.9°(c=1.008, MeOH) Anal. (C28H34N2O4S.0.4H2O) Calcd.(%): C, 67.01; H, 6.99; N, 5.58; S,6.39. Found(%): C, 66.96; H, 7.04; N, 5.67; S,6.32.

[0766] Compound Number II-10

[0767] 1 H-NMR(CDCl3) δ: 0.96(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s), 1.52-2.44(14H, m), 4.26(1H, m), 5.33-5.49(2H, m), 6.26(1H, d, J=8.4 Hz), 6.31 and 7.15(each 2H, each t, each J=2.1 Hz), 7.81 and 7.89 (each 2H, each d, each J=8.4 Hz). IR(CHCl3): 3514, 3446, 3144, 1708, 1663, 1514, 1377, 1173 cm−1. [α]D22+64.1±0.9°(c=1.000, MeOH) Anal. (C27H34N2O5S.0.2H2O) Calcd.(%): C, 64.57; H, 6.90; N, 5.58; S, 6.38. Found(%): C, 64.50; H, 6.97; N, 5.71; S, 6.28.

[0768] Compound Number II-11

[0769] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.43(14H, m), 4.12(2H, s), 4.22(1H, m), 5.33-5.49(2H, m), 6.06(1H, d, J=8.7 Hz), 7.04(1H, d, J=1.2 Hz), 7.22-7.34(2H, m), 7.63 (1H, d, J=1.2 Hz). IR(CHCl3): 3517, 3451, 3087, 3065, 2670, 1708, 1708, 1647, 1549, 1508 cm−1. [α]D21.5+41.9±0.8°(c=1.015, MeOH) Anal. (C28H35NO3S) Calcd.(%): C, 72.22; H, 7.58; N, 3.01; S,6.89. Found(%): C, 72.07; H, 7.57; N, 3.21; S,6.77.

[0770] Compound Number II-12

[0771] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.21(each 3H, each s), 1.50-2.44 (14H, m), 4.24(1H, m), 5.32-5.48(2H, m), 6.24(1H, d, J=8.7 Hz), 7.17 and 7.60(each 2H, each d, each J=8.7 Hz), 7.41-7.46 (2H, m), 7.54(1H, m), 7.80-7.84(2H, m). IR(CHCl3): 3510, 3451, 3371, 3139, 1709, 1647, 1609, 1496, 1163 cm−1. [α]D22.5+47.1±0.9°(c=1.006, MeOH) Anal. (C29H36N2O5S.0.4H2O) Calcd.(%): C, 65.49; H, 6.97; N, 5.27; S, 6.03. Found(%): C, 65.51; H, 6.87; N, 5.39; S, 5.89.

[0772] Compound Number II-14

[0773] 1 H-NMR(CHCl3) δ: 0.92(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s), 1.53-2.47(14H, m), 4.17(1H, m), 5.35-5.55(2H, m), 6.35 and 7.17 (each 2H, each t, each J=2.1 Hz), 6.38(1H, d, J=8.7 Hz), 8.09 and 8.17 (each 1H, each d, each J=1.5 Hz). IR(CHCl3): 3510, 3409, 3144, 3107, 1727, 1.709, 1657, 1538, 1503, 1456, 1387, 1166 cm−1. [α]D25+46.1±0.9°(c=1.005, MeOH) Anal. (C25H32N2O5S2.0.2H2O) Calcd.(%): C, 59.08; H, 6.43; N, 5.51; S, 12.62. Found(%): C, 59.10; H, 6.45; N, 5.69; S, 12.58.

[0774] Compound Number II-15

[0775] mp.119-121° C. 1H-NMR(CDCl3) δ: 0.97(1H, d, J=10.2 Hz), 1.11 and 1.24(each 3H, each s), 1.53-2.49(14H, m), 4.29(1H, m), 5.39-5.57 (2H, m), 6.37 and 7.22(each 2H, each t, each J=2.1 Hz), 7.13 (1H, d, J=8.4 Hz), 7.50 and 7.93(each 1H, each d, each J=3.9 Hz). IR(Nujol): 3365, 3145, 3100, 1739, 1621, 1548, 1405, 1367, 1187 cm−1. [α]D26.5+45.5±0.8°(c=1.012, MeOH) Anal. (C25H32N2O5S2) Calcd.(%): C, 59.74; H, 6.02; N, 5.57; S, 12.76. Found(%): C, 59.56; H, 6.33; N, 5.64; S, 12.76.

[0776] Compound Number II-17

[0777] 1 H-NMR(CDCl3) δ: 0.96 (1H, d, J=10.5 Hz), 1.11 and 1.23(each 3H, each s), 1.54-2.49(14H, m), 4.25(1H, m), 5.35-5.56(2H, m), 6.33 (2H, t, J=2.4 Hz), 6.56(1H, d, J=7.8 Hz), 7.17(2H, t, J=2.4 Hz), 7.58(1H, t, J=7.8 Hz), 7.93(1H, m), 8.04(1H, d, J=7.8 Hz), 8.24(1H, m). IR (CHCl3): 3513, 3389, 3144, 2669, 1726, 1709, 1659, 1515, 1470, 1455, 1375 cm−1. [α]D25+54.0±0.9°(c=1.008, MeOH) Anal. (C27H34N2O5S.0.2H2O) Calcd.(%): C, 64.46; H, 6.90; N, 5.53; S,6.38. Found(%): C, 64.45; H, 6.89; N, 5.75; S,6.42.

[0778] Compound Number II-18

[0779] 1 H-NMR(CDCl3) δ: 0.96(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s), 1.52-2.42(14H, m), 2.29(3H, t), 4.26(1H, m), 5.35-5.49(2H, m), 5.96(1H, brs), 6.19(1H, t, J=3.2 Hz), 6.26(1H, d, J=8.1 Hz), 7.25 (1H, m), 7.81(4H, s). IR(CHCl3): 3511, 3446, 3152, 1708, 1662, 1514, 1485, 1368, 1164 cm−1. [α]D27+59.4±1.0°(c=1.006, MeOH) Anal. (C28H36N2O5S) Calcd.(%): C, 65.60; H, 7.08; N, 5.46; S,6.25. Found(%): C, 65.41; H, 7.00; N, 5.67; S,6.24.

[0780] Compound Number II-19

[0781] 1 H-NMR(CDCl3) δ: 0.97(1H, d, J=10.5 Hz), 1.03 and 1.22(each 3H, each s), 1.452-2.46 (14H, m), 4.26(1H, m), 5.33-5.50(2H, m), 6.20 (2H, t, J=2.1 Hz), 6.22(1H, d, J=8.1 Hz), 6.68(2H, t, J=2.1 Hz), 7.15 and 7.67 (each 2H, each d, each J=8.1 Hz). IR(CHCl3): 3511, 3452, 3103, 2666, 1709, 1652, 1523, 1496 cm−1. [α]D23+57.7±1.0°(c=1.010, MeOH) Anal. (C28H36N2O3.0.1H2O) Calcd.(%): C, 74.67; H, 8.10; N, 6.22. Found(%): C, 74.69; H, 8.21; N, 6.38.

[0782] Compound Number II-20

[0783] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.06 and 1.20(each 3H, each s), 1.49-2.40(14H, m), 4.21(1H, m), 5.31-5.45(2H, m), 6.19(1H, d, J=8.4 Hz), 6.88(1H, d, J=3.6 Hz), 7.22-7.35(2H, m), 7.52-7.55(2H, m), 7.74 and 7.91(each 2H, each d, each J=8.4 Hz), 7.98(1H, d, J=8.4 Hz). IR(CHCl3): 3481, 3440, 3145, 3116, 2661, 1709, 1660, 1516, 1485, 1446, 1377, 1261, 1178, 1130 cm−1. [α]D26+56.6±1.0°(c=1.000, MeOH) Anal. (C31H36N2O5S.0.1H2O) Calcd.(%): C, 67.64; H, 6.63; N, 5.09; S, 5.82. Found(%): C, 67.68; H, 6.72; N, 5.35; S, 5.73.

[0784] Compound Number II-21

[0785] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.09 and 1.22 (each 3H, each s), 1.52-2.45(14H, m), 4.24(1H, m), 4.63(2H, s), 5.34-5.50(2H, m), 6.25-6.27(2H, m), 6.40(1H, d, J=8.4 Hz), 7.25(1H, dd, J=1.8 and 3.0 Hz), 7.80 and 7.85(each 2H, each d, each J=8.7 Hz). IR(CHCl3): 3581, 3518, 3445, 3149, 2666, 1709, 1661, 1515, 1472, 1371, 1182, 1150 cm−1. [α]D27+58.1±1.0°(c=1.007, MeOH) Anal. (C28H36N2O6S) Calcd.(%): C, 63.61; H, 6.86; N, 5.30; S, 6.07. Found(%): C, 63.50; H, 6.84; N, 5.44; S, 5.89.

[0786] Compound Number II-31

[0787] mp.98-100° C. 1H-NMR(CDCl3)) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.43(14H, m), 4.13(2H, s), 4.20 (1H, m), 5.33-5.49(2H, m), 5.97(1H, d, J=8.4 Hz), 6.77(1H, m), 7.21-7.35(6H, m). IR(KBr): 3407, 2674, 1703, 1630, 1511 cm−1. [α]D24+46.8±0.9°(c=1.006, MeOH) Anal. (C28H35NO3S) Calcd.(%): C, 72.22; H, 7.58; N, 3.01; S, 6.89. Found(%): C, 72.04; H, 7.36; N, 3.27; S, 6.91.

[0788] Compound Number II-37

[0789] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.41(14H, m), 4.20(1H, m), 5.39-5.47(2H, m), 6.19(1H, d, J=8.4 Hz), 7.35(1H, d, J=3.9 Hz), 7.51-7.64(4H, m), 7.98(2H, m). IR(CHCl3): 3516, 3446, 2667, 1709, 1657, 1529, 1504, 1327, 1157 cm−1. [α]D20+55.6°±1.0°(c=1.004, MeOH) Anal. (C27H3NO5S.0.2H2O) Calcd.(%) C, 62.45; H, 6.48; N, 2.70; S, 12.35. Found(%): C, 62.46; H, 6.40; N, 2.75; S, 12.19.

[0790] Compound Number II-47

[0791] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.41(14H, m), 4.21(1H, m), 5.34-5.48(2H, m), 6.21(1H, d, J=8.4 Hz), 7.36 and 7.63(each 1H, each d, each J=3.9 Hz), 7.70(1H, dd, J=1.5 and 5.1 Hz), 7.75(1H, dd, J=1.5 and 3.9 Hz). IR(CHCl3): 3516, 3446, 3097, 1708, 1656, 1529, 1504, 1337, 1153 cm−1. [α]D25+54.1±0.9°(c=1.000, MeOH) Anal. (C25H31NO5S3) Calcd.(%): C, 57.56; H, 5.99; N, 2.68; S, 18.44. Found(%): C, 57.33; H, 5.95; N, 2.68; S, 18.38.

[0792] Compound Number II-55

[0793] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.22(each 3H, each s), 1.50-2.41(14H, m), 2.39(3H, d, J=0.6 Hz), 4.21(1H, m), 5.35-5.48(2H, m), 5.99(1H, m), 6.15(1H, d, J=8.7 Hz), 6.20(1H, t, J=3.3 Hz), 7.18(1H, dd, J=1.8 and 3.3 Hz), 7.31 and 7.54(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3511, 3446, 3150, 3101, 1708, 1658, 1529, 1504, 1375, 1183, 1160 cm−1. [α]D23+50.3±0.9°(c=1.007, MeOH) Anal. (C26H34N2O5S2.0.2H2O) Calcd.(%): C, 59.79; H, 6.64; N, 5.36; S, 12.28. Found(%): C, 59.72; H, 6.61; N, 5.51; S, 12.37.

[0794] Compound Number II-59

[0795] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.07 and 1.21(each 3H, each s), 1.49-2.41(14H, m), 4.19(1H, m), 5.33-5.47(2H, m), 5.99(1H, d, J=8.7 Hz), 7.01(1H, dd, J=3.6 and 5.4 Hz), 7.04 and 7.28(each 1H, each d, each J=3.6 Hz), 7.29(1H, dd, J=1.2 and 3.6 Hz), 7.43(1H, dd, J=1.2 and 5.4 Hz). IR(CHCl3): 3518, 3449, 3430, 2672, 1708, 1646, 1530, 1500, 1421 cm−1. [α]D25.5+45.9±0.9°(c=1.010, MeOH) Anal. (C25H31NO3S3) Calcd.(%): C, 61.32; H, 6.38; N, 2.86; S, 19.64. Found(%): C, 61.17; H, 6.42; N, 3.00; S, 19.80.

[0796] Compound Number II-60

[0797] 1 H-NMR (CHCl3) δ: 0.96 (1H,d,J=10.2 Hz),1.10 and 1.22 (each 3H, each s), 1.51-1.79 (3H, m), 1.83-2.44 (11H, m), 4.26 (1H, m), 5.33-5.49 (2H, m), 6.21 (1H, d, J=8.7 Hz), 7.25 (2H, d, J=9.0 Hz), 7.34-7.47 (5H,m), 7.60 (2H, d, J=9.0 Hz) IR (CHCl3): 3453, 3062, 3029, 3014, 2925, 2870, 1739, 1708, 1651, 1595, 1583, 1557, 1515, 1481cm−1. [α]D22+61.0°(c=1.01,CH3OH) Anal. (C29H35NO3S.0.1H2O) Calcd.(%): C, 72.65; H, 7.48; N, 2.92; S, 6.69. Found (%): C, 72.50; H, 7.45; N, 3.19; S,6.69.

[0798] Compound Number II-81

[0799] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.07 and 1.21(each 3H, each s), 1.49-2.41(14H, m), 2.46(3H, d, J=1.2 Hz), 4.18(1H, m), 5.33-5.47(2H, m), 5.99(1H, d, J=8.4 Hz), 6.66(1H, m), 6.99(1H, d, J=3.9 Hz), 7.10(1H, d, J=3.3 Hz), 7.26(1H, d, J=3.9 Hz). IR(CHCl3): 3509, 3449, 2671, 1708, 1645, 1530, 1500, 1420 cm−1. [α]D25.5+43.5±0.8°(c=1.002, MeOH) Anal. (C26H33NO3S3) Calcd.(%): C, 61.99; H, 6.60; N, 2.78; S, 19.10. Found(%): C, 61.77; Hl, 6.68; N, 2.83; S, 18.91.

[0800] Compound Number II-82

[0801] mp.118-120° C. 1H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s), 1.51-2.42(14H, m), 2.53(3H, d, J=0.9 Hz), 4.20 (1H, m), 5.35-5.48(2H, m), 6.17(1H, d, J=8.7 Hz), 6.77(1H, m), 7.34 (1H, d, J=3.9 Hz), 7.57(1H, d, J=3.6 Hz), 7.60(1H, d, J=3.9 Hz). IR (Nujol): 3399, 3082, 1733, 1613, 1543, 1328, 1318, 1151 cm−1. [α]D25.5+54.0±0.9°(c=1.012, MeOH) Anal. (C26H33NO5S3) Calcd.(%): C, 58.29; H, 6.21; N, 2.61; S, 17.95. Found(%): C, 58.08; H, 6.18; N, 2.73; S, 17.66.

[0802] Compound Number II-88

[0803] mp.91-92° C. 1H-NMR(CDCl3) δ: 0.95(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s),1.51-2.44(14H, m), 4.16(2H, s), 4.20 (1H, m), 5.34-5.49(2H, m), 5.99(1H, d, J=8.7 Hz), 6.79(1H, d, J=3.9 Hz), 6.96 (1H, dd, J=1.2 and 4.8 Hz), 7.05(1H, m), 7.28(1H, dd, J=3.0 and 4.8 Hz), 7.32(1H, d, J=3.9 Hz). IR(Nujol): 3408, 2677, 1703, 1626, 1541, 1514, 1246 cm−1. [α]D26+43.8±0.8°(c=1.005, MeOH) Anal. (C26H33NO3S2) Calcd.(%): C, 66.21; H, 7.05; N, 2.97; S, 13.60. Found(%): C, 66.00; H, 7.81; N, 3.11; S, 13.69.

[0804] Compound Number II-92

[0805] mp.165-166° C. 1H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.20(each 3H, each s), 1.50-2.45(14H, m), 4.17(1H, m), 5.33-5.51(2H, m), 6.04(1H, d, J=8.4 Hz), 6.51(1H, dd, J=1.5 and 3.3 Hz), 7.15(1H, dd, J=2.4 and 3.3 Hz), 7.52-7.57(2H, m), 7.65(1H, m), 7.74(1H, dd, J=1.8 and 2.1 Hz), 7.89-7.93(1H, m). IR(CHCl3): 3510, 3449, 3144, 1733, 1708, 1650, 1570, 1507, 1384, 1185, 1176 cm−1. [α]D24+33.8±0.7°(c=1.011, MeOH) Anal. (C27H34N2O5S) Calcd.(%): C, 65.04; H, 6.87; N, 5.62; S, 6.43. Found(%): C, 64.95; H, 6.68; N, 5.69; S, 6.40.

[0806] Compound Number II-93

[0807] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 150-2.46(14H, m), 4.19(1H, m), 5.33-5.50(2H, m), 6.03(1H, d, J=8.7 Hz), 6.52(1H, dd, J=1.5 and 3.3 Hz), 7.11(1H, dd, J=3.9 and 4.8 Hz), 7.17(1H, dd, J=2.1 and 3.3 Hz), 7.70-7.72(2H, m), 7.74(1H, dd, J=1.2 and 3.9 Hz). IR(CHCl3): 3510, 3448, 3143, 2666, 1733, 1708, 1650, 1572, 1507, 1387, 1179 cm−1. [α]D24+39.1°±0.8° (c=1.003, MeOH) Anal. (C25H32N2O5S2) Calcd.(%): C, 59.50; H, 6.39; N, 5.55; S, 12.71. Found(%): C, 59.49; H, 6.46; N, 5.47; S, 12.70.

[0808] Compound Number II-94

[0809] mp.132-133° C. 300 MHz 1H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.54-2.44(14H, m), 4.19(1H, m), 5.33-5.50 (2H, m), 6.03(1H, d, J=8.7 Hz), 6.52(1H, dd, J=1.5 and 3.3 Hz), 7.11(1H, dd, J=3.9 and 4.8 Hz), 7.17(1H, dd, J=2.1 and 3.3 Hz), 7.70-7.72(2H, m), 7.74(1H, dd, J=1.5 and 3.9 Hz). IR(CHCl3): 3510, 3448, 3143, 3099, 1733, 1708, 1650, 1572, 1507, 1473, 1387, 1179 cm−1. [α]D24+39.1±0.8°(c=1.003, MeOH) Anal. (C25H32N2O5S2) Calcd.(%): C, 59.50; H, 6.39; N, 5.55; S, 12.71. Found(%): C, 59.49; H, 6.46; N, 5.47; S, 12.70.

[0810] Compound Number II-98

[0811] mp.138-139° C. 1H-NMR(CDCl3) δ: 0.97(1H, d, J=10.2 Hz), 1.13 and 1.24(each 3H, each s), 1.50-2.47(14H, m), 4.24(1H, m), 5.36-5.52 (2H, m), 6.06(1H, d, J=8.4 Hz), 6.98(1H, d, J=3.9 Hz), 6.99 and 7.05 (each 1H, each d, each J=16.2 Hz), 7.28-7.34(3H, m), 7.37 (1H, d, J=3.9 Hz). IR(CHCl3): 3518, 3449, 3431, 2665, 1708, 1642, 1538, 1519, 1500 cm−1. [α]D24+49.1±0.9°(c=1.014, MeOH) Anal. (C27H33NO3S2) Calcd.(%): C, 67.05; H, 6.88; N, 2.90; S, 13.26. Found(%): C, 67.94; H, 6.86; N, 2.99; S, 13.23.

[0812] Compound Number II-99

[0813] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=9.9 Hz), 1.07 and 1.22 (each 3H, each s), 1.50-2.44(14H, m), 4.20(1H, m), 5.30-5.51(2H, m), 5.97(1H, d, J=9.0 Hz), 6.58(2H, s), 6.95(1H, d, J=3.9 Hz), 7.02(1H, dd, J=1.5 and 4.8 Hz), 7.25-7.31(2H, m), 7.31(1H, d, J=3.9 Hz). IR(CHCl3): 3517, 3449, 3430, 2664, 1708, 1642, 1536, 1519, 1501 cm−1. [α]D24+38.6±0.8°(c=1.006, MeOH) Anal. (C27H33NO3S2.0.2H2O) Calcd.(%): C, 66.55; H, 6.91; N, 2.87; S, 13.16. Found(%): C, 66.52; H, 6.81; N, 3.11; S, 12.93.

[0814] Compound Number II-100

[0815] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s), 1.50-2.39(14H, m), 2.44(3H, d, J=0.9 Hz), 4.20(1H, m), 5.34-5.49(2H, m), 5.98(1H, d, J=8.7 Hz), 6.70(1H, m), 7.06(1H, d, J=3.9 Hz), 7.10(1H, d, J=1.8 Hz), 7.30(1H, d, J=3.9 Hz). IR(CHCl3): 3518, 3450, 3430, 3110, 2669, 1740, 1708, 1645, 1530, 1499, 1420 cm−1. [α]D24+46.0±0.9°(c=0.968, MeOH) Anal. (C26H33NO3S3) Calcd.(%): C, 61.99; H, 6.60; N, 2.78; S, 19.10. Found(%): C, 61.99; H, 6.61; N, 2.87; S, 19.18.

[0816] Compound Number II-101

[0817] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s), 1.51-2.42(14H, m), 2.47(3H, d, J=0.9 Hz), 4.21(1H, m), 5.35-5.49(2H, m), 6.18(1H, d, J=8.7 Hz), 7.04(1H, m), 7.36 and 7.60(each 1H, each d, each J=3.9 Hz), 7.91(1H, d, J=1.5 Hz). IR(CHCl3): 3510, 3447, 3115, 2670, 1708, 1656, 1529, 1504, 1443, 1329, 1156, 1143 cm−1. [α]D24+53.8±0.9°(c=1.008, MeOH) Anal. (C26H33NO5S3) Calcd.(%): C, 58.29; H, 6.21; N, 2.61; S, 17.96. Found(%): C, 58.07; H, 6.05; N, 2.69; S, 17.94.

[0818] Compound Number II-102

[0819] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s), 1.50-2.45(14H, m), 4.22(1H, m), 5.35-5.49(2H, m), 6.04(1H, d, J=8.7 Hz), 6.52 and 6.69(each 1H, each d, each J=12.0 Hz), 6.99 (1H, dd, J=3.6 and 5.1 Hz), 7.07(1H, d, J=3.9 Hz), 7.13(1H, d, J=3.9 Hz), 7.27(1H, dd, J=0.9 and 5.1 Hz) 7.36(1H, d, J=3.9 Hz). IR (CHCl3): 3510, 3449, 3430, 2664, 1708, 1643, 1536, 1501 cm−1. [α]D24+40.3±0.8°(c=1.011, MeOH) Anal. (C27H33NO3S2.0.3H2O) Calcd.(%): C, 66.31; H, 6.92; N, 2.86; S, 13.11. Found(%): C, 66.29; H, 6.81; N, 3.07; S, 13.13.

[0820] Compound Number II-103

[0821] mp.117-118° C. 1H-NMR(CDCl3) δ: 0.97(1H, d, J=10.2 Hz), 1.13 and 1.24(each 3H, each s), 1.50-2.47(14H, m), 4.24(1H, m), 5.36-5.52(2H, m), 6.06(1H, d, J=8.7 Hz), 6.97 and 7.15(each 1H, each d, each J=15.9 Hz), 6.98(1H, d, J=3.9 Hz), 7.01(1H, dd, J=3.3 and 4.8 Hz), 7.09 (1H, d, J=3.3 Hz), 7.23(1H, d, J=4.8 Hz), 7.36(1H, d, J=3.9 Hz). IR(CHCl3): 3517, 3450, 2670, 1738, 1708, 1641, 1537, 1518, 1500 cm−1. [α]D24+55.7±1.0°(c=1.001, MeOH) Anal. (C27H33NO3S2) Calcd.(%): C, 67.05; H, 6.88; N, 2.90; S, 13.26. Found(%): C, 66.91; H, 6.83; N, 2.97; S, 13.13.

[0822] Compound Number II-107

[0823] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s), 1.51-2.44(14H, m), 4.20(1H, m), 5.34-5.50(2H, m), 6.22 and 6.23(total 1H, each d, J=8.1 and 8.7 Hz), 7.12(1H, dd, J=3.9 and 5.1 Hz), 7.44(2H, m), 7.60(1H, m), 7.69(1H, m). IR(CHCl3): 3509, 3447, 3092, 1708, 1653, 1530, 1503 cm−1. [α]D23+49.3±0.9°(c=1.002, MeOH) Anal. (C25H31NO4S3.0.4H2O) Calcd.(%): C, 58.54; H, 6.25; N, 2.73; S, 18.75. Found(%): C, 58.62; H, 6.16; N, 2.88; S, 18.72.

[0824] Compound Number II-108

[0825] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.10(total 3H, each s), 1.22 and 1.23(total 3H, each s), 1.51-2.44(14H, m), 2.52 and 2.53(total 3H, each d, J=0.6 Hz), 4.20(1H, m), 5.35-5.50(2H, m), 6.23 and 6.24(total 1H, each d, J=8.7 and 8.4 Hz), 6.77(1H, m), 7.39-7.46 (3H, m). IR (CHCl3): 3510, 3447, 3429, 3093, 2665, 1708, 1652, 1530, 1502, 1437 cm−1. [α]D23+47.4±0.9°(c=1.008, MeOH) Anal. (C26H33NO4S3.0.3H2O) Calcd.(%): C, 59.47; H, 6.45; N, 2.67; S, 18.32. Found(%): C, 59.59; H, 6.16; N, 2.76; S, 18.11.

[0826] Compound Number II-112

[0827] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s), 1.51-2.43(14H, m), 3.38(3H, s), 4.18(1H, m), 5.33-5.50(2H, m), 5.83(1H, d, J=8.7 Hz), 6.16(1H, d, J=3.9 Hz), 7.14(1H, m), 7.21-7.27 (4H, m), 7.33-7.39(2H, m). IR(CHCl3): 3514, 3450, 2661, 1739, 1709, 1628, 1597, 1495, 1479, 1415, 1132 cm−1. [α]D23.5+50.8°±0.9° (c=1.005, MeOH) Anal. (C28H36N2O3S.0.2H2O) Calcd.(%): C, 69.45; H, 7.58; N, 5.78; S, 6.62. Found(%): C, 69.45; H, 7.39; N, 5.99; S, 6.65.

[0828] Compound Number II-113

[0829] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s), 1.50-2.44(14H, m), 2.31(3H, s), 4.22(1H, m), 5.35-5.49(2H, m), 6.01(1H, d, J=8.7 Hz), 7.03-7.21(4H, m), 7.38(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3448, 3429, 1739, 1709, 1647, 1529, 1500, 1473, 1421 cm−1. [α]D20+46.2°±1.0°(c=1.003, MeOH) Anal. (C28H35NO3S2.0.2H2O) Calcd.(%): C, 67.08; H, 7.12; N, 2.79; S, 12.79. Found(%): C, 67.12; H, 7.04; N, 2.94; S, 12.88.

[0830] Compound Number II-114

[0831] mp.112-115° C. 1H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.39(14H, m), 2.42(3H, s), 4.20(1H, m), 5.34-5.47(2H, m), 6.17(1H, d, J=8.7 Hz), 7.34(1H, d, J=3.9 Hz), 7.41 (2H, m), 7.59(1H, d, J=3.9 Hz), 7.78(2H, m). IR(CHCl3): 3516, 3446, 1739, 1707, 1655, 1529, 1504, 1331, 1151 cm−1. [α]D20+53.0°±0.9°(c=1.002, MeOH) Anal. (C28H35NO5S2.0.2H2O) Calcd.(%): C, 63.06; H, 6.69; N, 2.63; S, 12.02. Found(%): C, 63.07; H, 6.62; N, 2.73; S, 12.04.

[0832] Compound Number II-115

[0833] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s), 1.50-2.44(14H, m), 3.77(3H, s), 4.22(1H, m), 5.35-5.49(2H, m), 6.04(1H, d, J=8.7 Hz), 6.74-6.89(3H, m), 7.17-7.23(2H, m), 7.40 (1H, d, J=3.9 Hz). IR(CHCl3): 3514, 3448, 3431, 1739, 1707, 1649, 1529, 1500, 1477 cm−1. [α]D20+45.8°±0.9°(c=1.011, MeOH) Anal. (C28H35NO4S2.0.3H2O) Calcd.(%): C, 64.78; H, 6.91; N, 2.70; S, 12.35. Found(%): C, 64.62; H, 6.83; N, 2.85; S, 12.65.

[0834] Compound Number II-116

[0835] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.41(14H, m), 3.86(3H, s), 4.20(1H, m), 5.34-5.47 (2H, m), 6.17(1H, d, J=8.7 Hz), 7.12(1H, m), 7.35(1H, d, J=3.9 Hz), 7.40-7.48(2H, m), 7.56(1H, m), 7.60(1H, d, J=3.9 Hz). IR(CHCl3): 3514, 3446, 2667, 1707, 1657, 1599, 1529, 1504, 1481, 1329, 1252, 1151 cm−1. [α]D20+52.6°±0.9°(c=1.011, MeOH) Anal. (C28H35NO6S2.0.2H2O) Calcd.(%): C, 61.22; H, 6.50; N, 2.55; S, 11.67. Found(%): C, 61.10; H, 6.36; N, 2.65; S, 11.73.

[0836] Compound Number II-117

[0837] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.5 Hz), 1.07 and 1.20(each 3H, each s), 1.52-2.43(14H, m), 4.18(1H, m), 5.33-5.50(2H, m), 6.42(1H, d, J=8.4 Hz), 7.07(1H, m), 7.33-7.39(2H, m), 7.46-7.51(2H, m), 7.56 (1H, d, J=3.9 Hz). IR(CHCl3): 3587, 3442, 3280, 1707, 1643, 1531, 1329, 1308, 1149 cm−1. [α]D20+53.2°±0.9°(c=1.010, MeOH) Anal. (C27H33NO6S2.0.4H2O) Calcd.(%): C, 60.18; H, 6.32; N, 2.60; S, 11.90. Found(%): C, 60.19; H, 6.06; N, 2.63; S, 11.99.

[0838] Compound Number II-118

[0839] 1 H-NMR(CDCl3) δ: 0.91(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.45(14H, m), 4.20(1H, m), 5.33-5.50(2H, m), 6.17(1H, d, J=8.7 Hz), 6.72(2H, m), 6.79(1H, m), 7.11(2H, m), 7.38(1H, d, J=3.9 Hz). IR(CHCl3): 3342, 2669, 1707, 1622, 1583, 1535 cm−1. [α]D23+45.6°±0.9°(c=1.007, MeOH) Anal. (C27H33NO4S2.0.2H2O) Calcd.(%): C, 64.44; H, 6.69; N, 2.78; S, 12.74. Found(%): C, 64.33; H, 6.59; N, 2.83; S, 13.07.

[0840] Compound Number II-119

[0841] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.43(14H, m), 3.79(3H, s), 4.10(2H, s), 4.20(1H, m), 5.33-5.49(2H, m), 5.98(1H, d, J=8.7 Hz), 6.76-6.85(4H, m), 7.24(1H, m), 7.32(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3450, 3431, 2669, 1738, 1709, 1641, 1600, 1437, 1261 cm−1. [α]D23.5+42.8°±0.8°(c=1.005, MeOH.) Anal. (C29H37NO4S) Calcd.(%): C, 70.27; H, 7.52; N, 2.83; S, 6.47. Found(%): C, 70.05; H, 7.55; N, 2.84; S, 6.45.

[0842] Compound Number II-125

[0843] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=9.9 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.42(14H, m), 2.28(3H, s), 4.12(2H, s), 4.20(1H, m), 5.33-5.48 (2H, m), 5.98(1H, d, J=9.0 Hz), 6.71(1H, d, J=3.6 Hz), 7.17 (4H, s), 7.30(1H, d, J=3.6 Hz). IR(CHCl3): 3518, 3450, 3430, 1739, 1709, 1641, 1543, 1506, 1471, 1458 cm−1. [α]D22.5+42.9°±0.8°(c=1.000, MeOH) Anal. (C29H37NO3S) Calcd.(%): C, 72.61; H, 7.77; N, 2.92; S, 6.68. Found(%): C, 72.43; H, 7.78; N, 3.09; S, 6.62.

[0844] Compound Number II-126

[0845] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.42(14H, m), 3.84(3H, s), 4.12(2H, s), 4.19(1H, m), 5.33-5.48 (2H, m), 5.98(1H, d, J=9.0 Hz), 6.77(1H, dt, J=0.9 and 3.9 Hz), 6.88(1H, d, J=8.1 Hz), 9.90(1H, m), 7.15(1H, m), 7.23(1H, m), 7.28(1H, d, J=3.9 Hz). IR(CHCl3): 3509, 3450, 3431, 2664, 1739, 1708, 1639, 1544, 1506, 1464 cm−1. [α]D24+40.4°±0.8°(c=1.003, MeOH) Anal. (C29H37NO4S.0.1H2O) Calcd.(%): C, 70.02; H, 7.53; N, 2.81; S, 6.45. Found(%): C, 69.92; H, 7.53; N, 2.96; S, 6.46.

[0846] Compound Number II-127

[0847] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s),1.18(3H, t, J=7.8 Hz), 1.50-2.42(14H, m), 2.64(2H, q, J=7.8 Hz), 4.15(2H, s), 4.19(1H, m), 5.33-5.48(2H, m), 5.96(1H, d, J=9.3 Hz), 6.68 (1H, d, J=3.6 Hz), 7.16-7.25(4H, m), 7.29(1H, d, J=3.6 Hz). IR (CHCl3): 3516, 3450, 3431, 2667, 1739, 1709, 1641, 1543, 1506, 1471, 1456 cm−1. [α]D21+41.9±0.8°(c=1.013, MeOH) Anal. (C30H39NO3S.0.1H2O) Calcd.(%): C, 72.72; H, 7.97; N, 2.83; S, 6.47. Found(%): C, 72.55; H, 7.88; N, 3.19; S, 6.62.

[0848] Compound Number II-129

[0849] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.22(each 3H, each s),1.50-2.42(14H, m), 2.43(3H, s), 4.20(1H, m), 4.24(2H, s), 5.34-5.49 (2H, m), 5.99(1H, d, J=8.7 Hz), 6.58(1H, m), 6.67(1H, d, J=3.3 Hz), 6.83(1H, d, J=3.9 Hz), 7.32(1H, d, J=3.9 Hz). IR (CHCl3): 3516, 3450, 3431, 2667, 1709, 1643, 1545, 1508, 1471, 1458 cm−1. [α]D22+42.8±0.8°(c=1.006, MeOH) Anal. (C27H35NO3S2) Calcd.(%): C, 66.77; H, 7.26; N, 2.88; S, 13.20. Found(%): C, 66.60; H, 7.23; N, 2.93; S, 13.19.

[0850] Compound Number II-132

[0851] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s), 1.50-2.44(14H, m), 2.31(3H, s), 4.21(1H, m), 4.25(2H, s), 5.34-5.49 (2H, m), 6.01(1H, d, J=8.7 Hz), 6.83(1H, d, J=3.9 Hz), 7.03 (1H, m), 7.11-7.20(3H, m), 7.27(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3450, 3431, 2665, 1739, 1709, 1643, 1543, 1508, 1473 cm1. [α]D22+42.6±1.0°(c=0.861, MeOH) Anal. (C29H37NO3S2H2O) Calcd.(%): C, 67.59; H, 7.31; N, 2.72; S, 12.44. Found(%): C, 67.49; H, 7.27; N, 2.82; S, 12.35.

[0852] Compound Number II-133

[0853] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.5 Hz), 1.09 and 1.21(each 3H, each s), 1.50-2.44(14H, m), 4.15(2H, s), 4.20(1H, m), 5.33-5.49(2H, m), 6.0(1H, d, J=9.3 Hz), 6.13(1H, dd, J=0.6 and 3.0 Hz), 6.32(1H, dd, J=1.8 and 3.0 Hz), 6.84 and 7.22(each 1H, each d, each J=3.6 Hz), 7.47(1H, dd, J=0.6 and 1.8 Hz). IR(CHCl3): 3518, 3450, 3431, 2669, 1739, 1709, 1643, 1545, 1506 cm−1. [α]D23+45.8±0.9°(c=1.003, MeOH) Anal. (C26H33NO4S.0.6H2O) Calcd.(%): C, 66.95; H, 7.39; N, 3.00; S, 6.87. Found(%): C, 67.04; H, 7.17; N, 3.11; S, 7.03.

[0854] Compound Number II-134

[0855] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.5 Hz), 1.10 and 1.22(each 3H, each s), 1.52-2.45(14H, m), 3.96(2H, s), 4.20(1H, m), 5.33-5.49(2H, m), 6.00(1H, d, J=8.7 Hz), 6.30(1H, dd, J=0.9 and 1.8 Hz), 6.81(1H, d, J=3.6 Hz), 7.31-7.33(2H, m), 7.38(1H, t, J=1.8 Hz). IR(CHCl3): 3516, 3450, 3431, 2663, 1739, 1709, 1643, 1545, 1506 cm−1. [α]D21+46.5±0.9°(c=1.002, MeOH) Anal. (C26H33NO4S.0.1H2O) Calcd.(%): C, 68.27; H, 7.32; N, 3.06; S, 7.01. Found(%): C, 68.08; H, 7.14; N, 3.21; S, 7.19.

[0856] Compound Number II-135

[0857] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s), 1.50-2.42(14H, m), 4.20(1H, m), 4.41(2H, s), 5.33-5.49(2H, m), 6.01(1H, d, J=8.7 Hz), 6.91(1H, d, J=3.6 Hz), 7.11(1H, s), 7.27-7.35(3H, m), 7.68-7.77(2H, m). IR(CHCl3): 3512, 3446, 3431, 1709, 1645, 1543, 1508 cm−1. [α]D24+44.9±0.9°(c=1.002, MeOH) Anal. (C30H35NO3S2.0.3H2O) Calcd.(%): C, 68.35; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.17; H, 6.52; N, 2.68; S, 12.04.

[0858] Compound Number II-136

[0859] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.21(each 3H, each s), 1.50-2.41(14H, m), 4.19(1H, m), 4.29(2H, s), 5.33-5.48(2H, m), 6.02(1H, d, J=8.4 Hz), 6.51(1H, s), 6.91(1H, d, J=3.6 Hz), 7.16-7.25 (2H, m), 7.34(1H, d, J=3.6 Hz), 7.42(1H, d, J=8.4 Hz), 7.50(1H, m). IR(CHCl3): 3516, 3450, 3431, 1739, 1709, 1643, 1545, 1508, 1454 cm−1. [α]D23+42.3±0.8°(c=1.001, MeOH) Anal. (C30H35NO4S.0.3H2O) Calcd.(%): C, 70.50; H, 7.02; N, 2.74; S, 6.27. Found(%): C, 70.36; H, 6.94; N, 2.70; S, 6.17.

[0860] Compound Number II-138

[0861] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.20(each 3H, each s), 1.49-2.42(14H, m), 4.20(1H, m), 4.19(2H, s), 5.33-5.48(2H, m), 5.99(1H, d, J=9.0 Hz), 6.80(1H, d, J=3.6 Hz), 7.22 (1H, d, J=7.5 Hz), 7.31-7.50(7H, m), 7.57(2H, m). IR(CHCl3): 3518, 3450, 3431, 2671, 1739, 1709, 1643, 1543, 1506, 1471, 1456 cm−1. [α]D24+38.7±0.8°(c=1.014, MeOH) Anal. (C34H39NO3S.0.2H2O) Calcd.(%): C, 74.88; H, 7.28; N, 2.57; S, 5.88. Found(%): C, 74.92; H, 7.30; N, 2.75; S, 5.99.

[0862] Compound Number II-139

[0863] 1 H-NMR(CDCl3) δ: 0.97(1H, d, J=10.2 Hz), 1.06 and 1.22(each 3H, each s),1.52-2.48(14H, m), 4.11(2H, s), 4.31(1H, m), 5.34-5.51(2H, m), 6.15(1H, d, J=9.0 Hz), 7.19-7.30(6H, m), 7.76(1H, d, J=8.1 Hz), 7.83(1H, s), 8.15(1H, s) IR(CHCl3): 3516, 3442, 2667, 1739, 1709, 1651, 1514, 1495, 1471, 1454, 1435 cm−1. [α]D24+42.8±0.8°(c=1.011, MeOH) Anal. (C32H37NO3S) Calcd.(%): C, 74.53; H, 7.23; N, 2.72; S, 6.22. Found(%): C, 74.25; H, 7.20; N, 2.97; S, 6.05.

[0864] Compound Number II-140

[0865] 1 H-NMR(CDCl3) δ: 0.98(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s),1.52-2.49(14H, m), 4.10(2H, s), 4.32(1H, m), 5.35-5.53(2H, m), 6.17(1H, d, J=8.7 Hz), 7.19-7.32(6H, m), 7.64(1H, d, J=0.9 Hz), 7.76(1H, s), 8.21(1H, d, J=8.4 Hz). IR(CHCl3): 3518, 3442, 2671, 1739, 1707, 1651, 1514, 1493, 1469, 1454, 1404 cm−1. [α]D24+47.1±0.9°(c=1.001, MeOH) Anal. (C32H37NO3S.0.2H2O) Calcd.(%): C, 74.01; H, 7.26; N, 2.70; S, 6.17. Found(%): C, 73.89; H, 7.44; N, 2.93; S, 6.04.

[0866] Compound Number II-141

[0867] mp.134-135° C. 300 MHz 1H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 0.98 and 1.15(each 3H, each s),1.48-2.43(14H, m), 4.20(1H, m), 4.40 and 4.54(each 1H, each d, J=16.5 Hz), 5.33-5.50(2H, m), 6.04(1H, d, J=8.4 Hz), 6.99-7.30(6H, m), 7.55(1H, s), 7.73(1H, d, J=8.4 Hz). IR(CHCl3): 3518, 3437, 2669, 1741, 1709, 1653, 1510, 1471, 1454 cm−1. [α]D25+54.2±0.9°(c=1.003, MeOH) Anal. (C32H37NO3S.0.1H2O) Calcd.(%): C, 74.27; H, 7.25; N, 2.71; S, 6.20. Found(%): C, 74.11; H, 7.16; N, 3.15; S, 6.25.

[0868] Compound Number II-142

[0869] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s),1.49-2.43(14H, m), 3.94(2H, s), 4.22(1H, m), 5.33-5.49(2H, m), 6.03(1H, d, J=8.7 Hz), 7.04(1H, s), 7.17-7.33(6H, m). IR(CHCl3): 3516, 3448, 3433, 2669, 1739, 1709, 1645, 1549, 1508, 1471, 1454 cm−1. [α]D25+40.5±0.8°(c=1.003, MeOH) Anal. (C28H35NO3S.0.1H2O) Calcd.(%): C, 71.95; H, 7.59; N, 3.00; S, 6.86. Found(%): C, 71.82; H, 7.49; N, 3.37; S, 6.83.

[0870] Compound Number II-143

[0871] 1 H-NMR(CDCl3) δ: 0.98(1H, d, J=10.5 Hz), 1.10 and 1.23(each 3H, each s),1.53-2.50(14H, m), 4.24(2H, s), 4.33(1H, m), 5.35-5.54(2H, m), 6.18(1H, d, J=8.4 Hz), 7.19-7.30(6H, m), 7.42(1H, t, J=7.8 Hz), 7.78(1H, s), 8.18(1H, d, J=7.8 Hz). IR(CHCl3): 3514, 3442, 2671, 1709, 1651, 1516, 1495, 1471, 1454, cm−1. [α]D25+53.6±0.9°(c=1.003, MeOH), Anal. (C32H37NO3S.0.1H2O) Calcd.(%): C, 74.27; H, 7.25; N, 2.71; S, 6.20. Found(%): C, 74.18; H, 7.24; N, 2.90; S, 6.14.

[0872] Compound Number II-147

[0873] mp.117-118° C. 300 MHz 1H-NMR(CDCl3) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.21(each 3H, each s), 1.55-2.42(14H, m), 3.87(3H, s), 4.06 (2H, s), 4.18(1H, m), 5.35-5.49(2H, m), 5,56(1H, brs), 5.89(1H, d, J=8.7 Hz), 6.72-6.77(3H, m), 6.87(1H, d, J=8.1 Hz), 7.31(1H, d, J=3.6 Hz). IR(Nujol): 3373, 3184, 2667, 1705, 1622, 1599, 1547, 1520, 1286 cm−1. [α]D23+42.0±0.8°(c=1.008, MeOH) Anal. (C29H37NO5S) Calcd.(%): C, 68.07; H, 7.29; N, 2.74; S, 6.27. Found(%): C, 67.84; H, 7.43; N, 2.71; S, 6.18.

[0874] Compound Number II-148

[0875] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=9.9 Hz), 1.10 and 1.23(each 3H, each s), 1.53-2.45(14H, m), 3.87(3H, s), 2.96-3.01(2H, m), 3.10-3.16(2H, m), 4.22(1H, m), 5.34-5.50(2H, m), 6.01(1H, d, J=8.4 Hz), 6.71(1H, d, J=3.9 Hz), 7.16-7.32(6H, m). IR(CHCl3): 3518, 3450, 3431, 2671, 1739, 1709, 1641, 1545, 1508 cm−1. [α]D22+44.3±0.8°(c=1.006, MeOH) Anal. (C29H37NO3S.0.1H2O) Calcd.(%): C, 72.34; H, 7.79; N, 2.91; S, 6.66. Found(%): C, 72.24; H, 7.68; N, 3.11; S, 6.73.

[0876] Compound Number II-149

[0877] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s), 1.52-2.45(14H, m), 2.43(3H, d, J=0.9 Hz), 3.07-3.18(4H, m), 4.21(1H, m), 5.35-5.50(2H, m), 6.02(1H, d, J=8.4 Hz), 6.53-6.57(2H, m), 6.76 and 7.30(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3516, 3450, 3431, 2667, 1709, 1641, 1543, 1508 cm−1. [α]D22+43.1±0.8°(c=1.005, MeOH) Anal. (C28H37NO3S2.0.3H2O) Calcd.(%): C, 66.58; H, 7.50; N, 2.77; S, 12.70. Found(%): C, 66.47; H, 7.46; N, 2.99; S, 12.62.

[0878] Compound Number II-150

[0879] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s), 1.52-2.45(14H, m), 3.19(4H, s), 4.21(1H, m), 5.34-5.50(2H, m), 6.01(1H, d, J=8.4 Hz), 6.75(1H, d, J=3.9 Hz), 6.79(1H, m), 6.91 (1H, dd, J=3.6 and 5.1 Hz), 7.13(1H, dd, J=0.9 and 5.1 Hz), 7.29(1H, d, J=3.9 Hz). IR(CHCl3): 3514, 3450, 3433, 2667,n 1739, 1709, 1641, 1545, 1508 cm−1. [α]D24+33.5±0.8°(c=1.009, MeOH) Anal. (C27H35NO3S2) Calcd.(%): C, 66.77; H, 7.26; N, 2.88; S, 13.20. Found(%): C, 66.48; H, 7.31; N, 2.97; S, 13.22.

[0880] Compound Number II-151

[0881] 1 H-NMR(CDCl3) δ: 0.97(1H, d, J=9.9 Hz), 1.12 and 1.23(each 3H, each s), 1.53-2.47(14H, m), 3.00-3.06(2H, m), 3.12-3.17(2H, m), 4.27 (1H, m), 5.34-5.51(2H, m), 6.24(1H, d, J=9.0 Hz), 6.75(1H, m), 6.90(1H, dd, J=3.6 and 5.4 Hz), 7.12(1H, dd, J=1.2 and 5.4 Hz), 7.25 and 7.64(each 2H, each d-like). IR(CHCl3): 3516, 3452, 2665, 1738, 1709, 1649, 1523, 1495 cm−1. [α]D24+54.5±0.9°(c=1.016, MeOH) Anal. (C29H37NO3S) Calcd.(%): C, 72.61; H, 7.77; N, 2.92; S, 6.68. Found(%): C, 72.51; H, 7.69; N, 2.98; S, 6.62.

[0882] Compound Number II-152

[0883] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s), 1.51-2.45(14H, m), 2.92-2.97(2H, m), 3.08-3.13(2H, m), 4.22 (1H, m), 5.34-5.50(2H, m), 6.00(1H, d, J=8.7 Hz), 6.69(1H, d, J=3.6 Hz), 6.92-7.00 (2H, m), 7.09-7.15(2H, m), 7.28(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3450, 3431, 1741, 1709, 1641, 1543, 1510, 1471 cm−1. [α]D23+42.6±0.8°(c=1.014, MeOH) Anal. (C29H36FNO3S) Calcd.(%): C, 69.99; H, 7.29; N, 2.81; S, 6.44; F, 3.82. Found(%): C, 69.87; H, 7.29; N, 2.88; S, 6.50; F, 3.85.

[0884] Compound Number II-156

[0885] mp.93-95° C. 1H-NMR(CDCl3) δ: 0.96(1H, d, J=10.2 Hz), 1.13 and 1.23(each 3H, each s), 1.52-2.47(14H, m), 4.08(2H, s), 4.27(1H, m), 5.34-5.51(2H, m), 6.21(1H, d, J=8.7 Hz), 7.18-7.32(6H, m), 7.61 and 7.66(each 1H, each s), 7.74(1H, d, J=8.4 Hz). IR(KBr): 3367, 1705, 1618, 1556, 1533, 1508 cm−1. [α]D23+60.4±0.8°(c=1.012, MeOH) Anal. (C32H37NO3S) Calcd.(%): C, 74.53; H, 7.23; N, 2.72; S, 6.22. Found(%): C, 74.31; H, 7.37; N, 2.99; S, 6.10.

[0886] Compound Number II-157

[0887] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.2 Hz), 1.06 and 1.19(each 3H, each s), 1.47-2.42(14H, m), 4.20(1H, m), 4.28(2H, s), 5.32-5.47(2H, m), 5.98(1H, d, J=8.7 Hz), 6.80(1H, d, J=3.3 Hz), 7.32-7.36(2H, m), 7.41-7.50(2H, m), 7.68(1H, s), 7.77-7.83(3H, m). IR(CHCl3): 3518, 3450, 3431, 1739, 1709, 1641, 1545, 1508, 1471 cm−1. [α]D23+42.7±0.8°(c=1.003, MeOH) Anal. (C32H37NO3S.0.2H2O) Calcd.(%): C, 74.01; H, 7.26; N, 2.70; S, 6.17. Found(%): C, 73.94; H, 7.30; N, 2.89; S, 6.15.

[0888] Compound Number II-158

[0889] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.5 Hz), 1.11 and 1.22(each 3H, each s), 1.51-2.45(14H, m), 2.94-3.00(2H, m), 3.06-3.12(2H, m), 3.83 (3H, s), 4.22(1H, m), 5.34-5.50(2H, m), 6.00(1H, d, J=8.7 Hz), 6.73 (1H, d, J=3.6 Hz), 6.84-6.89(2H, m), 7.09(1H, dd, J=1.5 and 7.8 Hz), 7.20 (1H, dt, J=1.5 and 7.8 Hz), 7.30(1H, d, J=3.6 Hz). IR(CHCl3): 3518, 3450, 3431, 1741, 1709, 1639, 1545, 1506, 1496, 1466 cm−1. [α]D25+41.3±0.8°(c=1.007, MeOH) Anal. (C30H39FNO4S) Calcd.(%): C, 70.69; H, 7.71; N, 2.75; S, 6.29. Found(%): C, 70.42; H, 7.64; N, 2.78; S, 6.37.

[0890] Compound Number II-159

[0891] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.10 and 1.22(each 3H, each s), 1.53-2.48(14H, m), 2.96-3.04(2H, m), 3.07-3.16(2H, m), 4.22 (1H, m), 5.34-5.52(2H, m), 6.04(1H, d, J=8.7 Hz), 6.74(1H, d, J=3.6 Hz), 6.77-6.85 (2H, m), 7.05-7.11 (2H, m), 7.31(1H, d, J=3.6 Hz). IR(CHCl3): 359, 3510, 3429, 3190, 1709, 1636, 1545, 1508, 1456 cm−1. [α]D25+42.7±0.8°(c=1.009, MeOH) Anal. (C29H37NO4S.0.3H2O) Calcd.(%): C, 69.51; H, 7.56; N, 2.80; S, 6.40. Found(%): C, 69.25; H, 7.43; N, 2.89; S, 6.43.

[0892] Compound Number II-160

[0893] mp.125-126° C. 300 MHz 1H-NMR(CDCl3) δ: 0.96(1H, d, J=10.2 Hz), 1.13 and 1.23(each 3H, each s), 1.52-2.47(14H, m), 4.10(2H, s), 4.27 (1H, m), 5.34-5.51(2H, m), 6.20(1H, d, J=9.0 Hz), 7.19-7.33(6H, m), 7.62 and 7.69(each 1H, each s), 7.73(1H, d, J=8.4 Hz). IR(KBr): 3415, 3199, 1736, 1703, 1633, 1523 cm−1. [α]D25+53.3±0.8°(c=1.002, MeOH) Anal. (C32H37NO3S.0.1H2O) Calcd.(%): C, 74.27; H, 7.25; N, 2.71; S, 6.23. Found(%): C, 74.19; H, 7.16; N, 2.81; S, 6.23.

[0894] Compound Number II-161

[0895] mp.98-101° C. 1H-NMR(CDCl3) δ: 0.97(1H, d, J=10.5 Hz), 1.14 and 1.24(each 3H, each s), 1.53-2.47(14H, m), 4.08(2H, s), 4.27 (1H, m), 5.35-5.51(2H, m), 6.21(1H, d, J=8.7 Hz), 6.90(1H, dd, J=1.2 and 5.1 Hz), 6.93(1H, m), 7.24-7.29(2H, m), 7.63(1H, s), 7.75(1H, d, J=8.1 Hz). IR(KBr): 3394, 3097, 1707, 1643, 1533, 1500 cm−1. [α]D25+58.7±1.0°(c=1.006, MeOH) Anal. (C30H35NO3S2.0.3H2O) Calcd.(%): C, 68.35; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.27; H, 6.76; N, 2.94; S, 12.17.

[0896] Compound Number II-162

[0897] mp.106-109° C. 1H-NMR(CDCl3) δ: 0.97(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, each s), 1.53-2.47(14H, m), 4.26(2H, s), 4.27(1H, m), 5.35-5.51(2H, m), 6.22(1H, d, J=8.7 Hz), 6.82(1H, m), 6.93(1H, dd, J=3.6 and 5.1 Hz), 7.16(1H, dd, J=1.2 and 5.1 Hz), 7.32(1H, dd, J=8.1 and 1.8 Hz), 7.68(2H, m), 7.76(1H, d, J=8.1 Hz). IR(KBr): 3396, 3070, 1707, 1645, 1535, 1500 cm−1. [α]D25+59.9±1.0°(c=1.005, MeOH) Anal. (C30H35NO3S2.0.2H2O) Calcd.(%): C, 68.59; H, 6.79; N, 2.67; S, 12.21. Found(%): C, 68.57; H, 6.62; N, 2.76; S, 12.17.

[0898] Compound Number II-163

[0899] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s), 1.49-2.44(14H, m), 4.12(2H, s), 4.23(1H, m), 5.34-5.49(2H, m), 6.09(1H, d, J=8.7 Hz), 6.82 and 6.93(each 1H, each m), 7.13-7.17 (2H, m), 7.34(1H, d, J=1.5 Hz). IR(CHCl13): 3512, 3448, 3431, 1739, 1709, 1645, 1550, 1508, 1471, 1456 cm−1. [α]D25+43.3±0.8°(c=1.007, MeOH) Anal. (C26H33NO3S2.0.1H2O) Calcd.(%): C, 65.95; H, 7.07; N, 2.96; S, 13.54. Found(%): C, 66.12; H, 7.06; N, 3.04; S, 13.66.

[0900] Compound Number II-164

[0901] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.22 (each 3H, each s), 1.49-2.44(14H, m), 3.95(2H, s), 4.22(1H, m), 5.34-5.49 (2H, m), 6.06(1H, d, J=8.7 Hz), 6.92 and 6.96(each 1H, each m), 7.07(1H, d, J=1.5 Hz), 7.28(1H, m), 7.30(1H, d, J=1.5 Hz). IR(CHCl3): 3510, 3431, 1739, 1709, 1645, 1550, 1508, 1471 cm−1. [α]D25+41.1±0.8°(c=1.009, MeOH) Anal. (C26H33NO3S2.0.2H2O) Calcd.(%): C, 65.70; H, 7.08; N, 2.95; S, 13.49. Found(%): C, 65.57; H, 6.97; N, 3.08; S, 13.63.

[0902] Compound Number II-165

[0903] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.22(each 3H, each s), 1.50-2.44(14H, m), 3.74(2H, s), 4.23(1H, m), 5.34-5.50(2H, m), 6.07(1H, d, J=8.0 Hz), 6.23(1H, s), 7.08(1H, d, J=1.5 Hz), 7.24(1H, s), 7.31(1H, d, J=1.5 Hz), 7.36(1H, m). IR(CHCl3): 3510, 3448, 3431, 2663, 1709, 1645, 1550, 1508, 1471 cm−1. [α]D25+44.2±0.8°(c=1.001, MeOH) Anal. (C26H33NO4S.0.2H2O) Calcd.(%): C, 68.00; H, 7.33; N, 3.05; S, 6.98. Found(%): C, 68.00; H, 7.30; N, 3.15; S, 7.12.

[0904] Compound Number II-166

[0905] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.2 Hz), 1.05 and 1.19(each 3H, each s), 1.48-2.40(14H, m), 4.17(1H, m), 4.58(2H, s), 5.31-5.46(2H, m), 5.96(1H, d, J=8.7 Hz), 6.72 and 7.26(each 1H, each d, each J=3.9 Hz), 7.37-7.51(4H, m), 7.79(1H, d, J=8.1 Hz), 7.87 and 7.97 (each 1H, each m). IR(CHCl3): 3516, 3450, 3431, 2667, 1739, 1709, 1641, 1543, 1508, 1471 cm−1. [α]D25.5+41.9±0.8°(c=1.011, MeOH) Anal. (C32H37NO3S.0.2H2O) Calcd.(%): C, 74.01; H, 7.26; N, 2.70; S, 6.17. Found(%): C, 74.10; H, 7.13; N, 2.99; S, 6.15.

[0906] Compound Number II-167

[0907] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.05 and 1.20(each 3H, each s), -1.48-2.42(14H, m), 4.20(1H, m), 4.39(2H, m), 5.31-5.46(2H, m), 6.00(1H, d, J=9.0 Hz), 6.96(1H, s), 7.30-7.33(2H, m), 7.40-7.50 (3H, m), 7.78(1H, d, J=8.1 Hz), 7.87 and 7.95(each 1H, each m). IR(CHCl3): 3518, 3448, 3431, 2665, 1738, 1709, 1645, 1549, 1508, 1471 cm−1. [α]D24+37.9±0.8°(c=1.004, MeOH) Anal. (C32H37NO3S.0.1H2O) Calcd.(%): C, 74.27; H, 7.25; N, 2.71; S, 6.20. Found(%): C, 74.13; H, 7.18; N, 2.87; S, 6.26.

[0908] Compound Number II-169

[0909] 1 H-NMR(CDCl3) δ: 0.98(1H, d, J=10.5 Hz), 1.10 and 1.23(each 3H, each s),1.53-2.50(14H, m), 4.23(2H, s), 4.33(1H, m), 5.35-5.54(2H, m), 6.18(1H, d, J=8.7 Hz), 6.92(1H, dd, J=1.2 and 4.8 Hz), 7.01(1H, m), 7.22(1H, d, J=7.8 Hz), 7.24(1H, dd, J=3.0 and 4.8 Hz), 7.42(1H, d, J=7.8 and 8.1 Hz), 7.79(1H, s), 8.18(1H, d, J=8.1 Hz). IR(CHCl3): 3516, 3442, 2667, 1709, 1651, 1516, 1495, 1471 cm−1. [α]D26+50.9±0.9°(c=1.009, MeOH), Anal. (C30H35NO3S2.0.2H2O) Calcd.(%): C, 68.59; H, 6.79; N, 2.67; S, 12.21. Found(%): C, 68.51; H, 6.69; N, 2.73; S, 12.39.

[0910] Compound Number II-170

[0911] 1 H-NMR(CDCl3) δ: 0.99(1H, d, J=10.2 Hz), 1.11 and 1.24(each 3H, each s), 1.53-2.50(14H, m), 4.03(2H, s), 4.34(1H, m), 5.36-5.54 (2H, m), 6.20(1H, d, J=8.4 Hz), 7.24(1H, d, J=8.4 Hz), 7.24(1H, d, J=7.2 Hz), 7.30(1H, m), 7.35(1H, t, J=1.8 Hz), 7.42(1H, dd, J=7.2 and 8.1 Hz), 7.81(1H, s), 8.19(1H, d, J=7.2 Hz). IR(CHCl3): 3518, 3442, 1739, 1709, 1651, 1516, 1496, 1471 cm−1. [α]D25+54.3±1.0°(c=1.002, MeOH) Anal. (C30H35NO4S.0.1H2O) Calcd.(%): C, 71.00; H, 6.99; N, 2.76; S, 6.32. Found(%): C, 70.95; H, 6.82; N, 2.74; S, 6.35.

[0912] Compound Number II-173

[0913] 1 H-NMR(CDCl3) δ: 0.99(1H, d, J=10.5 Hz), 1.16 and 1.24(each 3H, each s), 1.53-2.48(14H, m), 3.93(2H, s), 4.32(1H, m), 5.34-5.52(2H, m), 6.35(1H, d, J=8.7 Hz), 7.31-7.42(2H, m), 7.56(1H, d, J=6.9 Hz), 7.71(1H, dd, J=1.5 and 8.1 Hz), 7.78-7.83(2H, m), 7.92(1H, s). IR (CHCl3): 3516, 3452, 3026, 2667, 1738, 1709, 1649, 1641, 1514, 1481, 1469, 1454 cm−1. [α]D24+67.5±1.1°(c=1.005, MeOH) Anal. (C30H35NO3.0.1H2O) Calcd.(%): C, 78.43; H, 7.72; N, 3.05. Found(%): C, 78.36; H, 7.99; N, 3.24.

[0914] Compound Number II-174

[0915] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s),1.50-2.42(14H, m), 3.21(2H, t, J=8.7 Hz), 4.02(2H, s), 4.20 (1H, m), 4.59(2H, t, J=8.7 Hz), 5.34-5.49(2H, m), 6.01(1H, d, J=8.7 Hz), 6.80 (1H, d, J=3.6 Hz), 7.06(1H, d, J=1.8 Hz), 7.19(1H, m), 7.30 (1H, d, J=3.6 Hz). IR(CHCl3): 3512, 3450, 3431, 2667, 1739, 1709, 1641, 1543, 1508, 1460 cm−1. [α]D25+35.7±0.8°(c=1.002, MeOH), Anal. (C30H36BrNO4S) Calcd.(%): C, 61.43; H, 6.19; Br, 13.62; N, 2.39; S, 5.47. Found(%): C, 61.26; H, 6.11; Br, 13.54; N, 2.46; S, 5.47.

[0916] Compound Number II-175

[0917] 1 H-NMR(CDCl3) δ: 0.96(1H, d, J=10.2 Hz), 1.14 and 1.23(each 3H, each s),1.52-2.46(14H, m), 4.21((2H, s), 4.28(1H, m), 5.34-5.51(2H, m), 6.23(1H, d, J=9.0 Hz), 6.94(1H, dd, J=1.2 and 4.8 Hz), 7.05(1H, m), 7.21-7.26(2H, m), 7.35(1H, dd, J=7.5 and 8.1 Hz), 7.71(1H, d, J=7.5 Hz), 7.75(1H, s). IR(CHCl3): 3510, 3448, 3427, 2665, 1709, 1649, 1539, 1504, 1469, 1454 cm−1. [α]D25+47.4±0.9°(c=1.005, MeOH), Anal. (C32H37NO3S.0.1H2O) Calcd.(%): C, 74.27; H, 7.25; N, 2.71; S, 6.20. Found(%): C, 74.15; H, 7.14; N, 2.89; S, 6.26.

[0918] Compound Number II-176

[0919] 1 H-NMR(CDCl3) δ: 0.97(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, each s), 1.53-2.47(14H, m), 4.22((2H, s), 4.27(1H, m), 5.35-5.51(2H, m), 6.22(1H, d, J=8.7 Hz), 6.94(1H, dd, J=1.2 and 4.8 Hz), 7.05(1H, m), 7.21-7.26(2H, m), 7.35(1H, dd, J=7.5 and 8.1 Hz), 7.71(1H, d, J=7.5 Hz), 7.75(1H, s). IR(CHCl3): 3512, 3448, 3427, 2665, 1709, 1649, 1539, 1504, 1469 cm−1. [α]D25+46.1±0.9°(c=1.011, MeOH), Anal. (C30H35NO3S2) Calcd.(%): C, 69.06; H, 6.76; N, 2.68; S, 12.29. Found(%): C, 68.77; H, 6.84; N, 2.78; S, 12.30.

[0920] Compound Number II-177

[0921] 1 H-NMR(CDCl3) δ: 0.96(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, each s),1.53-2.46(14H, m), 2.31(3H, s), 4.17((2H, s), 4.28(1H, m), 5.34-5.51 (2H, m), 6.22(1H, d, J=9.0 Hz), 7.09 and 7.15(each 2H, each d, J=7.8 Hz), 7.19(1H, d, J=7.2 Hz), 7.34(1H, dd, J=7.2 and 7.8 Hz), 7.70 (1H, d, J=7.8 Hz), 7.75(1H, s). IR(CHCl3): 3510, 3448, 3427, 2669, 1709, 1649, 1537, 1504, 1469 cm−1. [α]D25+45.6±0.9°(c=1.005, MeOH), Anal. (C33H39NO3S.0.1H2O) Calcd.(%): C, 74.57; H, 7.43; N, 2.64; S, 6.03. Found(%): C, 74.46; H, 7.48; N, 2.78; S, 6.15.

[0922] Compound Number II-178

[0923] 1 H-NMR(CDCl3) δ: 0.97(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, each s),1.53-2.47(14H, m), 2.31(3H, s), 4.28(1H, m), 4.40((2H, s), 5.35-5.51 (2H, m), 6.23(1H, d, J=8.7 Hz), 6.92-6.94(2H, m), 7.16(1H, dd, J=1.5 and 5.1 Hz), 7.28(1H, d, J=7.5 Hz), 7.36(1H, t, J=7.5 Hz), 7.72 (1H, d, J=7.5 Hz), 7.75(1H, s). IR(CHCl3): 3508, 3448, 3427, 2663, 1709, 1649, 1539, 1504, 1469 cm−1. [α]D25+46.2±0.9°(c=1.005, MeOH), Anal. (C30H35NO3S2) Calcd.(%): C, 69.06; H, 6.76; N, 2.68; S, 12.29. Found(%): C, 68.84; H, 6.86; N, 2.79; S, 12.28.

[0924] Compound Number II-179

[0925] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s), 1.51-2.42(14H, m), 4.09(2H, s), 4.18(1H, m), 5.33-5.48(2H, m), 5.96(1H, d, J=9.3 Hz), 6.54(1H. d, J=3.6 Hz), 7.24-7.42(10H, m). IR(CHCl3): 3510, 3450, 3431, 1739, 1709, 1641, 1543, 1506, 1479, 1458 cm−1. [α]D24.5+39.4±0.8°(c=1.007, MeOH) Anal. (C34H39NO3S.0.1H2O) Calcd.(%): C, 75.13; H, 7.27; N, 2.58; S, 5.90. Found(%): C, 75.05; H, 7.32; N, 2.69; S, 6.17.

[0926] Compound Number II-180

[0927] 1 H-NMR(CDCl3) δ: 1.00(1H, d, J=10.2 Hz), 1.15 and 1.26(each 3H, each s), 1.55-2.49(14H, m), 4.30(1H, m), 5.37-5.53(2H, m), 6.38(1H, d, J=8.1 Hz), 7.32(1H, m), 7.49-7.58(3H, m), 7.64-7.67(2H, m), 7.92 (1H, s). IR(CHCl3): 3514, 3446, 1714, 1655, 1618, 1514, 1469, 1446 cm−1. [α]D25+66.7±1.1°(c=1.005, MeOH) Anal. (C30H33NO4.0.2H2O) Calcd.(%): C, 75.83; H, 7.08; N, 2.95. Found(%): C, 75.69; H, 7.05; N, 3.08.

[0928] Compound Number II-181

[0929] mp.103-104° C. 300 MHz 1H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.49-2.42(14H, m), 3.79(3H, s), 4.07 ((2H, s), 4.20(1H, m), 5.33-5.48(2H, m), 5.98(1H, d, J=8.7 Hz), 6.75 (1H, d, J=3.6 Hz), 6.85 and 7.15(each 2H, each d, J=8.4 Hz), 7.31 (1H, d, J=3.6 Hz). IR(CHCl3): 3519, 3450, 3431, 1741, 1709, 1641, 1612, 1543, 1510, 1464 cm−1. [α]D25+43.8±0.8°(c=1.009, MeOH) Anal. (C29H37NO4S) Calcd.(%): C, 70.27; H, 7.52; N, 2.83; S, 6.47. Found(%): C, 70.33; H, 7.55; N, 3.05; S, 6.46.

[0930] Compound Number II-182

[0931] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.07 and 1.21(each 3H, each s),1.49-2.42(14H, m), 4.20(1H, m), 4.37(2H, s), 5.33-5.48(2H, m), 5.99(1H, d, J=8.4 Hz), 6.82(1H, d, J=3.6 Hz), 7.21(1H, s), 7.30 (1H, d, J=3.6 Hz), 7.34-7.37(2H, m), 7.69(1H, m), 7.86(1H, m). IR (CHCl3): 3512, 3450, 3431, 2671, 1739, 1709, 1643, 1543, 1508, 1471, 1460 cm−1. [α]D25+40.2±0.8°(c=1.005, MeOH), Anal. (C30H35NO3S2.0.4H2O) Calcd.(%): C, 68.12; H, 6.82; N, 2.64; S, 12.12. Found(%): C, 68.05; H, 6.70; N, 2.87; S, 12.00.

[0932] Compound Number II-183

[0933] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.47(14H, m), 4.13(2H, s), 4.20(1H, m), 5.33-5.50(2H, m), 6.01(1H, d, J=9.0 Hz), 6.80(1H, m), 6.82(1H, m), 6.86(1H, m), 7.12 (1H, m), 7.15(1H, m), 7.31(1H, d, J=3.9 Hz). IR(CHCl3): 3597, 3510, 3448, 3427, 3190, 1709, 1633, 1545, 1508, 1456 cm−1. [α]D24+41.8°±0.8°(c=1.004, MeOH) Anal. (C28H35NO4S.0.3H2O) Calcd.(%): C, 69.11; H, 7.37; N, 2.88; S, 6.59. Found(%): C, 68.94; H, 7.42; N, 2.96; S, 6.73.

[0934] Compound Number II-184

[0935] 1 H-NMR(CDCl3) δ: 1.00(1H, d, J=10.5 Hz), 1.17 and 1.25(each 3H, each s), 1.55-2.50(14H, m), 3.93 (2H, s), 4.32(1H, m), 5.35-5.49(2H, m), 6.37(1H, d, J=8.7 Hz), 7.31-7.43(2H, m), 7.54-7.63(3H, m), 7.84 (1H, d, J=7.2 Hz), 8.16(1H, s). IR (CDCl3): 3514, 3450, 2667, 1709, 1651, 1572, 1514, 1481, 1452 cm−1. [α]D24+58.3±1.0°(c=1.003, MeOH) Anal. (C30H35NO3.0.1H2O) Calcd.(%): C, 78.43; H, 7.72; N, 3.05. Found(%): C, 78.26; H, 7.73; N, 3.28.

[0936] Compound Number II-185

[0937] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s), 1.52-2.42(14H, m), 4.16(2H, s), 4.19(1H, m), 5.33-5.47(2H, m), 5.99(1H, d, J=9.3 Hz), 6.78(1H, d, J=3.6 Hz), 7.00-7.12(2H, m), 7.20-7.27 (2H, m), 7.30(1H, d, J=3.6 Hz). IR(CHCl3): 3510, 3450, 3431, 1741, 1709, 1643, 1543, 1508, 1456 cm−1. [α]D24+38.0±0.8°(c=1.03, CHCl3) Anal. (C28H34FNO3S.0.5H2O) Calcd.(%): C, 68.26; H, 7.16; N, 2.86; S, 6.51; F, 3.86. Found(%): C, 68.24; H, 7.08; N, 2.93; S, 6.50; F, 3.80.

[0938] Compound Number II-188

[0939] mp.53-55° C. 300 MHz 1H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.51-2.42(14H, m), 4.07(2H, s), 4.19 (1H, m), 5.05(2H, s), 5.33-5.48(2H, m), 5.98(1H, d, J=9.0 Hz), 6.76 (1H, d, J=3.6 Hz), 6.92 and 7.15(each 2H, each d, J=8.7 Hz), 7.31(1H, d, J=3.6 Hz), 7.32.-7.43 (5H, m) IR(CHCl3): 3518, 3450, 3431, 1741, 1709, 1641, 1612, 1545, 1510, 1469, 1456 cm−1. [α]D24+36.0±0.8°(c=1.005, MeOH), Anal. (C35H41NO4S.0.4H2O) Calcd.(%): C, 72.61; H, 7.28; N, 2.42; S, 5.54. Found(%): C, 72.58; H, 7.33; N, 2.65; S, 5.53.

[0940] Compound Number II-189

[0941] 300 MHz 1H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21 (each 3H, each s),1.51-2.42(14H, m), 4.07(2H, s), 4.19(1H, m), 4.51-4.53 (2H, m), 5.26-5.46(4H, m), 5.98(1H, d, J=8.7 Hz), 6.05(1H, m), 6.76 (1H, d, J=3.6 Hz), 6.87 and 7.14(each 2H, each d, J=8.7 Hz), 7.31 (1H, d, J=3.6 Hz). IR(CHCl3): 3511, 3450, 3431, 1741, 1709, 1641, 1612, 1543, 1508, 1471, 1458 cm−1. [α]D24+39.7±0.8°(c=1.008, MeOH), Anal. (C31H39NO4S.0.2H2O) Calcd.(%): C, 70.88; H, 7.56; N, 2.67; S, 6.10. Found(%): C, 70.86; H, 7.60; N, 2.68; S, 6.17.

[0942] Compound Number II-190

[0943] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s),1.50-2.43(14H, m), 4.04(2H, s), 4.20(1H, m), 5.33-5.49(2H, m), 5.94(2H, s), 5.98(1H, d, J=8.7 Hz), 6.68-6.78(4H, m), 7.31(1H, d, J=3.9 Hz). IR(CHCl3): 3518, 3450, 3431, 1739, 1709, 1641, 1543, 1504, 1489, 1444, 1250, 1041 cm−1. [α]D24+42.2±0.8°(c=1.010, MeOH), Anal. (C29H35NO5S) Calcd.(%): C, 68.34; H, 6.92; N, 2.75; S, 6.29. Found(%): C, 68.19; H, 6.88; N, 2.86; S, 6.20.

[0944] Compound Number II-191

[0945] mp.76-80° C. 1H-NMR(CDCl3) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.21 (each 3H, each s),1.51-2.43(14H, m), 4.13(2H, s), 4.20(1H, m), 5.34-5.49(2H, m), 6.00(1H, d, J=8.4 Hz), 6.78(1H, d, J=3.9 Hz), 6.90-7.04 (3H, m), 7.27(1H, m), 7.32(1H, d, J=3.9 Hz). IR(Nujol): 3408, 1703, 1631, 1514, 1250 cm−1. [α]D25+51.0±0.9°(c=1.001, MeOH), Anal. (C28H34FNO3S) Calcd.(%): C, 69.54; H, 7.09; N, 2.90; S, 6.63; F,3.93. Found(%): C, 69.77; H, 7.23; N, 2.95; S, 6.55; F,3.93.

[0946] Compound Number II-192

[0947] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s),1.51-2.44(14H, m), 4.19(2H, s), 4.20(1H, m), 5.34-5.49(2H, m), 6.00(1H, d, J=8.4 Hz), 6.78 and 7.32(each 1H, each d, each J=3.6 Hz), 7.40-7.54(4H, m). IR(CHCl3): 3516, 3450, 3431, 1739, 1709, 1643, 1543, 1508, 1331, 1167, 1130 cm−1. [α]D25+39.5±0.8°(c=1.012, MeOH), Anal. (C29H34F3NO3S) Calcd.(%): C, 65.27; H, 6.42; N, 2.62; S, 6.01; F,10.68. Found(%): C, 65.05; H, 6.46; N, 2.74; S, 6.02; F,10.63.

[0948] Compound Number II-193

[0949] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s), 1.51-2.26(14H, m), 4.19(1H, m), 4.26(2H, s), 5.33-5.49(2H, m), 6.00(1H, d, J=8.4 Hz), 6.79(1H, d, J=3.9 Hz), 7.20-7.25(3H, m), 7.30(1H, d, J=3.9 Hz), 7.37-7.40(1H, m). IR(CHCl3): 3516, 3450, 3431, 1741, 1709, 1643, 1543, 1508, 1471 cm−1. [α]D25+38.5±0.8°(c=1.00, CHCl3) Anal. (C28H34FNO3S.0.5H2O) Calcd.(%): C, 66.06; H, 6.93; N, 2.75; S, 6.30; Cl, 6.96. Found(%): C, 66.21; H, 6.87; N, 2.97; S, 6.24; Cl, 6.75.

[0950] Compound Number II-194

[0951] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.07 and 1.20(each 3H, each s), 1.49-2.42(14H, m), 2.30(6H, s), 4.15(2H, s), 4.19(1H, m), 5.33-5.48 (2H, m), 5.97(1H, d, J=8.7 Hz), 6.56(1H, d, J=3.9 Hz), 7.03-7.13 (3H, m), 7.26(1H, d, J=3.9 Hz). IR(CHCl3): 3518, 3450, 3431, 2671, 1739, 1709, 1641, 1543, 1506, 1471 cm−1. [α]D24+43.7±0.8°(c=1.004, MeOH) Anal. (C30H39FNO3S.0.1H2O) Calcd.(%): C, 72.72; H, 7.97; N, 2.83; S, 6.47. Found(%): C, 72.68; H, 7.95; N, 2.96; S, 6.48.

[0952] Compound Number II-195

[0953] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.21(each 3H, each s), 1.53-2.50(14H, m), 4.19(1H, m), 4.32(2H, s), 5.34-5.47(2H, m), 6.00(1H, d, J=8.7 Hz), 6.76(1H, d, J=3.6 Hz), 7.28-7.39(3H, m), 7.50 (1H, m), 7.66(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3450, 3431, 2669, 1741, 1709, 1643, 1543, 1508, 1456, 1315, 1163, 1126, 1059, 1038 cm−1. [α]D25+36.4±0.7°(c=1.03, CHCl3) Anal. (C29H34F3NO3S) Calcd.(%): C, 65.27; H, 6.42; N, 2.62; S, 6.01. Found(%): C, 65.34; H, 6.30; N, 2.82; S, 6.00.

[0954] Compound Number II-197

[0955] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.20(each 3H, each s),1.49-2.42(14H, m), 3.22(2H, t, J=8.7 Hz), 4.07(2H, s), 4.20 (1H, m), 4.57(2H, t, J=8.7 Hz), 5.33-5.48(2H, m), 5.99(1H, d, J=9.0 Hz), 6.79 (1H, t, 7.5 Hz), 6.80(1H, d, J=3.6 Hz), 6.95(1H, d, J=7.5 Hz), 7.09(1H, d, J=7.5 Hz), 7.30(1H, d, J=3.6 Hz). IR(CDCl3): 3514, 3450, 3431, 2667, 1739, 1709, 1641, 1545, 1506, 1458 cm−1. [α]D25+42.0±0.8°(c=1.004, MeOH), Anal. (C30H37NO4S.0.1H2O) Calcd.(%): C, 70.72; H, 7.36; N, 2.75; S, 6.29. Found(%): C, 70.59; H, 7.39; N, 2.95; S, 6.31.

[0956] Compound Number II-198

[0957] 1 H-NMR(CDCl3) δ: 0.92 (1H, d, J=10.5 Hz), 1.07 and 1.19 (each 3H, each s),1.47-2.41(14H, m), 4.20(1H, m), 4.24(2H, s), 5.32-5.47(2H, m), 6.00(1H, d, J=8.7 Hz), 6.78(1H, d, J=3.9 Hz), 7.21(1H, dd, J=1.8 and 8.4 Hz), 7.26(1H, d, J=5.7 Hz), 7.33(1H, d, J=3.9 Hz), 7.43(1H, d, J=5.7 Hz), 7.67(1H, d, J=1.8 Hz), 7.81(1H, d, J=8.4 Hz). IR(CHCl3): 3516, 3450, 3431, 1739, 1709, 1641, 1545, 1458 cm−1. [α]D25+40.9±0.8°(c=1.002, MeOH), Anal. (C30H35NO3S2.0.3H2O) Calcd.(%): C, 68.36; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.30; H, 6.68; N, 2.94; S, 12.25.

[0958] Compound Number II-199

[0959] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.07 and 1.20(each 3H, each s),1.49-2.42(14H, m), 4.20(1H, m), 4.27(2H, s), 5.32-5.48(2H, m), 5.99(1H, d, J=8.7 Hz), 6.80(1H, d, J=3.6 Hz), 7.24(1H, dd, J=1.5 and 8.1 Hz), 7.31(1H, dd, J=0.6 and 5.4 Hz), 7.33(1H, d, J=3.6 Hz), 7.40 (1H, d, J=5.4 Hz), 7.73(1H, m), 7.77(1H, d, J=8.1 Hz). IR (CHCl3): 3516, 3450, 3431, 1741, 1709, 1641, 1543, 1508, 1469 cm−1. [α]D25+41.5±0.8°(c=1.002, MeOH), Anal. (C30H35NO3S2.0.3H2O) Calcd.(%): C, 68.36; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.37; H, 6.73; N, 2.86; S, 12.21.

[0960] Compound Number II-200

[0961] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.06 and 1.19(each 3H, each s),1.48-2.41(14H, m), 4.19(1H, m), 4.39(2H, s), 5.32-5.47(2H, m), 5.99(1H, d, J=8.7 Hz), 6.86(1H, d, J=3.6 Hz), 7.21(1H, d, J=7.2 Hz), 7.30(1H, d, J=3.6 Hz), 7.35(1H, t, J=7.2 Hz), 7.36(1H, d, J=5.4 Hz), 7.42(1H, d, J=5.4 Hz), 7.74(1H, d, J=7.2 Hlz). IR(CHCl3): 3516, 3450, 3431, 1739, 1709, 1641, 1543, 1508, 1471, 1460 cm−1. [α]D25+42.0±0.8°(c=1.001, MeOH), Anal. (C30H35NO3S2.0.3H2O) Calcd.(%): C, 68.36; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.63; H, 6.78; N, 2.84; S, 12.26.

[0962] Compound Number II-201

[0963] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.2 Hz), 1.07 and 1.20(each 3H, each s),1.52-2.47(14H, m), 4.20(1H, m), 4.23(2H, s), 5.32-5.51(2H, m), 6.08(1H, d, J=8.7 Hz), 6.75(1H, d, J=3.6 Hz), 6.95(1H, dd, J=2.4 and 9.0 Hz), 7.10(1H, d, J=2.4 Hz), 7.19(1H, s), 7.27(1H, d, J=3.6 Hz), 7.66(1H, d, J=9.0 Hz). IR(CHCl3): 3427, 3249, 1707, 1633, 1601, 1545, 1510, 1442 cm−1. [α]D25+40.1±0.8°(c=1.007, MeOH), Anal. (C30H35NO4S2.0.3H2O) Calcd.(%): C, 66.34; H, 6.61; N, 2.58; S, 11.81. Found(%): C, 66.21; H, 6.70; N, 2.70; S, 11.75.

[0964] Compound Number II-202

[0965] 1 H-NMR(CDCl) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.53-2.45(14H, m), 4.17(1H, m), 4.24(2H, m), 4.69(2H, m), 5.35-5.47(2H, m), 6.02(1H, d, J=9.3 Hz), 6.72(1H, d, J=3.9 Hz), 7.23-7.31(4H, m), 7.40(1H, m). IR(CHCl3): 3516, 3450, 3431, 1709, 1641, 1527, 1508, 1456 cm−1. [α]D26+32.7±0.7°(c=1.00, CHCl3)

[0966] Compound Number II-203

[0967] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.2 Hz), 1.08 and 1.21(each 31H, each s), 1.54-2.48(18H, m), 3.20 (4H, m), 4.11-4.22(3H, m), 4.43(2H, s), 5.33-5.55(2H, m), 5.99(1H, d, J=8.4 Hz), 6.67(1H, d, J=4.2 Hz), 7.30-7.43 (4H, m), 7.64(1H, d, J=4.2 Hz). IR(CHCl3): 3514, 3448, 3420, 2555, 2459, 1711, 1643, 1543, 1508, 1456 cm−1. [α]D26+20.4±0.6°(c=1.05, CHCl3) Anal. (C33H44N2O3S.1.1H2O) Calcd.(%): C, 69.71; H, 8.19; N, 4.93; S, 5.64. Found(%): C, 69.69; H, 8.08; N, 4.92; S, 5.54.

[0968] Compound Number II-204

[0969] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.5 Hz), 1.07 and 1.21(each 3H, each s), 1.53-2.46(14H, m), 2.49(6H,s), 3.79(1H, d, J=10.8 Hz), 3.84 (1H, d, J=10.8 Hz), 4.19(1H, m), 4.35(1H, d, J=20.1 Hz), 4.37(1H, d, J=20.1 Hz), 5.36-5.54 (2H, m), 5.94(1H, d, J=9.0 Hz), 6.71(1H, d, J=3.6 Hz), 7.25-7.43(5H, m). IR(CHCl3): 3516, 3448, 3429, 2553, 2459, 1711, 1643, 1545, 1506, 1471 cm−1. [α]D26+20.9±0.6°(c=1.03, CHCl3) Anal. (C31H42N2O3S.3.1H2O) Calcd.(%): C, 64.35; H, 8.40; N, 4.84; S, 5.54. Found(%): C, 64.36; H, 7.87; N, 4.63; S, 5.17.

[0970] Compound Number II-205

[0971] 1 H-NMR(CDCl3) δ: 0.98(1H, d, J=10.5 Hz), 1.13 and 1.24(each 3H, each s), 1.53-2.47(14H, m), 3.20-3.27(4H, m), 4.28(1H, m), 5.35-5.51 (2H, m), 6.32(1H, d, J=8.4 Hz), 7.24(1H, d, J=7.5 Hz), 7.34 and 7.46 (each 1H, each m), 7.55(1H, dd, J=1.8 and 8.4 Hz), 7.67(1H, d, J=1.8 Hz), 8.00-8.04(2H, m). IR(CHCl3): 3518, 3448, 1709, 1649, 1597, 1514, 1294 cm−1. [α]D25+58.8±1.0°(c=1.001, MeOH) Anal. (C32H37NO4.0.2H2O) Calcd.(%): C, 76.37; H, 7.49; N, 2.78. Found(%): C, 76.33; H, 7.50; N, 2.88.

[0972] Compound Number II-206

[0973] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.07 and 1.22(each 3H, each s), 1.51-2.43(14H, m), 3.97(2H, s), 4.21(1H, m), 5.34-5.49(2H, m), 6.07(1H, d, J=3.3 Hz), 6.38(1H, d, J=9.3 Hz), 6.98-7.04(3H, m), 7.13-7.22(2H, m). IR (CHCl3): 3518, 3438, 1739, 1709, 1651, 1606, 1549, 1508 cm−1. [α]D26+57.2±1.0°(c=1.016, MeOH) Anal. (C28H34FNO4.0.1H2O) Calcd.(%): C, 71.65; H, 7.34; N, 2.98; F, 4.05. Found(%): C, 71.57; H, 7.44; N, 3.14; F, 4.01.

[0974] Compound Number II-207

[0975] 1 H-NMR(CDCl3) δ: 0.96(1H, d, J=10.5 Hz), 1.07 and 1.21(each 3H, each s), 1.52-2.43(14H, m), 4.00(2H, s), 4.21(1H, m), 5.34-5.49(2H, m), 6.09(1H, d, J=3.3 Hz), 6.40(1H, d, J=9.6 Hz), 7.01(1H, d, J=3.3 Hz), 7.22-7.36(5H, m). IR (CHCl3): 3516, 3439, 2667, 1738, 1709, 1651, 1606, 1547, 1498 cm−1. [α]D24+62.2±1.0°(c=1.007, MeOH) Anal. (C28H35NO4.0.2H2O) Calcd.(%): C, 74.21; H, 7.87; N, 3.09. Found(%): C, 74.14; H, 7.81; N, 3.25.

[0976] Compound Number II-208

[0977] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.2 Hz), 1.07 and 1.20(each 3H, each s),1.48-2.42(14H, m), 4.19(1H, m), 4.42(2H, s), 5.32-5.47(2H, m), 5.98(1H, d, J=8.7 Hz), 6.78(1H, d, J=2.1 Hz), 6.84(1H, d, J=3.9 Hz), 7.13(1H, dd, J=1.5 and 7.5 Hz), 7.19(1H, t, J=7.5 Hz), 7.30(1H, d, J=3.9 Hz), 7.50(1H, dd, J=1.5 and 7.5 Hz), 7.63(1H, d, 2.1 Hz). IR(CHCl3): 3516, 3450, 3431, 1741, 1709, 1641, 1543, 1508, 1471, 1458, 1427 cm−1. [α]D25+43.5±0.8°(c=1.010, MeOH), Anal. (C30H35NO4S.0.2H2O) Calcd.(%): C, 70.75; H, 7.01; N, 2.75; S, 6.30. Found(%): C, 70.80; H, 7.02; N, 2.96; S, 6.26.

[0978] Compound Number II-209

[0979] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s), 1.55-2.41(14H, m), 2.95(3H, s), 4.18-4.21(3H, m), 4.45(2H, s), 5.39-5.43(2H, m), 6.00(1H, d, J=8.7 Hz), 6.63-6.71(4H, m), 7.16-7.26(6H, m), 7.32(1H, m). IR(CHCl3): 3516, 3450, 3431, 1739, 1709, 1643, 1599, 1543, 1505, 1454 cm−1. [α]D26+32.2±0.7°(c=1.00, CHCl3) Anal. (C36H44N2O3S.0.6H2O) Calcd.(%): C, 72.59; H, 7.65; N, 4.70; S, 5.38. Found(%): C, 72.68; H, 7.47; N, 4.74; S, 5.29.

[0980] Compound Number II-211

[0981] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=9.9 Hz), 1.07 and 1.20(each 3H, each s), 1.49-2.41(14H, m), 4.19(1H, m), 4.30(2H, s), 5.32-5.48(2H, m), 5.99(1H, d, J=9.0 Hz), 6.82(1H, d, J=3.6 Hz), 7.24(1H, dd, J=1.5 and 8.1 Hz), 7.30-7.36(2H, m), 7.4-7.47(2H, m), 7.55(1H, d, J=8.1 Hz), 7.87-7.94(2H, m). IR(CHCl3): 3510, 3450, 3431, 2669, 1739, 1709, 1641, 1545, 1506, 1458, 1429 cm−1. [α]D24+39.4±0.8°(c=1.002, MeOH) Anal. (C34H37NO4S.0.1H2O) Calcd.(%): C, 73.25; H, 6.73; N, 2.51; S, 5.75. Found(%): C, 73.13; H, 6.53; N, 2.69; S, 5.79.

[0982] Compound Number II-212

[0983] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.43(14H, m), 3.79 and 3.86(each 3H, each s), 4.14(2H, s), 4.19(1H, m), 5.33-5.48(2H, m), 5.96(1H, d, J=8.4 Hz), 6.78-6.85 (3H, m), 7.00(1H, t, J=8.1 Hz), 7.30(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3450, 3431, 2667, 1739, 1709, 1641, 1543, 1506, 1481, 1273, 1076 cm−1. [α]D26+39.6±0.8°(c=1.007, MeOH) Anal. (C30H39NO5S.0.1H2O) Calcd.(%): C, 68.31; H, 7.49; N, 2.66; S, 6.08. Found(%): C, 68.17; H, 7.50; N, 2.76; S, 6.13.

[0984] Compound Number II-213

[0985] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22 (each 3H, each s),1.51-2.45(14H, m), 2.39(3H, s), 4.15(2H, s), 4.21(1H, m), 5.34-5.50 (2H, m), 5.87(1H, s), 6.04(1H, d, J=8.7 Hz), 6.86(1H, d, J=3.6 Hz), 7.32(1H, d, J=3.6 Hz). IR(CHCl3): 3514, 3450, 3431, 1709, 1645, 1608, 1545, 1508, 1471, 1456 cm−1. [α]D25+47.0±0.9°(c=1.017, MeOH), Anal. (C26H34N2O4S.0.3H2O) Calcd.(%): C, 65.60; H, 7.33; N, 5.88; S, 6.74. Found(%): C, 65.49; H, 7.31; N, 6.00; S, 6.86.

[0986] Compound Number II-214

[0987] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50-2.42(14H, m), 2.33(3H, s), 3.82(3H, s), 4.07(2H, s), 4.18 (1H, m), 5.33-5.48(2H, m), 5.96(1H, d, J=8.7 Hz), 6.69(1H, s), 6.74 (1H, d, J=7.8 Hz), 6.76(1H, d, J=3.6 Hz), 7.03(1H, d, J=7.8 Hz), 7.28 (1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3450, 3431, 1741, 1709, 1639, 1614, 1543, 1506, 1464 cm−1. [α]D24+43.3±0.8°(c=1.012, MeOH), Anal. (C30H39NO4S.0.1H2O) Calcd.(%): C, 70.45; H, 7.73; N, 2.74; S, 6.27. Found(%): C, 70.35; H, 7.78; N, 2.96; S, 6.20.

[0988] Compound Number II-215

[0989] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.07 and 1.21(each 3H, each s),1.49-2.43(14H, m), 3.84(3H, s), 4.20(1H, m), 4.32(2H, s), 5.33-5.48(2H, m), 5.99(1H, d, J=8.4 Hz), 6.83(1H, d, J=3.6 Hz), 7.01 (1:H, dd, J=2.4 and 8.7 Hz), 7.12(1H, d,J=2.4 Hz), 7.21(1H, s), 7.31 (1H, d, J=3.6 Hz), 7.71(1H, d, J=8.7 Hz). IR(CDCl3): 3516, 3450, 3431, 1739, 1709, 1643, 1601, 1543, 1508, 1458, 1427 cm−1. [α]D25+38.5±0.8°(c=1.004, MeOH), Anal. (C31H37NO4S2.0.1H2O) Calcd.(%): C, 67.26; H, 6.72; N, 2.53; S, 11.58. Found(%): C, 67.24; H, 6.73; N, 2.77; S, 11.51.

[0990] Compound Number II-216

[0991] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.07 and 1.20(each 3H, each s), 1.50-2.42(14H, m), 3.87(2H, s), 4.18(1H, m), 4.20(2H, s), 5.32-5.48 (2H, m), 5.98(1H, d, J=7.2 Hz), 6.81(1H, d, J=3.6 Hz), 7.23-7.41 (5H, m), 7.53(1H, d, J=7.5 Hz), 7.71-7.77(2H, m). IR(CHCl3): 3514, 3450, 3431, 1739, 1709, 1641, 1545, 1506, 1469, 1456 cm−1. [α]D25+38.5±0.8°(c=1.007, MeOH) Anal. (C35H39NO3S.0.2H2O) Calcd.(%): C, 75.42; H, 7.13; N, 2.51; S, 5.75. Found(%): C, 75.36; H, 7.18; N, 2.79; S, 5.50.

[0992] Compound Number II-217

[0993] 1 H-NMR(CDCl3) δ: 0.96(1H, d, J=10.2 Hz), 1.10 and 1.21(each 3H, each s), 1.52-2.44(14H, m), 3.14-3.24(4H, m), 4.13(2H, s), 4.24(1H, m), 5.32-5.49(2H, m), 6.19(1H, d, J=9.0 Hz), 7.06-7.18(4H, m), 7.22 (1H, d, J=8.1 H), 7.39(1H, dd, J=1.8 and 8.1 Hz), 7.51(1H, d, J=1.8 Hz). IR(CHCl3): 3516, 3452, 1738, 1709, 1649, 1570, 1518, 1491, 1471 cm−1. [α]D25+54.4±0.9°(c=1.002, MeOH) Anal. (C32H39NO4.0.1H2O) Calcd.(%): C, 78.85; H, 8.11.; N, 2.87. Found(%): C, 78.74; H, 8.14; N, 3.17.

[0994] Compound Number II-218

[0995] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.43(14H, m), 3.83, 3.85 and 3.86(each 3H, each s), 4.07 (2H, s), 4.19(1H, m), 5.33-5.49(2H, m), 5.97(1H, d, J=9.0 Hz), 6.62 (1H, d, J=8.7 Hz), 6.76(1H, td, J=0.9 and 3.6 Hz), 6.87(1H, d, J=8.7 Hz), 7.30 (1H, d, (1, J=3.6 Hz). IR(CHCl3): 3516, 3450, 3431, 1739, 1709, 1641, 1603, 1543, 1495, 1469, 1277, 1259, 1097 cm−1. [α]D26+38.4±0.8°(c=1.013, MeOH) Anal. (C31H41NO6S.0.2H2O) Calcd.(%): C, 66.57; H, 7.46; N, 2.50; S, 5.73. Found(%): C, 66.54; H, 7.42; N, 2.61; S, 5.71.

[0996] Compound Number II-219

[0997] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.42(14H, m), 2.18 and 2.29(each 3H, each s), 4.14(2H, s), 4.19(1H, m), 5.33-5.49(2H, m), 5.96(1H, d, J=8.4 Hz), 6.67(1H, td, J=0.9 and 3.6 Hz), 7.02-7.12(3H, m), 7.29(1H, t, J=3.6 Hz). IR (CDCl3): 3516, 3450, 3431, 1741, 1709, 1641, 1543, 1506, 1471 cm−1. [α]D26+42.8±0.8°(c=1.007, MeOH) Anal. (C30H39NO3S) Calcd.(%): C, 72.98; H, 7.96; N, 2.84; S, 6.50. Found(%): C, 72.67; H, 7.98; N, 2.94; S, 6.38.

[0998] Compound Number II-220

[0999] 1 H-NMR(CDCl3) δ: 0.95(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s), 1.51-2.44(14H, m), 3.83(3H, s), 3.84(6H, s), 4.07(2H, s), 4.20 (1H, m), 5.34-5.49(2H, m), 6.00(1H, d, J=8.7 Hz), 6.45(2H, s), 6.79 and 7.31 (each 1H, each d, each J=3.6 Hz). IR(CHCl3): 3516, 3450, 3431, 1741, 1709, 1641, 1593, 1543, 1506, 1464, 1421, 1331, 1240, 1130 cm−1. [α]D24+38.3±0.8°(c=1.004, MeOH) Anal. (C31H41NO6S.0.2H2O) Calcd.(%): C, 66.57; H, 7.46; N, 2.50; S, 5.73. Found(%): C, 66.48; H, 7.37; N, 2.59; S, 5.63.

[1000] Compound Number II-221

[1001] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.43(14H, m), 4.08(2H, s), 4.20(1H, m), 5.33-5.49(2H, m), 5.95(2H, s), 5.99(1H, d, J=8.7 Hz), 6.68-6.82(4H, m), 7.30(1H, d, J=3.6 Hz). IR(CHCl3): 3512, 3450, 3431, 1739, 1709, 1641, 1545, 1506, 1460, 1252, 1063 cm−1. [α]D24+41.8±0.8°(c=1.007, MeOH) Anal. (C29H35NO5S) Calcd.(%): C, 68.34; H, 6.92; N, 2.75; S, 6.29. Found(%): C, 68.04; H, 6.90; N, 2.79; S, 6.29.

[1002] Compound Number II-222

[1003] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.5 Hz), 1.09 and 1.21(each 3H, each s), 1.51-2.45(14H, m), 2.14(3H, s), 4.08(2H, s), 4.18(1H, m), 5.32-5.50 (2H, m), 6.08(1H, d, J=8.4 Hz), 6.76(1H, d, J=3.6 Hz), 6.97 (1H, d, J=7.8 Hz), 7.24(1H, t, J=8.4 Hz), 7.30(1H, d, J=3.6 Hz), 7.38-7.40 (2H, m), 7.74(1H, br s). IR(CHCl3): 3514, 3435, 3311, 1705, 1639, 1612, 1534, 1508, 1439 cm−1. [α]D25+40.1±0.8°(c=1.008, MeOH) Anal. (C30H38N2O4S.0.4H2O) Calcd.(%): C, 68.00; H, 7.38; N, 5.29; S, 6.05. Found(%): C, 68.11; H, 7.17; N, 5.22; S, 5.93.

[1004] Compound Number II-223

[1005] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s), 1.53-2.50(14H, m), 2.99(3H, s), 4.13(2H, s), 4.21(1H, m), 5.34-5.52 (2H, m), 6.02(1H, d, J=9.3 Hz), 6.80(1H, d, J=3.9 Hz), 7.04-7.07(2H, m), 7.16(1H, m), 7.25-7.32(3H, m). IR(CHCl3): 3510, 3440, 3431, 3371, 1709, 1639, 1608, 1543, 1508, 1471, 1386, 1335, 1151 cm−1. [α]D24+38.3±0.8°(c=1.006, MeOH) Anal. (C29H38N2O5S2.0.2H2O) Calcd.(%): C, 61.94; H, 6.88; N, 4.98; S, 11.40. Found(%): C, 61.99; H, 6.92; N, 4.95; S, 10.97.

[1006] Compound Number II-224

[1007] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s), 1.50-2.44(14H, m), 4.21(1H, m), 4.32(2H, s), 5.34-5.50(2H, m), 6.01(1H, d, J=9.0 Hz), 6.86, 6.88 and 7.14(each 1H, each d, each J=3.6 Hz), 7.23-7.37(4H, m), 7.53-7.56(2H, m).

[1008] Compound Number II-225

[1009] 1 H-NMR(CDCl3) δ: 0.94 (1H, d, J=10.2 Hz), 1.08 and 1.21(each 311, each s), 1.50-2.43(14H, m), 4.08(2H, s), 4.17-4.30(5H, m), 5.33-5.49 (2H, m), 5.98(1H, d, J=8.4 Hz), 6.71-6.80(4H, m), 7.28(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3450, 3431, 1739, 1709, 1639, 1602, 1543, 1506, 1475, 1456, 1284, 1090 cm−1. [α]D24.5+40.2±0.8°(c=1.011, MeOH) Anal. (C30H37NO5S.0.2H2O) Calcd.(%): C, 68.34; H, 7.15; N, 2.66; S, 6.08. Found(%): C, 68.35; H, 7.03; N, 2.71; S, 6.17.

[1010] Compound Number II-226

[1011] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.43(14H, m), 2.31 and 3.70(each 3H, each s), 4.15(2H, s), 4.19(1H, m), 5.33-5.49(2H, m), 5.98(1H, d, J=8.7 Hz), 6.77(1H, d, J=3.9 Hz), 6.96-7.11(3H, m), 7.31(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3450, 3431, 2669, 1738, 1709, 1641, 1545, 1506, 1471, 1259, 1011 cm−1. [α]D24+41.2±0.8°(c=1.003, MeOH) Anal. (C30H39NO4S) Calcd.(%): C, 70.69; H, 7.71; N, 2.75; S, 6.29. Found(%): C, 70.41; H, 7.76; N, 2.97; S, 6.04.

[1012] Compound Number II-227

[1013] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.51-2.42(14H, m), 2.16(3H, s), 4.09(2H, s), 4.18(1H, m), 5.32-5.50 (2H, m), 6.01(1H, d, J=8.7 Hz), 6.77(1H, d, J=3.6 Hz), 7.17 (2H, d, J=8.1 Hz), 7.32(1H, d, J=3.6 Hz), 7.43(1H, br s), 7.44(2H, d, J=8.1 Hz). IR(CHCl3): 3514, 3435, 3311, 1705, 1639, 1541, 1513, 1410 cm−1. [α]D24.5+40.8±0.8°(c=1.000, MeOH) Anal. (C30H38N2O4S.0.4H2O) Calcd.(%): C, 68.00; H, 7.38; N, 5.29; S, 6.05. Found(%): C, 68.06; H, 7.38; N, 5.28; S, 5.92.

[1014] Compound Number II-228

[1015] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.21(each 3H, each s), 1.51-2.42(14H, m), 2.99(3H, s), 4.11(2H, s), 4.20(1H, m), 5.33-5.49(2H, m), 6.01(1H, d, J=9.3 Hz), 6.78(1H, d, J=3.6 Hz), 6.86 (1H, br s), 7.17-7.25(4H, m), 7.31(1H, d, J=3.6 Hz). IR(CHCl3): 3510, 3448, 3431, 3371, 1707, 1639, 1543, 1510, 1471, 1456, 1387, 1330, 1155 cm−1. [α]D24.5+37.6±0.8°(c=1.006, MeOH) Anal. (C29H38N2O5S2.0.3H2O) Calcd.(%): C, 61.74; H, 6.90; N, 4.97; S, 11.37. Found(%): C, 61.84; H, 6.93; N, 5.03; S, 11.14.

[1016] Compound Number II-229

[1017] mp.149-150° C. 1H-NMR(CDCl3) δ: 0.92(1H, d, J=10.5 Hz), 1.05 and 1.19(each 3H, each s), 1.47-2.40(14H, m), 4.18(1H, m), 4.40 (2H, s), 5.31-5.46(2H, m), 5.98(1H, d, J=8.4 Hz), 6.88(1H, d, J=3.9 Hz), 7.30-7.35(2H, m), 7.42-7.48(3H, m), 7.58(1H, m), 8.08(1H, d, J=6.6 Hz), 8.14(1H, m). IR(CHCl3): 3514, 3450, 3431, 2667, 1738, 1707, 1643, 1543, 1508, 1471, 1458, 1444 cm−1. [α]D24.5+39.7±0.8°(c=1.008, MeOH) Anal. (C34H37NO3S2) Calcd.(%): C, 71.42; H, 6.52; N, 2.45; S, 11.22. Found(%): C, 71.21; H, 6.53; N, 2.51; S, 10.97.

[1018] Compound Number II-230

[1019] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.5 Hz), 1.06 and 1.19(each 3H, each s), 1.48-2.40(14H, m), 3.79(2H, s), 4.18(1H, m), 4.26(2H, s), 5.21-5.47(2H, m), 5.96(1H, d, J=8.4 Hz), 6.78(1H, d, J=3.6 Hz), 7.18 (1H, d, J=7.2 Hz), 7.27-7.40(4H, m), 7.53(1H, d, J=7.2 Hz), 7.72(1H, d, J=7.8 Hz), 7.78(1H, d, J=6.9 Hz). IR(CHCl3): 3510, 3450, 3431, 2669, 1739, 1709, 1641, 1543, 1506, 1471, 1456 cm−1. [α]D24+36.6±0.8°(c=1.006, MeOH) Anal. (C35H39NO3S.0.2H2O) Calcd.(%): C, 75.42; H, 7.13; N, 2.51; S, 5.75. Found(%): C, 75.46; H, 7.15; N, 2.73; S, 5.55.

[1020] Compound Number II-231

[1021] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=9.9 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.43(14H, m), 2.20, 2.45 and 3.67(each 3H, each s), 4.13 (2H, s), 4.19(1H, m), 5.33-5.49(2H, m), 5.97(1H, d, J=8.4 Hz), 6.77 (1H, td, J=0.9 and 3.9 Hz), 6.89 and 6.95(each 1H, each d, each J=7.8 Hz), 7.31(1H, d, J=3.6 Hz). IR(CHCl3): 3516, 3450, 3431, 1738, 1709, 1641, 1545, 1506, 1458, 1263, 1084, 1009 cm−1. [α]D24+39.8±0.8°(c=1.006, MeOH) Anal. (C31H41NO4S) Calcd.(%): C, 71.09; H, 7.89; N, 2.67; S, 6.12. Found(%): C, 70.80; H, 8.02; N, 2.92; S, 6.06.

[1022] Compound Number II-232

[1023] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.06 and 1.19(each 3H, each s), 1.49-2.41(14H, m), 4.18(1H, m), 4.50(2H, s), 5.32-5.47(2H, m), 5.98(1H, d, J=9.0 Hz), 6.89(1H, d, J=3.9 Hz), 7.29-7.38(4H, m), 7.47 (1H, m), 7.59(1H, d, J=8.4 Hz), 7.86(1H, m), 7.95(1H, d, J=7.8 Hz). IR(CHCl3): 3510, 3450, 3431, 2669, 1739, 1709, 1641, 1545, 1508, 1471, 1450, 1423 cm−1. [α]D24+40.3±0.8°(c=1.007, MeOH) Anal. (C34H37NO4S.0.2H2O) Calcd.(%): C, 73.01; H, 6.74; N, 2.50; S, 5.73. Found(%): C, 72.91; 11, 6.58; N, 2.59; S, 5.75.

[1024] Compound Number II-233

[1025] 1 H-NMR(CDCl3) δ: 0.92(1H, d, J=10.2 Hz), 1.08 and 1 .20(each 3H, each s),1.50-2.43(14H, m), 4.04(2H, s), 4.20(1H, m), 5.32-5.49(2H, m), 6.03(1H, d, J=9.0 Hz), 6.75(1H, d, J=3.6 Hz), 6.80 and 7.06(each 2H, each d, J=8.7 Hz), 7.32(1H, d, J=3.6 Hz). IR(CHCl3): 3446, 3510, 3182, 2673, 1709, 1635, 1614, 1545, 1512, 1471, 1458 cm−1. [α]D25+43.8±0.8°(c=1.000, MeOH), Anal. (C28H35NO4S) Calcd.(%): C, 69.82; H, 7.32; N, 2.91; S, 6.66. Found(%): C, 69.57; H, 7.43; N, 3.00; S, 6.61.

[1026] Compound Number II-295

[1027] mp.156-157° C. 1H-NMR(CDCl3) δ: 1.00(1H, d, J=10.2 Hz), 1.17 and 1.25 (each 3H, each s), 1.57-2.51(14H, m), 4.31(1H, m), 5.34-5.54(2H, m), 6.37(1H, d, J=9.3 Hz), 7.33-7.47(3H, m), 7.61(1H, s), 7.64(1H, m), 7.70-7.73 (2H, m), 7.87(1H, d, J=8.4 Hz), 8.15(1H, d, J=1.2 Hz). IR (CHCl3); 3518, 3452, 1741, 1709, 1649, 1510 cm−1. [α]D23+67.2±2.1°(c=0.503, MeOH) Anal. (C31H35NO3S.0.1H2O) Calcd.(%): C, 73.95; H, 7.05; N, 2.78; S, 6.37. Found(%): C, 73.94; H, 7.08; N, 3.04; S, 6.53.

[1028] Compound Number II-296

[1029] mp.126-127° C. 1H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.20(each 3H, each s), 1.50-2.46(14H, m), 4.17(1H, m), 5.33-5.51(2H, m), 6.04(1H, d, J=8.4 Hz), 6.51(1H, dd, J=1.5 and 3.3 Hz), 7.13(1H, dd, J=2.7 and 3.3 Hz), 7.22(1H, dd, J=7.8 and 9.0 Hz), 7.73(1H, dd, J=1.5 and 2.1 Hz), 7.91-7.96(2H, m). IR(CHCl3): 3513, 3449, 3144, 1733, 1709, 1651, 1592, 1507, 1496, 1385, 1181 cm−1. [α]D24+36.2±0.8°(c=1.005, MeOH) Anal. (C27H33FN2O5S) Calcd.(%): C, 62.77; H, 6.44; N, 5.42; F, 3.68; S, 6.21. Found(%): C, 62.71; H, 6.49; N, 5.39; F, 3.69; S, 6.21.

[1030] Compound Number II-297

[1031] mp.145-146° C. 1H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.20(each 3H, each s), 1.50-2.45(14H, m), 3.86(3H, s), 4.17(1H, m), 5.33-5.51 (2H, m), 6.04(1H, d, J=8.4 Hz), 6.48(1H, dd, J=1.5 and 3.3 Hz), 6.98 and 7.85(each 2H, each d, each J=9.0 Hz), 7.12(1H, dd, J=2.7 and 3.3 Hz), 7.71(1H, dd, J=1.8 and 2.1 Hz). IR(CHCl3): 3513, 3449, 3413, 3143, 1733, 1709, 1649, 1596, 1576, 1499, 1379, 1266, 1189, 1167 cm−1. [α]D24+34.5±0.7°(c=1.005, MeOH) Anal. (C28H36N2O6S) Calcd.(%): C, 63.61; H, 6.86; N, 5.30; S, 6.07. Found(%): C, 63.54; H, 6.93; N, 5.18; S, 6.08.

[1032] Compound Number II-298

[1033] 1 H-NMR(CDCl3) δ: 0.97(1H, d, J=10.5 Hz), 1.12 and 1.23(each 3H, each s), 1.50-2.50(14H, m), 4.23(1H, m), 5.39-5.51(2H, m), 6.09(1H, d, J=9.6 Hz), 6.35(1H, dd, J=2.4 and 3.9 Hz), 6.48(1H, dd, J=2.4 and 3.9 Hz), 7.02(1H, dd, J=3.6 and 4.8 Hz), 7.18(1H, dd, J=0.6 and 4.8 Hz), 7.41(1H, dd, J=0.6 and 3.6 Hz), 10.92(1H, brs). IR(CHCl3): 3506, 3447, 3220, 3164, 1704, 1617, 1537, 1508 cm−1. [α]D24+50.7±0.9°(c=1.009, MeOH) Anal. (C25H32N2O3S.0.2H2O) Calcd.(%): C, 67.59; H, 7.35; N, 6.31; S, 7.22. Found(%): C, 67.60; H, 7.23; N, 6.39; S, 7.34.

[1034] Compound Number II-299

[1035] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.44(14H, m), 2.27(3H, s), 4.05(2H, s), 4.20(1H, m), 5.33-5.49(2H, m), 6.01(1H, d, J=8.7 Hz), 6.71(1H, d, J=3.9 Hz), 7.09 (1H, dd, J=1.2 and 7.8 Hz), 7.17-7.32(3H, m), 7.28(1H, d, J=3.9 Hz). IR(CHCl3): 3516, 3450, 3431, 2669, 1747, 1709, 1641, 1543, 1506, 1456, 1369 cm−1. [α]D24+40.2°±0.8°(c=1.006, MeOH) Anal. (C30H37NO5S.0.2H2O) Calcd.(%): C, 68.34; H, 7.15; N, 2.66; S, 6.08. Found(%): C, 68.33; H, 6.94; N, 2.83; S, 6.31.

[1036] Compound Number II-300

[1037] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=9.9 Hz), 1.08 and 1.21(each 3H, each s), 1.50-2.41(14H, m), 2.60(3H, s), 4.20(1H, m), 5.34-5.48(2H, m), 6.18(1H, d, J=8.7 Hz), 7.28(1H, d-like), 7.36(1H, d, J=3.9 Hz), 7.40 (1H, t-like), 7.51(1H, dt, J=1.2 and 7.2 Hz), 7.61(1H, d, J=3.9 Hz), 8.15(1H, dd, J=1.2 and 8.1 Hz). IR(CHCl3): 3512, 3446, 1739, 1709, 1655, 1529, 1504, 1325, 1157 cm−1. [α]D24+51.1±0.9°(c=1.010, MeOH) Anal. (C28H35NO5S2) Calcd.(%): C, 63.49; H, 6.66; N, 2.64; S, 12.11. Found(%): C, 63.23; H, 6.53; N, 2.70; S, 12.17.

[1038] Compound Number II-301

[1039] 1 H-NMR(CDCl3) δ: 0.93(1H, d, J=10.2 Hz), 1.07 and 1.21(each 3H, each s), 1.50-2.40(14H, m), 2.42(3H, s), 4.20(1H, m), 5.34-5.47(2H, m), 6.17(1H, d, J=8.7 Hz), 7.32(1H, d-like), 7.34 and 7.57(each 1H, each d, each J=4.2 Hz), 7.86(2H, d-like). IR(CDCl3): 3512, 3446, 1741, 1707, 1655, 1529, 1504, 1331, 1153 cm−1. [α]D24+54.9±0.9°(c=1.008, MeOH) Anal. (C28H35NO5S2) Calcd.(%): C, 63.49; H, 6.66; N, 2.64; S, 12.11. Found(%): C, 63.16; H, 6.54; N, 2.70; S, 12.16.

[1040] Compound Number II-302

[1041] 1 H-NMR(CDCl3) δ: 0.96(1H, d, J=10.2 Hz), 1.14 and 1.25(each 3H, each s),1.53-2.47(14H, m), 4.25(1H, m), 5.37-5.52(2H, m), 6.23(1H, d, J=8.7 Hz), 7.16-7.22(2H, m), 7.36(1H, m), 7.46(1H, s), 7.45-7.49(1H, m). IR(CHCl3): 3516, 3446, 3429, 1734, 1703, 1652, 1606, 1521, 1496, 1457, 1419 cm−1. [α]D25+72.8°±1.1°(c=1.005, MeOH), Anal. (C28H31NO4S.0.3H2O) Calcd.(%): C, 69.63; H, 6.59; N, 2.90; S, 6.63. Found(%): C, 69.51; H, 6.72; N, 3.30; S, 6.56.

[1042] Compound Number III-1

[1043] 1 H-NMR(CDCl3) δ: 0.88(1H, d, J=10.2 Hz), 1.07 and 1.23(each 3H, each s), 1.56-2.51(13H, m), 2.67(1H, m), 4.41(1H, m), 5.29-5.41(2H, m), 6.07(1H, d, J=8.1 Hz), 6.34 and 7.16(each 2H, each t, each J=2.1 Hz), 7.35 and 7.52(each 1H, each d, each J=3.9 Hz). IR (CHCl3): 3511, 3431, 3144, .3101, 2668, 1708, 1656, 1530, 1505, 1455, 1384, 1167 cm−1. [α]D24+34.2±0.7°(c=1.007, MeOH) Anal. (C25H32N2O5S2.0.5H2O) Calcd.(%): C, 58.46; H, 6.48; N, 5.45; S, 12.48. Found(%): C, 58.77; H, 6.40; N, 5.65; S, 12.72.

[1044] Compound Number III-47

[1045] 1 H-NMR(CDCl3) δ: 0.94(1H, d, J=9.9 Hz), 1.07 and 1.23(each 3H, each s), 1.56-2.48(13H, m), 2.68(1H, m), 4.42(1H, m), 5.29-5.42(2H, m), 6.16(1H, d, J=8.4 Hz), 7.16(1H, dd, J=3.9 and 5.1 Hz), 7.42 and 7.63(each 1H, each d, each J=3.9 Hz), 7.70(1H, dd, J=1.5 and 5.1 Hz), 7.76(1H, dd, J=1.5 and 3.9 Hz). IR (CHCl3): 3516, 3431, 3365, 3097, 1708, 1654, 1530, 1505, 1402, 1336, 1153 cm−1. [α]D24+34.5±0.7°(c=1.010, MeOH) Anal. (C25H31NO5S3.0.1H2O) Calcd.(%): C, 57.36; H, 6.01; N, 2.68; S, 18.38. Found(%): C, 57.16; H, 5.88; N, 2.76; S, 18.36.

[1046] Compound Number III-55

[1047] 1 H-NMR (CDCl3) δ: 0.88(1H, d, J=9.9 Hz), 1.07 and 1.23(each 3H, each s), 1.58-2.34(12H, m), 2.39(3H, s), 2.44(1H, m), 2.68(1H, m), 4.41(1H, m), 5.29-5.42(2H, m), 5.99(1H, m), 6.08(1H, d, J=8.4 Hz), 6.20(1H, t, J=3.3 Hz), 7.19(1H, m), 7.38 and 7.55(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3510, 3431, 3150, 3100, 1708, 1656, 1530, 1505, 1375, 1161 cm−1. [α]D24+30.9±0.7°(c=1.000, MeOH) Anal. (C26H34N2O5S2.0.3H2O) Calcd.(%): C, 59.58; H, 6.65; N, 5.35; 12.24. Found(%): C, 59.57; H, 6.48; N, 5.51; S, 12.22.

[1048] Compound Number III-80

[1049] 1 H-NMR(CDCl3) δ: 0.90(1H, d, J=9.9 Hz), 1.06 and 1.23(each 3H, each s), 1.58-2.48(13H, m), 2.67(1H, m), 4.41(1H, m), 5.29-5.42(2H, m), 6.27(1H, d, J=8.1 Hz), 7.38-7.44(3H, m), 6.34(1H, d, J=3.9 Hz), 8.14(1H, dd, J=1.5 and 3.0 Hz). IR(CHCl3): 3517, 3431, 3361, 3114, 1708, 1654, 1530, 1504, 1332. 1151 cm−1. [α]D24+33.7±0.7°(c=1.003, MeOH) Anal. (C25H31NO5S3.0.2H2O) Calcd.(%): C, 57.16; H, 6.02; N, 2.67; S, 18.31. Found(%): C, 57.09; H, 5.88; N, 2.76; S, 18.15.

[1050] Compound Number IV-1

[1051] 1 H-NMR(CDCl3) δ: 0.84 and 1.22(each 3H, each s), 1.43(1H, d, J=10.5 Hz), 1.53-2.50(14H, m), 4.09(1H, m), 5.30-5.41(2H, m), 6.17 (1H, d, J=8.7 Hz) 6.33 and 7.16(each 2H, each t-like), 7.40 and 7.57 (each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3514, 3432, 3144, 3102, 1708, 1657, 1531, 1506, 1456, 1384, 1167 cm−1. [α]D23−45.4±0.9°(c=1.010, MeOH) Anal. (C25H30N2O5S2.0.3H2O) Calcd.(%): C, 59.10; H, 6.07; N, 5.51; S, 12.62. Found(%): C, 59.12; H, 5.83; N, 5.53; S, 12.41.

[1052] Compound Number IV-47

[1053] 1 H-NMR(CDCl3) δ: 0.85 and 1.22(each 3H, each s), 1.44(1H, d, J=10.2 Hz), 1.54-2.51(14H, m), 4.10(1H, m), 5.31-5.41(2H, m), 6.21 (1H, d, J=8.4 Hz), 7.11(1H, dd, J=3.9 and 4.8 Hz), 7.44 and 7.63 (each 1H, each d, each J=3.9 Hz), 7.70(1H, dd, J=1.2 and 4.8 Hz), 7.75 (1H, dd, J=1.2 and 3.9 Hz). IR(CHCl3): 3517, 3423, 3366, 3097, 2665, 1708, 1655, 1530, 1505, 1335, 1153 cm−1. [α]D23−46.4±0.9°(c=1.010, MeOH) Anal. (C25H31NO5S3.0.3H2O) Calcd.(%): C, 56.97; H, 6.04; N, 2.66; S, 18.25. Found(%): C, 57.10; H, 5.96; N, 2.70; S, 18.02.

[1054] Compound Number V-88

[1055] mp.105-106° C.; 1H-NMR(CDCl3) δ: 1.06(1H, m), 1.19-1.29(2H, m), 1.42-1.47(2H, m), 1.58-1.78(4H, m), 2.00-2.19(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.82(1H, m), 4.16(2H, s), 5.30-5.42(2H, m), 5.99(1H, d, J=7.5 Hz), 6.79(1H, dt, J=0.9 and 3.9 Hz), 6.96(1H, dd, J=1.5 and 4.8 Hz), 7.05(1H, m), 7.28(1H, dd, J=3.0 and 4.8 Hz), 7.37(1H. d, J=3.9 Hz). IR(KBr): 3367, 2667, 1700, 1612, 1543, 1520, 1317, 1244 cm−1. [α]D24+70.2±1.1°(c=1.006, MeOH) Anal. (C24H29NO3S2) Calcd.(%): C, 64.98; H, 6.59; N, 3.16; S, 14.46. Found(%): C, 64.92; H, 6.52; N, 3.32; S, 14.48.

[1056] Compound Number VI-1

[1057] 1 H-NMR(CDCl3) δ: 1.24-2.13(13H, m), 2.22(1H, m), 2.32(2H, t, J=7.2 Hz), 3.41(1H, m), 3.44(1H, m), 5.18-5.36(2H, m), 6.19(1H, m), 6.33 and 7.15(each 2H, each t, each J=2.4 Hz), 7.28 and 7.55(each 2H, each t, each J=3.9 Hz). IR(CHCl3): 3512, 3439, 3144, 3100, 1708, 1658, 1535, 1508, 1446, 1167 cm−1. [α]D26+69.5±1.1°(c=1.012, MeOH) Anal. (C23H28N2O5S.0.5H2O) Calcd.(%): C, 56.89; H, 6.02; N, 5.77; S, 13.21. Found(%): C, 56.91; H, 5.96; N, 5.91; S, 13.37.

[1058] Compound Number VI-31

[1059] 1 H-NMR(CDCl3) δ: 1.18-2.10(13H, m), 2.11(1H, m), 2.21-2.35(2H, m), 3.35(1H, m), 3.46(1H, m), 4.12(2H, s), 5.17-5.34(2H, m), 5.88(1H, m), 6.74(1H, d, J=3.9 Hz), 7.21-7.38(6H, m). IR(CHCl3): 3511, 3432, 3065, 1708, 1642, 1547, 1515, 1455 cm−1. [α]D2330 69.1±1.1°(c=1.009, MeOH) Anal. (C26H31NO3S.0.1H2O) Calcd.(%): C, 71.07; H, 7.16; N, 3.19; S, 7.30. Found(%): C, 70.91; H, 7.18; N, 3.19; S, 7.34.

[1060] Compound Number VI-40

[1061] 1 H-NMR(CDCl3) δ: 1.18-2.15(14H, m), 2.24-2.34(2H, m), 3.36(1H, m), 3.58(1H, m), 5.19-5.40(2H, m), 6.07(1H, m), 7.28-7.42(3H, m), 7.51(1H, d, J=0.6 Hz), 7.56-7.59(2H, m), 7.72(1H, d, J=0.6 Hz). IR (CHCl3): 3514, 3446, 1709, 1649, 1550, 1520, 1491 cm−1. [α]D22+79.4±1.2°(c=1.004, MeOH) Anal. (C25H29NO3S.0.2H2O) Calcd.(%): C, 70.29; H, 6.94; N, 3.28; S, 7.51. Found(%): C, 70.26; H, 6.68; N, 3.48; S, 7.44.

[1062] Compound Number VI-47

[1063] 1 H-NMR(CDCl3) δ: 1.14-2.16(13H, m), 2.23(1H, m), 2.30-2.37(2H, m), 3.41(1H, m), 3.45(1H, m), 5.18-5.36(2H, m), 6.19(1H, m), 7.11 (1H, dd, J=3.9 and 5.1 Hz), 7.32 and 7.62(each 1H, each d, each J=3.9 Hz), 7.39(1H, dd, J=1.5 and 5.1 Hz), 7.75(1H, dd, J=1.5 and 3.9 Hz). IR(CHCl3): 3512, 3440, 3096, 1708, 1657, 1534, 1507, 1402, 1336, 1153 cm−1. [α]D25+69.2±1.1°(c=1.006, MeOH) Anal. (C23H27NO5S3.0.1H2O) Calcd.(%): C, 55.57; H, 5.51; N, 2.83; S, 19.42. Found(%): C, 55.55; H, 5.32; N, 2.85; S, 19.21.

[1064] Compound Number VI-55

[1065] 1 H-NMR(CDCl3) δ: 1.18-2.18(13H, m), 2.23(1H, m), 2.31-2.35 (2H, m), 2.38(3H, s), 3.43(2H, m), 5.18-5.36(2H, m), 5.98(1H, m), 6.14(1H, m), 6.19(1H, t, J=3.3 Hz), 7.17(1H, m), 7.29 and 7.53(each 1H, each d, each J=3.9 Hz). IR(CHCl3): 3512 3440, 3150, 3101, 1708, 1658, 1535, 1508, 1375, 1161 cm−1. [α]D24+30.9±0.7°(c=1.000, MeOH) Anal. (C26H34N2O5S2.0.3H2O) Calcd.(%): C, 59.58; H, 6.65; N, 5.35; S, 12.24. Found(%): C, 59.57; H, 6.48; N, 5.51; S, 12.22.

[1066] Compound Number VI-80

[1067] 1 H-NMR(CDCl3) δ: 1.16-2.14(13H, m), 2.23(1H, m), 2.28-2.36(2H, m), 3.54-3.46(2H, m), 5.17-5.37(2H, m), 6.14(1H, m), 7.32(1H, d, J=3.9 Hz), 7.38-7.44(2H, m), 7.61(1H, d, J=3.9 Hz), 8.15(1H, dd, J=1.2 and 3.0 Hz). IR(CHCl3): 3508, 3431, 3114, 1708, 1656, 1534, 1508, 1331, 1152, 1102cm−1. [α]D24+66.5±1.1°(c=1.003, MeOH) Anal. (C23H27NO5S3.0.3H2O) Calcd.(%): C, 55.35; H, 5.57; N, 2.81; S, 19.28. Found(%): C, 55.29; H, 5.54; N, 2.85; S, 19.01.

[1068] Compound Number VI-104

[1069] 1 H-NMR(CDCl3) δ: 1.18-2.14(13H, m), 2.25(1H, m), 2.31-2.39(2H, m), 3.32(2H, m), 3.56(1H, m), 4.09(2H, d, J=0.3 Hz), 5.18-5.38(2H, m), 5.89(1H, m), 6.68(1H, d, J=3.6 Hz), 6.94(1H, dd, J=3.6 and 5.1 Hz), 7.02(1H, dd, J=1.5 and 3.6 Hz), 7.23(1H, d, J=3.6 Hz), 7.35(1H, dd, J=1.5 and 5.1 Hz). IR(CHCl3): 3514, 3433, 1709, 1645, 1545, 1516, 1458 cm−1. [α]D23+61.8±1.0°(c=1.008, MeOH) Anal. (C24H29NO3S3.0.2H2O) Calcd.(%): C, 60.14; H, 6.18; N, 2.92; S, 20.07. Found(%): C, 60.08; H, 6.11; N, 2.90; S, 20.05.

[1070] Compound Number VI-122

[1071] 1 H-NMR(CDCl3) δ: 1.06-2.15(13H, m), 2.27(1H, m), 2.28-2.38(2H, m), 3.31(1H, m), 3.54(1H, m), 4.24(2H, d, J=0.6 Hz), 5.17-5.36(2H, m), 5.87(1H, m), 6.78(1H, d, J=3.6 Hz), 7.21-7.42(6H, m). IR(CHCl3): 3514, 3433, 3062, 2669, 1709, 1643, 1545, 1514 cm−1. [α]D22+64.3±1.0°(c=1.000, MeOH) Anal. (C26H31NO3S2.0.5H2O) Calcd.(%): C, 65.24; H, 6.74; N, 2.93; S, 13.40. Found(%): C, 65.23; H, 6.55; N, 3.00; S, 13.46.

[1072] Compound Number VI-123

[1073] 1 H-NMR(CDCl3) δ: 1.06-2.15(13H, m), 2.23(1H, m), 2.28-2.38(2H, m), 3.35(1H, m), 3.54(1H, m), 5.20(2H, s), 5.19-5.37(2H, m), 5.95(1H, m), 6.94-7.04(4H, m), 7.27-7.35(3H, m). IR(CHCl3): 3514, 3433, 1709, 1647, 1599, 1547, 1518, 1495 cm−1. [α]D24+67.8±1.1°(c=1.008, MeOH) Anal. (C26H31NO4S.0.2H2O) Calcd.(%): C, 68.30; H, 6.92; N, 3.06; S, 7.01. Found(%): C, 68.31; H, 6.84; N, 3.16; S, 7.11.

[1074] Compound Number VI-124

[1075] 1 H-NMR(CDCl3) δ: 1.06-2.14(13H, m), 2.24(1H, m), 2.30-2.37(2H, m), 3.31(1H, m), 3.53(1H, m), 4.50(2H, d, J=0.9 Hz), 5.15-5.36(2H, m), 5.89(1H, m), 6.65-6.79(3H, m), 6.95(1H, d, J=3.9 Hz), 7.15-7.21 (2H, m), 7.33(1H, d, J=3.9 Hz). IR(CHCl3): 3512, 3440, 1707, 1643, 1603, 1547, 1506 cm−1. [α]D22+67.3±1.1°(c=1.009, MeOH) Anal. (C26H32N2O3S.0.3H2) Calcd.(%): C, 68.18; H, 7.17; N, 6.20; S, 7.00. Found(%): C, 68.04; H, 7.09; N, 6.25; S, 7.02.

[1076] Compound Number VI-133

[1077] 1 H-NMR(CDCl3) δ: 1.18-1.81(7H, m), 1.85-1.94(2H, m), 2.01-2.13 (2H, m), 2.22-2.33(3H, m), 3.41(1H, m), 3.33(1H, m), 3.49(2H, s), 3.54 (1H, m), 4.15(2H, s), 5.17-5.37(2H, m), 5.90(1H, m), 6.12(1H, dd, J=0.9 and 3.0 Hz), 6.31(1H, dd, J=1.8 and 3.0 Hz), 6.81 and 7.30 (each 1H, each d, each J=3.6 Hz), 7.34(1H, dd, J=0.9 and 1.8 Hz). IR(CHCl3): 3516, 3433, 1709, 1643, 1547, 1516 cm−1. [α]D23+71.3±1.1°(c=1.004, MeOH) Anal. (C24H29NO4S.0.3H2O) Calcd.(%): C, 66.58; H, 6.89; N, 3.24; S, 7.41. Found(%): C, 66.55; H, 6.63; N, 3.37; S, 7.51.

[1078] Compound Number VI-303

[1079] 1 H-NMR(CDCl3) δ: 1.18-2.14(13H, m), 2.26(1H, m), 2.31-2.36(2H, m), 3.30(1H, m), 3.64(1H, m), 3.82(3H, s), 5.19-5.39(2H, m), 6.06(1H, m), 6.89-7.0(6H, m), 7.66(2H, d, J=8.1 Hz). IR(CHCl3): 3514, 3446, 1709, 1649, 1550, 1520, 1491 cm−1. [α]D22+76.3±1.2°(c=1.009, MeOH) Anal. (C28H33NO5.0.2H2O) Calcd(%): C, 71.99; H, 7.21; N, 3.00. Found(%): C, 72.05; H, 7.35; N, 2.93.

[1080] The compounds prepared in Examples above were tested for determining the in vivo and in vitro activities according to the method as shown in Experimental examples below.

[1081] Experiment 1 Binding Activity to PGD2 Receptor

[1082] (1) Preparation of Human Platelet Membrane Fraction

[1083] Blood was collected using a plastic syringe containing 3.8% sodium citrate from the vein of healthy volunteers (adult male and female), then put into a plastic test tube and mixed by slow-reversion. The sample was then centrifuged at 1800 rpm, for 10 min at room temperature, and the supernatant containing PRP (platelet-rich plasma) was collected. The PRP was re-centrifuged at 2300 rpm, for 22 min at room temperature to obtain platelets. The platelets were homogenized using a homogenizer (Ultra-Turrat) followed by centrifugation 3 times at 20,000 rpm, 10 min at 4° C. to obtain a platelet membrane fraction. After protein determination, the membrane fraction was adjusted to 2 mg/ml and preserved in a refrigerator at −80° C. until using for the binding test.

[1084] (2) Binding to PGD2 Receptor

[1085] To a binding-reaction solution (50 mM Tris/HCl, pH 7.4, 5 mM MgCl2) (0.2 ml) were added the human platelet membrane fraction (0.1 mg) and 5 nM [3H]PGD2 (115 Ci/mmol), and the mixture was reacted at 4° C. for 90 min. After the reaction, the mixture was filtered through a glass fiber filter paper and washed several times with cooled physiological saline, then the radioactivity retained on the filter paper was measured. The specific-binding ratio was calculated by subtracting the non-specific binding ratio which is the radioactivity similarly measured in the presence of 10 μM PGD2 from the total binding. The inhibitory activity of each compound was expressed as the concentration required for 50% inhibition (IC50), which was determined by depicting a substitution curve by plotting the binding ratio (%) in the presence of each compound, where the binding ratio in the absence of a test compound is 100%.

[1086] Experiment 2 Binding Activity to TXA2 Receptor

[1087] (1) Preparation of Human Platelet Membrane Fraction

[1088] The human platelet membrane fraction was prepared in accordance with Experiment 1 (1).

[1089] (2) Binding to TXA2 Receptor

[1090] To a binding-reaction solution (50 mM Tris/HCl, pH 7.4, 10 mM MgCl2) (0.2 ml) were added the human platelet membrane fraction (0.05 mg) and 2 nM Sodium [3H](+)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1]hept-2-exo-yl]heptenoate (Japanese Patent Publication (Kokoku) No.79060/1993, hereinafter referred to as (+)-S-145 sodium salt) (26.4 Ci/mmol), and the mixture was reacted at room temperature for 90 min. After the reaction, the resultant mixture was filtered through a glass fiber filter paper and washed several times with cooled physiological saline, then the radioactivity retained on the filter paper was measured. The specific-binding ratio was calculated by subtracting the non-specific binding ratio (the radio activity similarly determined in the presence of 10 μM (+)-S-145 sodium salt) from the total binding. The inhibitory activity of each compound was expressed as the concentration required for 50% inhibition (IC50), which was determined by depicting a substitution curve by plotting the binding ratio (%) in the presence of each compound, where the binding ratio in the absence of a test compound is 100%.

[1091] Experiment 3 Evaluation of Antagonistic Activity Against PGD2 Receptor

[1092] Receptor Using Human Platelet

[1093] Peripheral blood was collected from a healthy volunteer using a syringe in which {fraction (1/9)} volume of a citric acid/dextrose solution was previously added. The sample was subjected to centrifugation at 1200 rpm for 10 min to obtain the supernatant (PRP: platelet rich plasma). The resultant PRP was washed 3 times with a washing buffer and the number of platelets was counted with a micro cell counter. A suspension adjusted to contain the platelets at a final concentration of 5×108/ml was warmed at 37° C., then subjected to the pre-treatment with 3-isobutyl-1-methylxanthine (0.5 mM) for 5 min. To the suspension was added a test compound diluted at various concentration, and 10 minutes later, 0.1 μM PGD2 was added to induce the reaction 2 minutes later, hydrochloric acid was added to terminate the reaction. The platelet was destroyed with an ultrasonic homogenizer. After centrifugation, the cAMP in the supernatant was determined by radioimmunoassay. PGD2 receptor antagonism of a drug was evaluated as follows: the inhibition rate regarding cAMP increased by the addition of PGD2 was determined at each concentration, and the concentration of the drug required for 50% inhibition (IC50) was calculated.

[1094] The results of Experiment 1-3 are shown below. The results of Experiment of compounds of Example are shown in Table 68 and Table 69 and the results of Experiment of compounds of Example of reference are shown in Table 70 and Table 71.

TABLE 68
	Binding activity	Binding activity	Inhibitory
	to PGD2 receptor	to TXA2 receptor	activity for the
	in human platelet	in human platelet	increase of cAMP
	membrane	membrane	caused by PGD2
	fraction	fraction	in human platelet
Compd. No..	IC50(μM)	IC50(μM)	IC50(μM)
I-5A-59a		0.011	0.079
I-7A-1a	0.0076	0.0046	0.035
I-7A-31a		0.063	0.057
I-7A-47a	0.073	0.003	0.018
I-7A-59a		0.0098	0.012
I-7A-88a		0.034	0.036
I-7A-104a		0.024	0.082
I-7A-143a		0.084	0.036
I-7I-1a		0.0026	0.064
I-7I-31a		0.065	0.092
I-7I-47a		0.0012	0.085
I-7I-88a		0.033	0.025
I-71-126a		0.061	0.021
I-71-270a		0.0009	0.026
I-7I-307a		0.051	0.097
I-7M-1e		0.044	0.039
I-7M-59a		0.040	0.024
I-7M-143a		0.021	0.026
I-7M-270a		0.0014	0.012
I-7M-307a		0.100	0.024
I-7M-315a		0.039	0.028
I-7M-316a		0,062	0.11
I-7M-317a		0.074	0.018
I-7M-318a		0.068	0.028
I-7M-333a		0.013	0.094
I-7M-337a		0.037	0.019
I-7M-343a		0.029	0.033
I-7M-393a		0.019	0.11
I-7M-424a		0.0076	0.02
I-7M-446a		0.0063	0.027
I-7P-1a		0.034	0.036
I-7R-1a		0.01	0.018
I-7R-270a		0.012	0.027

[1095]

TABLE 69
	Binding activity	Binding activity	Inhibitory
	to PGD2 receptor	to TXA2 receptor	activity for the
	in human platelet	in human platelet	increase of cAMP
	membrane	membrane	caused by PGD2
	fraction	fraction	in human platelet
Compd. No..	IC50(μM)	IC50(μM)	IC50(μM)
II-5A-1a	0.027	0.0012	0.066
II-5A-31a		0.013	0.045
II-5A-55a	0.0053	0.0006	0.017
II-5A-88a		0.022	0.019
II-5A-104a		0.013	0.047
II-5A-143a		0.047	0.024
II-5B-55a	0.0042	0.0012	0.011
II-5F-55a		0.0019	0.061
II-6A-55a	0.047	0.026	0.1
II-7A-31a		0.082	0.027
II-7A-47a		0.0038	0.059
II-7A-55a	0.0062	0.0042	0.057
II-7A-55e		0.019	0.19
II-7A-59a		0.040	0.042
II-7A-143a		0.037	0.019
II-7I-55a	0.0018	0.0023	0.063
II-7I-59a		0.015	0.015
II-7I-126a		0.102	0.013
II-7I-239a		0.046	0.042
II-7I-270a		0.0006	0.032
II-7I-343a		0.0041	0.079
II-7M-1a		0.0012	0.054
II-7M-1e		0.011	0.12
II-7M-1k		0.020	0.02
II-7M-31a		0.047	0.033
II-7M-47a	0.024	0.0018	0.073
II-7M-55a	0.0013	0.0022	0.013
II-7M-59a		0.027	0.021
II-7M-88a		0.122	0.014
II-7M-126a		0.119	0.026
II-7M-197a		0.012	0.019
II-7M-239a		0.055	0.028
II-7M-270a		0.0006	0.034
II-7M-307a		0.077	0.021
II-7M-332a		0.0017	0.067
II-7M-343a		0.0045	0.075
II-7N-55a	0.0065	0.0025	0.02
II-7P-55a		0.0084	0.047
II-7R-55a		0.0036	0.013
II-7R-270a		0.015	0.023
II-7U-55a		0.021	0.077

[1096]

TABLE 70
	Binding activity	Binding activity	Inhibitory
	to PGD2 receptor	to TXA2 receptor	activity for the
	in human platelet	in human platelet	increase of cAMP
	membrane	membrane	caused by PGD2
	fraction	fraction	in human platelet
Compd. No..	IC50(μM)	IC50(μM)	IC50(μM)
I-1	0.0043	0.003	0.0013
I-10	0.0016	0.092	0.0018
I-31	0.0082	0.130	0.0057
I-47	0.0041	0.0062	0.007
I-59	0.00041	0.016	0.0046
I-66	0.0046	0.034	0.044
I-79	0.00042	0.015	0.024
I-80	0.0066	0.0052	0.039
I-82	0.032	0.0018	0.053
I-88	0.0076	0.078	0.0047
I-93	0.0070	0.072	0.0084
I-94	0.001	0.083	0.01
I-104	0.0001	0.039	0.0016
I-106	0.013	0.013	0.0093
I-117	0.0091	0.0038	0.047
I-128	0.020	0.048	0.01
I-129	0.011	0.052	0.022
I-131	0.044	0.019	0.041
I-132	0.032	0.012	0.043
I-136	0.023	0.016	0.015
I-143	0.0027	0.028	0.0019
I-146	0.044	0.019	0.073
I-160	0.028	0.02	0.085
I-168	0.00046	0.034	0.029
I-169	0.00061	0.032	0.026
I-170	0.00092	0.027	0.017
I-182	0.061	0.028	0.011.

[1097]

TABLE 71
	Binding activity	Binding activity	Inhibitory
	to PGD2 receptor	to TXA2 receptor	activity for the
	in human platelet	in human platelet	increase of cAMP
	membrane	membrane	caused by PGD2
	fraction	fraction	in human platelet
Compd. No..	IC50(μM)	IC50(μM)	IC50(μM)
II-1	0.002	0.012	0.011
II-18	0.0079	0.030	0.0003
II-37	0.026	0.0043	0.035
II-47	0.00096	0.0036	0.004
II-55	0.0015	0.0044	0.0039
II-59	0.0001	0.014	0.024
II-101	0.072	0.0040	0.045
II-117	0.022	0.0026	0.024
II-126	0.0046	0.045	0.004
II-138	0.032	0.072	0.025

[1098] Experiment 4 Change of Plasma Concentration of Drug in Rat

[1099] Compound (0.5 to 2 mg/kg) was administered intravenously to Jcl-SD male rats. The concentration of the unchanged compound was measured at 2, 5, 15, 30, 60, 120, and 240 min after the administration by the use of HPLC (determination limit; 0.05 μg/ml) and LC/MS/MS (determination limit; 0.001 μg/ml) and the half life of the disappearance was calculated.

TABLE 72
                      half life of the
                      disappearance
Compd. No..           (min)
Reference Compd.I-1   9.4
I-7M-1a               26.3
Reference Compd.I-143 4.7
I-7M-143a             38.4
Reference Compd.II-59 11.0
II-7I-59a             67.0
II-7M-59a             92.6

[1100] A half-life of the disappearance of a compound of the present invention was observed to be about 3 to 8 times as long as that of the compound of reference and the metabolic stability was confirmed.

[1101] Experiments for comparing the present compound having a dual antagonistic activity against PGD2/TXA2 receptors (e.g., II-7I-55a, II-7M-55a) with a PGD2 receptor antagonist (e.g., B-1, B-2) and a TXA2 antagonist (e.g., A) are shown below. 582

[1102] The experiments were carried out in accordance with the above Experiment 1-3 for the purpose of comparing the compound having a dual antagonistic activity against PGD2/TXA2 receptor with a PGD2 receptor antagonist and a TXA2 receptor antagonist.

TABLE 73
	Experiment 1	Experiment 2	Experiment 3
	Antagonistic	Antagonistic	Antagonistic
	activity	activity	activity
	against PGD2	against TXA2	against PGD2
	receptor	receptor	receptor
Compd.	IC50 (μM)	IC50 (μM)	IC50 (μM)
Compound	0.0018	0.0023	0.063
(II-7I-55a)
Compound	0.0013	0.0022	0.013
(II-7M-55a)
TXA2 receptor	>10	0.0038	>10
antagonist (A)
PGD2 receptor	0.022	0.37	0.030
antagonist
(B-1)

[1103] Comparative Experiment 2

[1104] Antigen-Induced Bronchial Hyperresponsiveness

[1105] Male Hartley guinea pigs were actively sensitized to ovalbumin (OVA) by inhalation of aerosolized solution of 1% ovalbumin twice at a week interval. One week after the second sensitization, the animals were treated with antihistamine, diphenhydramine (10 mg/kg, i.p.), and then challenged with 1% OVA aerosol for 5 min. Twenty four hours later, acetylcholine at doses at 3.13, 6.25, 12.5, 25, 50 and 100 micro g/kg was sequentially injected into the animals which were anesthetized with pentobarbital (30 mg/kg, i.p.). The bronchoconstriction induced by each dose of acetylcholine was monitored by the modified method of Konzett-Rössler technique, and made a dose-response curve of acetylcholine. Using the dose-response curve, the dose required for 200% increase in bronchoconstriction from baseline (PD200) was calculated in each animal and used as an indication of bronchial responsiveness. Compounds were orally administered 1 hour before antigen challenge. **: P<0.01 vs Vehicle(Dunnett's test), ##: P<0.01 vs Vehicle(Student's t test).

TABLE 74
Log PD200
Vehicle                      1.033 ± 0.053
Compound (II-7I-55a)10 mg/kg 1.442 ± 0.055**
Compound (II-7M-55a)10 mg/kg 1.485 ± 0.119**
Negative control             1.517 ± 0.067##

[1106]

TABLE 75
Log PD200
Vehicle                1.125 ± 0.023
Compound (B-2)10 mg/kg 1.237 ± 0.052
Negative control       1.465 ± 0.074##

[1107]

TABLE 76
Log PD200
Vehicle              1.11 ± 0.06
Compound (A)1 mg/kg  1.29 ± 0.04
Compound (A)10 mg/kg 1.61 ± 0.09**
Negative control     1.69 ± 0.06##

[1108] As shown in Table 74 to Table 76, a PGD2 receptor antagonist (B-2) did not inhibit the induction of bronchial hyperresponsiveness, but TXA2 receptor antagonist (A) and PGD2/TXA2 dual receptor antagonist, (e.g., II-71-55a, II-7M-55a) suppressed it, indicating that TXA2 receptor antagonism is necessary for improvement of bronchial hyperresponsiveness.

[1109] Comparative Experiment 3

[1110] Antigen-Induced Increase in the Eosinophil Number in Bronchoalveolar Lavage Fluid.

[1111] Bronchoalveolar lavage was performed with 10 mL of saline, after the animals were sensitized and challenged with antigen. The number of total cells in the recovered fluid was stained with Türk and counted using hemocytometer. *: P<0.05, **:P<0.01 vs Vehicle(Dunnett's test), ##: P<0.01 vs Vehicle(Student's t test). ( ): inhibition %.

TABLE 77
Total cells (× 106cells/animal)
Vehicle                       23.36 ± 2.33
Compound (II-7I-55a) 10 mg/kg 12.26 ± 1.54**(80%)
Compound (II-7M-55a) 10 mg/kg 18.29 ± 1.46 (36%)
Negative control              9.43 ± 0.78##

[1112]

TABLE 78
Total cells (× 106 cells/animal)
Vehicle                 17.12 ± 2.20
Compound (B-2) 10 mg/kg 9.72 ± 2.32* (53%)
Negative control        3.20 ± 0.52##

[1113]

TABLE 79
Total cells (× 106 cells/animal)
Vehicle               13.89 ± 2.42
Compound (A) 10 mg/kg 15.20 ± 2.20 (−12%)
Negative control      2.98 ± 0.28##

[1114] As shown in Table 77 to Table 79, PGD2 receptor antagonist (B-2) and PGD2/TXA2 dual receptor antagonist (II-71-55a, II-7M55a) significantly suppressed the eosinophil infiltration. But a TXA2 receptor antagonist (A) did not show any inhibitory actions. These results indicate that PGD2 receptor antagonism is necessary for suppression of inflammatory cell infiltration.

[1115] Comparative Experiment 4

[1116] Acceleration of Vascular Permeability of Conjunctiva Induced by PGD2 and U-46619

[1117] Using male Hartley guinea pigs, PGD2- and TxA2 receptor-mediated increase in conjunctival vascular permeability was produced by instillation of each 10 μl solution of either 0.1% PGD2 or U-46619 (TXA2 receptor agonist) to the both eyes without anesthetization. Immediately after that, Evans blue dye (20 mg/kg) was intravenously injected. 30 min after the challenge, guinea pigs were sacrificed by bleeding under anesthesia with Pentobarbital (30 mg/kg, i.p.) and the tissue of conjunctiva was removed. The dye leaked into the tissue was extracted in formamide 3 ml at 60° C. for more than 24 h, and then centrifuged. The absorbance of the supernatant was measured at 620 nm. The amount of dye was calculated from the calibration curve of Evans blue dye. Each compound was suspended in 0.5% methyl-cellulose and administrated orally at 1 h before the challenge. The antagonistic activity was evaluated by the inhibition ratio against the dye leaked into conjunctiva caused by PGD2 or U-46619 at each (lose and then a 50% effective dose of inhibition (ED50 value) of each compound was calculated.

	TABLE 80
		ED50 (mg/kg)
	Compound	PGD2	TXA2 (U-46619)
	II-7I-55a	0.33	0.030
	II-7M-55a	0.043	0.083
	PGD2 receptor antagonist	0.099	>10
	(B-2)
	TXA2 receptor antagonist	>30	0.017
	(A)

[1118] As shown in Table 80, a PGD2 receptor antagonist (B-2) inhibited the increase in vascular permeability in conjunctiva by the stimulation with PGD2 but did not inhibit that caused by U-46619, viceversa, a TXA2 receptor antagonist (A) suppressed only U-46619-induced response. PGD2/TXA2 dual receptor antagonist (e.g., I-7I-55a, II-7M-55a) showed both responses. Thus, the inhibition of both receptor-mediated responses was ascertained in vivo.

Formulation Example

[1119] It is to be noted that the following Formulation Examples 1 to 8 are mere illustration, but not intended to limit the scope of the invention. The term “Active ingredient” means a compound of the present invention, the prodrug thereof, their pharmaceutically acceptable salt, or their hydrate.

Formulation Example 1

[1120] Hard gelatin capsules are prepared using the following ingredients:

Dose
(mg/capsule)
Active ingredient  250
Starch, dried      200
Magnesium stearate 10
Total              460 mg

Formulation Example 2

[1121] Tablet are prepared using the following ingredients:

Dose
(mg/tablet)
Active ingredient        250
Cellulose, microcrystals 400
Silicon dioxide, fumed   10
Stearic acid             5
Total                    665 mg

[1122] The ingredients are blended and compressed to form tablets each weighing 665 mg.

Formulation Example 3

[1123] An aerosol solution is prepared containing the following components:

Weight
Active ingredient                0.25
Ethanol                          25.75
Propellant 22 (chlorodifluoromethane) 74.00
Total                            100.00

[1124] The active ingredient is mixed with ethanol and the admixture added to a portion of the propellant 22, cooled to −30° C. and transferred to a filling device. The required amount is then fed to a stainless steel container and diluted with the reminder of the propellant. The valve units are then fitted to the container.

Formulation Example 4

[1125] Tablets, each containing 60 mg of active ingredient, are made as follows.

	Active ingredient	60	mg
	Starch	45	mg
	Microcrystals cellulose	35	mg
	Polyvinylpyrrolidone (as 10% solution in	4	mg
	water)
	Sodium carboxymethyl starch	4.5	mg
	Magnesium stearate	0.5	mg
	Talc	1	mg
	Total	150	mg

[1126] The active ingredient, starch, and cellulose are passed through a No. 45 mesh U.S. sieve, and the mixed thoroughly. The aqueous solution containing polyvinylpyrrolidone is mixed with the resultant powder, and the admixture then is passed through a No. 14 mesh U.S. sieve. The granules so produced are dried at 50° C. and passed through a No. 18 mesh U.S. sieve. The sodium carboxymethyl starch, magnesium stearate, and talc, previously passed through No. 60 mesh U.S. sieve, are then added to the granules which, after mixing, are compressed on a tablet machine to yield tablets each weighing 150 mg.

Formulation Example 5

[1127] Capsules, each containing 80 mg of active ingredient, are made as follows:

	Active ingredient	80	mg
	Starch	59	mg
	Microcrystals cellulose	59	mg
	Magnesium stearate	2	mg
	Total	200	mg

[1128] The active ingredient, cellulose, starch, and magnesium stearate are blended, passed through a No. 45 mesh U.S. sieve, and filled into hard gelatin capsules in 200 mg quantities.

Formulation Example 6

[1129] Suppositories, each containing 225 mg of active ingredient, are made as follows:

Active ingredient               225 mg
Saturated fatty acid glycerides 2000 mg
Total                           2225 mg

[1130] The active ingredient; is passed through a No. 60 mesh U.S. sieve and suspended in the saturated fatty acid glycerides previously melted using the minimum heat necessary. The mixture is then poured into a suppository mold of nominal 2 g capacity and allowed to cool.

Formulation Example 7

[1131] Suspensions, each containing 50 mg of active ingredient per 5 ml dose, are made as follows:

	Active ingredient	50	mg
	Sodium carboxymethyl cellulose	50	mg
	Syrup	1.25	ml
	Benzoic acid solution	0.10	ml
	Flavor	q.v.
	Color	q.v.
	Purified water to total	5	ml

[1132] The active ingredient is passed through a No. 45 U.S. sieve, and mixed with the sodium carboxymethyl cellulose and syrup to form a smooth paste. The benzoic acid solution, flavor and color are diluted with a portion of the water and added, with stirring. Sufficient water is then added to produce the required volume.

Formulation Example 8

[1133] An intravenous formulation may be prepared as follows:

Active ingredient 100 mg
Isotonic saline   1000 ml

[1134] The solution of the above ingredients is generally administered intravenously to a subject at a rate of 1 ml per minute.

Industrial Applicability

[1135] The pharmacological effect of the compound of the present invention is compared with that of TXA2 receptor antagonist and PGD2 receptor antagonist in the following table.

	TABLE 81
	TXA2 receptor	PGD2 receptor
	antagonist	antagonist	Compound (I)
Bronchial asthma
Eosinophilic	x	⊚	⊚
infiltration
Advance of respiratory	⊚	x	⊚
anaphylaxis
Respiratory	⊚	x	⊚
contraction

[1136] In bronchial asthma, a TXA2 receptor antagonist itself can inhibit advance of respiratory anaphylaxis and respiratory contraction, but has no effect for eosinophilic infiltration. A PGD2 receptor antagonist itself can inhibit eosinophilic infiltration, but has no effect for advance of respiratory anaphylaxis and respiratory contraction. On the other hand, a compound having a dual antagonistic activity against PGD2/TXA2 receptors like the compound (I) is efficient for all of eosinophilic infiltration, advance of respiratory anaphylaxis and respiratory contraction.

[1137] A TXA2 receptor antagonist has no effect for eosinophilic infiltration but was ascertained to increase the inhibitory effect for eosinophilic infiltration caused by a PGD2 receptor antagonist. That is, a TXA2 receptor antagonist and a PGD2 receptor antagonist were ascertained to show a synergistic effect. Then, a compound having a dual antagonistic activity against PGD2ITXA2 receptors like the compound (I) is very efficient.

[1138] The compound having a dual antagonistic activity against PGD2/TXA2 receptors is useful for treating systemic mastocytosis and disorder of systemic mast cell activation as well as tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, itching, atopic dermatitis, alimentary allergy, ischemic reperfusion injury, cerebrovascular disorder, an d inflammation, and effective for treating or improving condition of diseases such as arteriosclerosis, myocardial infarction, acute myocardial ischemia angina, cardiovascular shock or preventing unexpected death and the like, especially asthma or nasal blockage.

[1139] With a dual antagonistic activity against both a TXA2 receptor and a PGD2 receptor, the present compound can overcome some problems such as that due to the metabolic rate difference of each compound, which occur upon simultaneous administration of both a TXA2 receptor antagonist and a PGD2 receptor antagonist.

Claims

1. A compound of the formula (I):

2. A compound as described in claim 1 wherein A is alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond; R is —C(═O)—R1, —CH2—R1, or tetrazolyl; R1 is hydroxy, alkyloxy, or optionally substituted amino; provided compounds wherein A is —CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 (R1 is hydroxy or alkyloxy), or A is —CH2—CH═CH—CH2—CH2—CH2—and R is —C(═O)—R1 wherein R1 is hydroxy or alkyloxy are excluded, a prodrug, a pharmaceutically acceptable salt or a solvate thereof.

3. A compound as described in claim 1 or 2, wherein A is alkylene intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond,

4. A compound as described in claim 1 or 2, wherein A is C1 to C4 or C7 to C9 alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond, a prodrug, a pharmaceutically acceptable salt, or a solvate thereof.

5. A compound as described in claim 1 or 2, wherein A is —CH2—CH2—CH2—, —CH2—CH2—CH(F)—, —CH2CH═CH—, —CH2—O—CH2—, —CH2CH═C(F)—, —CH2—CH2—CH2—CH2—, —CH2CH═CH—CH2—, —CH2—CH2—CH═CH—, —CH═CH—CH2—CH2—, —CH2—CH2—O—CH2—, —CH2—CH2—S—CH2—, —CH2—CO—NH—CH2—, —CH2—CH2—CH2—CH2—CH2—, CH2CH═CH—CH2—CH2—, —CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—O—CH2—, —CH2—CH2—CH2—S—CH2—, —CH2—CH2—CO—NH—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—CH(Me)—, —CH2—CH2—CH2—CH2—CH2—C(Me)2—, —CH2—CH2—CH2—CH2—CH2—CH(F)—, —CH2—CH═CH—CH2—CH2—CH(Me)—, —CH2—CH═CH—CH2—CH2—C(Me)2—, —CH2—CH═CH—CH2—CH2—CH(F)—, —CH2—CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—CH2—CH═C(Me)—, —CH2—CH2—CH2—CH2—C(Me)═CH—, —CH2—CH2—CH2—CH2—CH═C(F)—, —CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH═CH—CH2—O—CH2—, —CH2—CH═CH—CH2—S—CH2—, —CH2—CH═C(F)—CH2—O—CH2—, —CH2—CH2—O—CH2—CH═CH—, —CH2—CH2—CH2—CH2—S—CH2—, —CH2—CH2—CH2—CO—NH—CH2—, —CH2—CH2—CH═N—O—CH2—, —CH2—CH2—S—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—CH2—, —CH2—CH═CH—CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH2—CH2—CH2—CH2—CH2—CH2—CH2—, or —CH2—CH═CH—CH2—CH2—CH2—CH2—CH2—,

6. A compound as described in claim 5, wherein A is —CH2—CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—CH═CH—, —CH2—CH2—CH2—CH2—O—CH2—, —CH2—CH═CH—CH2—O—CH2—, —CH2—CH═CH—CH2—S—CH2—, or —CH2—CH2—CH2—CH2—S—CH2—,

7. A compound as described in claim 6, wherein A is —CH2—CH2—CH2—CH2—O—CH2—,

8. A compound as described in any one of claims 1 to 7, wherein X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl,

9. A compound as described in claim 8, wherein at least one of X1 and X3 is optionally substituted heteroaryl,

10. A compound as described in claim 9, wherein X1 and X3 are each independently optionally substituted heteroaryl,

11. A compound as described in claim 9, wherein at least one of X1 and X3 is optionally substituted thienyl or optionally substituted benzothienyl,

12. A compound as described in any one of claims 1 to 11, wherein X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or —NH—C(═O)—NH—,

13. A compound as described in any one of claims 1 to 12, wherein m is 0 and p is 0,

14. A compound as described in any one of claims 1 to 13, wherein R is —C(═O)—R1 and R1 is hydroxy, alkyloxy, or optionally substituted amino,

15. A pharmaceutical composition containing a compound, a prodrug, a pharmaceutically acceptable salt, or a solvate thereof as described in any one of claims 1 to 14.

16. A pharmaceutical composition having a dual antagonistic activity against PGD2/TXA2 receptors as described in claim 15.

17. A pharmaceutical composition as described in claim 15, which is used for the treatment of asthma.

18. A pharmaceutical composition as described in claim 15, which is used for the treatment of nasal blockage.

19. A pharmaceutical composition as described in claim 15, which is used for the treatment of allergic conjunctivitis.

20. A pharmaceutical composition as described in claim 15, which is used for the treatment of allergic rhinitis.

21. Use of the compound as described in any one of claims 1 to 14 for the preparation of a pharmaceutical composition for treating asthma, nasal blockage, allergic conjunctivitis or allergic rhinitis.

22. A method for treating nasal blockage, allergic conjunctivitis or allergic rhinitis, which comprises administrating a compound as described in any one of claims 1 to 14.

23. A compound of the formula: X3—X2—X1—COOH wherein X3 is pyrrolyl optionally substituted with alkyl, alkyloxy or halogen, indolyl optionally substituted with alkyl, alkyloxy or halogen, indolinyl optionally substituted with alkyl, alkyloxy or halogen, or 1,2,3,4-tetrahydroquinolyl optionally substituted with alkyl, alkyloxy or halogen; X2 is —SO2—, —S— or —CH2—; X1 is thienyl, or a salt thereof.

24. A compound as described in claim 23, wherein a substituent of the formula: —X1—X2—X3 is 5-(1-pyrrolylsulfonyl)thiophen-2-yl, 5-[(2-methyl-1-pyrrolyl)sulfonyl]thiophen-2-yl, or 5-[(2,5-dimethyl-1-pyrrolyl)sulfonyl]thiophen-2-yl, or a salt thereof.