Herbicidal pyrazole derivatives

BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to novel 4-benzoylpyrazole derivatives and selective herbicides containing such derivatives as active ingredients, which are useful particularly as upland field herbicides.
2. Discussion of Background
Various herbicides have been developed for practical use from extensive research and development of herbicides for many years, and such herbicides have contributed to a reduction of the labor force required for controlling weeds or to improvement of the productivity of agricultural or horticultural plants.
Even now, it is still desired to develop a new herbicide having superior herbicidal properties. In particular, it is desired to develop an agricultural or horticultural herbicide which is capable of selectively controlling weeds without adversely affecting the crop plant and at a low dose. However, conventional herbicides do not necessarily provide such desired herbicidal properties.
On the other hand, certain compounds of 4-benzoylpyrazole derivatives are known to have herbicidal activities. For example, pyrazolate (common name) and pyrazoxyfen (common name) are practically used as herbicides for paddy fields. While exhibiting excellent herbicidal activities as paddy field herbicides, these compounds are not suitable as upland herbicides since their herbicidal activities are weak against weeds of upland fields. Among 4-benzoylpyrazole derivatives, it is desired to develop a superior compound useful as an upland field herbicide.
SUMMARY OF THE INVENTION
The present invention provides a pyrazole derivative having the formula: ##STR2## wherein A is an alkyl group having from 1 to 3 carbon atoms, an alkenyl group having from 2 to 4 carbon atoms or an alkynyl group having from 2 to 4 carbon atoms; B is a hydrogen atom, an alkyl group having from 1 to 3 carbon atoms, a halogen atom, a haloalkyl group having from 1 to 3 carbon atoms, an alkoxy group having from 1 to 3 carbon atoms, an alkylthio group having from 1 to 3 carbon atoms, an alkoxyalkyl group having from 2 to 4 carbon atoms, an alkylthioalkyl group having from 2 to 4 carbon atoms or an alkoxycarbonyl group having from 2 to 4 carbon atoms; X is an alkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms, a halogen atom, a nitro group, a cyano group, a haloalkyl group having from 1 to 6 carbon atoms, an alkoxyalkyl group having from 2 to 6 carbon atoms, an alkylcarbonyl group having from 2 to 6 carbon atoms, an alkoxycarbonyl group having from 2 to 6 carbon atoms, an aminocarbonyl group substituted independently by hydrogen or alkyl having from 1 to 6 carbon atoms, a haloalkoxy group having from 1 to 6 carbon atoms, an alkylthio group having from 1 to 6 carbon atoms or an alkylthioalkyl group having from 2 to 6 carbon atoms; Y is a --COOR1 group (wherein R1 is a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 3 to 8 carbon atoms, a cycloalkylalkyl group having from 4 to 8 carbon atoms, an alkynyl group having from 3 to 6 carbon atoms, an alkenyl group having from 2 to 6 carbon atoms, a haloalkyl group having from 1 to 6 carbon atoms, a halocycloalkyl group having from 3 to 8 carbon atoms, a haloalkynyl group having from 3 to 6 carbon atoms, a haloalkenyl group having from 2 to 6 carbon atoms or a phenyl group which may be substituted by alkyl having from 1 to 3 carbon atoms, halogen, nitro or alkoxy having from 1 to 3 carbon atoms), a --COO--L--OR1 group (wherein L is an alkylene group having from 1 to 6 carbon atoms which may be substituted by alkyl having from 1 to 3 carbon atoms, and R1 is as defined above), a --COO--L--R2 group (wherein L is as defined above, and R2 is a phenyl group which may be substituted by alkyl having from 1 to 3 carbon atoms, halogen, nitro or alkoxy having from 1 to 3 carbon atoms), a --COO--M group (wherein M is a 3 to 6-membered alicyclic residue containing not more than 2 sulfur or oxygen atoms and formed by a linkage of from 1 to 4 carbon atoms), a --COO--L--M group (wherein L and M are as defined above), a COO--L--O--L--R2 group (wherein L and R2 are as defined above), a --COO--L--S(O).sub.n --R1 group (wherein L and R1 are as defined above, and n is an integer of from 0 to 2), a --CON(R3)(R4) group (wherein each of R3 and R4 is a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 3 to 8 carbon atoms, a cycloalkylalkyl group having from 4 to 8 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms, an alkynyl group having from 2 to 6 carbon atoms, an alkenyl group having from 2 to 6 carbon atoms, a haloalkyl group having from 1 to 6 carbon atoms, a halocycloalkyl group having from 3 to 8 carbon atoms, a haloalkynyl group having from 2 to 6 carbon atoms, a haloalkenyl group having from 2 to 6 carbon atoms or a phenyl group which may be substituted by alkyl having from 1 to 3 carbon atoms, halogen, nitro or alkoxy having from 1 to 3 carbon atoms), a --CON--(CH.sub.2).sub.n group (wherein n is an integer of from 4 to 6), a ##STR3## group (wherein R5 is an alkyl group having from 1 to 3 carbon atoms), a ##STR4## group, a --CONHSO.sub.2 CH.sub.3 group, a --CONHSO.sub.2 CF.sub.3 group, a --COO--L--N(R3)(R4) group (wherein L, R3 and R4 are as defined above), a --COO--L--CO--R1 group (wherein L and R1 are as defined above), a --COO--L--CO--O--R1 group (wherein L and R1 are as defined above), a --COO--L--CN group (wherein L is as defined above), a --COO--L--NO.sub.2 group (wherein L is as defined above), a --COOSi(R5).sub.3 group (wherein R5 is as defined above), a --COO--N.dbd.C(R6)(R7) group (wherein each of R6 and R7 which may be the same or different is an alkyl group having from 1 to 3 carbon atoms), a --COO--N.dbd.C--(CH.sub.2).sub.n group (wherein n is an integer of from 4 to 6), a --COO--L--O--SO.sub.2 --R1 group (wherein L and R1 are as defined above), a --COO--L--O--CO--R1 group (wherein L and R1 are as defined above), a --COO--L--O--L--O--R1 group (wherein L and R1 are as defined above), a --COO--L--Si(R5).sub.3 group (wherein L and R5 are as defined above), a --C(O)S--R1 group (wherein R1 is as defined above), a --C(S)O--R1 group (wherein R1 is as defined above), a --C(S)S--R1 group (wherein R1 is as defined above), a --L--O--R1 (wherein L and R1 are as defined above), a --L--O--L--O--R8 group (wherein L is as defined above, and R8 is a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms), a --L--O--M group (wherein L and M are as defined above), a --L--O--L--M group (wherein L and M are as defined above), a --L--NR8R9 group (wherein R8 is as defined above, and R9 is an alkyl group having from 1 to 6 carbon atoms), a --L--O--CH.sub.2 Ph group (wherein L is as defined above), --L--O--L--COOR9 group (wherein L and R9 are as defined above), a --L--CN group (wherein L is as defined above), a --L--S(O).sub.n --R1 group (wherein L and R1 are as defined above, and n is an integer of from 0 to 2), a --L--S--L--O--R9 group (wherein L and R9 are as defined above), a --L--O--COR9 group (wherein L and R9 are as defined above), a L--O--SO.sub.2 R9 group (wherein L and R9 are as defined above) or a --L--O--L--CN group (wherein L is as defined above); Z is a halogen atom, a nitro group, an alkoxy group having from 1 to 3 carbon atoms, a trifluoromethyl group, a cyano group or a --S(O).sub.n R10 group (wherein R10 is an alkyl group having from 1 to 3 carbon atoms or a haloalkyl group having from 1 to 3 carbon atoms, and n is an integer of from 0 to 2); Q is a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms which may be substituted by halogen, an alkenyl group having from 1 to 6 carbon atoms which may be substituted by halogen, an alkynyl group having from 1 to 6 carbon atoms which may be substituted by halogen, a cyanomethyl group, a --C(O)--R11 group (wherein R11 is a phenyl group which may be substituted by the same or different substituents selected from the group consisting of alkyl having from 1 to 6 carbon atoms, alkenyl having from 1 to 6 carbon atoms, alkynyl having from 1 to 6 carbon atoms, haloalkyl having from 1 to 6 carbon atoms, haloalkenyl having from 1 to 6 carbon atoms, haloalkynyl having from 1 to 6 carbon atoms, halogen, nitro and trifluoromethyl, an alkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms or a hydroxyl group), a --S(O).sub.2 R11 group (wherein R11 is as defined above), a --P(O)(OR11).sub.2 group (wherein R11 is as defined above), a --L--C(O)--R11 group (wherein L and R11 are as defined above), a --L--C(O)--N(R12)(R13) (wherein L is as defined above, each of R12 and R13 is a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms), a --L--R14 group (wherein L is as defined above, R14 is a phenyl group which may be substituted by the same or different substituents selected from the group consisting of halogen, nitro and trifluoromethyl, an alkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms or a hydroxy group), a --L--N(R12)(R13) group (wherein L, R12 and R13 are as defined above), a --L--OR15 group (wherein R15 is a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an alkenyl group having from 1 to 6 carbon atoms), a --L--OC(O)R16 group (wherein R16 is an alkyl group having from 1 to 6 carbon atoms or an alkoxy group having from 1 to 6 carbon atoms), a --L--S(O).sub.n R15 group (wherein R15 is as defined above, and n is an integer of 0 or 2), a --L--SC(O)R12 group (wherein R12 is as defined above), ##STR5## group (wherein each of L1 and L2 is a methylene group, an oxygen atom or a sulfur atom, R16 is a hydrogen atom or an alkyl group having from 1 to 3 carbon atoms, and n is an integer of 2 or 3), and a salt thereof.
The present invention also provides a selective herbicidal composition comprising a herbicidally effective amount of at least one pyrazole derivative of the formula I as defined above or its salt and an agricultural carrier or diluent.
Further, the present invention provides a method for selectively controlling weeds, which comprises applying the pyrazole derivative of the formula I as defined above or its salt to the locus to be protected.
Now, the present invention will be described in detail with reference to the preferred embodiments.
In the compound of the formula I of the present invention, A, B, X, Y, Z and Q are preferably selected from the following substituents, respectively:
A: Me, Et, n-Pr, i-Pr, CH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 C.tbd.CH
B: H, Me, Et, n-Pr, i-Pr, Cl, Br, CH.sub.2 Cl, CF.sub.3, OMe, OEt, OPr-i, SMe, CH.sub.2 OMe, CH.sub.2 SMe, CO.sub.2 Me, CO.sub.2 Et
X: Me, Et, n-Pr, i-Pr, n-Bu, i-Bu, s-Bu, t-Bu, OMe, OEt, OPr-n, OPr-i, OBu-n, OBu-i, OBu-s, OBu-t, F, Cl, Br, I, NO.sub.2, CN, CH.sub.2 F, CHF.sub.2, CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 Cl, CCl.sub.3, CHClMe, CH.sub.2 CH.sub.2 Cl, CHClCH.sub.2 Cl, CH.sub.2 Br, CHBrMe, CH.sub.2 CH.sub.2 Br, CH.sub.2 OMe, CH.sub.2 OEt, CH.sub.2 OPr-n, CH.sub.2 OPr-i, CH.sub.2 OBu-n, CH.sub.2 OBu-i, CH.sub.2 OBu-s, CH.sub.2 OBu-t, CHMeOMe, CHMeOEt, CHMeOPr-n, CHMeOPr-i, CHMeOBu-n, CHMeOBu-i, CHMeOBu-s, CHMeObu-t, CH.sub.2 CH.sub.2 OMe, CH.sub.2 CH.sub.2 OEt, CH.sub.2 CH.sub.2 OPr-i, Ac, COEt, COPr-n, COPr-i, COOMe, COOEt, COOPr-i, CONHMe, CONHEt, CONMe.sub.2, CONEt.sub.2, CONEtMe, OCHF.sub.2, OCF.sub.3, OCH.sub.2 CF.sub.3, SMe, SEt, CH.sub.2 SMe, CH.sub.2 SEt, CHMeSMe, CHMeSEt
Y: CH.sub.2 OH, CH.sub.2 OMe, CH.sub.2 OEt, CH.sub.2 OPr-n, CH.sub.2 OPr-i, CH.sub.2 OBu-n, CH.sub.2 OBu-i, CH.sub.2 OBu-s, CH.sub.2 OBu-t, CH.sub.2 OAm-n, CH.sub.2 OAm-i, CH.sub.2 OAm-t, CH.sub.2 OC.sub.6 H.sub.13 -n, ##STR6## CH.sub.2 OCH.dbd.CH.sub.2, CH.sub.2 OCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 OCH.sub.2 CMe.dbd.CH.sub.2, CH.sub.2 OCHMeCH.dbd.CH.sub.2, CH.sub.2 OCH.sub.2 C.tbd.CH, CH.sub.2 OCHMeC.tbd.CH, CH.sub.2 OCMe.sub.2 C.tbd.CH, CH.sub.2 OCH.sub.2 CH.sub.2 F, CH.sub.2 OCH.sub.2 CF.sub.3, CH.sub.2 OCH.sub.2 CH.sub.2 Cl, CH.sub.2 OCH.sub.2 Cl.sub.3, CH.sub.2 OCH.sub.2 CH.sub.2 Br, ##STR7## CH.sub.2 OCH.sub.2 CCl.dbd.CH.sub.2, CH.sub.2 OCH.sub.2 CCl.dbd.CHCl, CH.sub.2 OCH.sub.2 CH.sub.2 OMe, CH.sub.2 OCH.sub.2 CH.sub.2 OEt, CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i, ##STR8## CH.sub.2 OPh, CH.sub.2 OPh-Cl-4, CH.sub.2 OPh-NO.sub.1 -4, CH.sub.2 NHMe, CH.sub.2 NHEt, CH.sub.2 NMe.sub.2, CH.sub.2 NEt.sub.2, CH.sub.2 NEtMe, CH.sub.2 OCH.sub.2 Ph, CH.sub.2 OCH.sub.2 COOMe, CH.sub.2 OCH.sub.2 COOEt, CH.sub.2 OCHMeCOOMe, CH.sub.2 OCH.sub.2 COOBu-t CH.sub.2 OCHMeCOOEt, CH.sub.2 CN, CH.sub.2 SMe, CH.sub.2 SEt, CH.sub.2 SPr-n, CH.sub.2 SPr-i, CH.sub.2 SBn-t, CH.sub.2 SCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 SCH.sub.2 C.tbd.CH, ##STR9## CH.sub.2 SCH.sub.2 CH.sub.2 Cl, CH.sub.2 SOMe, CH.sub.2 SOEt, CH.sub.2 SO.sub.2 Me, CH.sub.2 SO.sub.2 Et, CH.sub.2 SO.sub.2 Pr-n, CH.sub.2 SO.sub.2 Pr-i, CH.sub.2 SCH.sub.2 CH.sub.2 OMe, CH.sub.2 SCH.sub.2 CH.sub.2 OEt, CH.sub.2 SPh, CH.sub.2 OAc, CH.sub.2 OCOEt, CH.sub.2 OCOPr-i, CH.sub.2 OSO.sub.2 Me, CH.sub.2 OSO.sub.2 Et, CH.sub.2 OCH.sub.2 CH.sub.2 CN, CHMeOH, CHMeOMe, CHMeOEt, CHMeOPr-n, CHMeOPr-i, CHMeOBu-n, CHMeOBu-i, CHMeOBu-s, CHMeOBu-t, ##STR10## CHMeOCH.dbd.CH.sub.2, CHMeOCH.sub.2 CH.dbd.CH.sub.2, CHMeOCH.sub.2 C.tbd.CH, CHMeOCH.sub.2 CF.sub.3, CHMeOCH.sub.2 CH.sub.2 Cl, CHMeOCH.sub.2 CCl.sub.3, CHMeOCH.sub.2 CH.sub.2 Br, ##STR11## CHMeOCH.sub.2 CH.sub.2 OMe, CHMeOCH.sub.2 CH.sub.2 Et, ##STR12## CHMeOPh, CHMeNHMe, CHMeNMe.sub.2, CHMeNEt.sub.2, CHMeOCH.sub.2 COOMe, CHMeOCH.sub.2 COOEt, CHMeOCHMeCOOMe, CHMeCN, CHMeSMe, CHMeSEt, CHMeSPr-n, CHMeSPr-i, CHMeSCH.sub.2 CH.dbd.CH.sub.2, CHMeSCH.sub.2 C.tbd.CH, ##STR13## CHMeSCH.sub.2 CH.sub.2 Cl, CHMeSOMe, CHMeSOEt, CHMeSO.sub.2 Me, CHMeSO.sub.2 Et, CHMeSO.sub.2 Pr-i, CHMeSCH.sub.2 CH.sub.2 OMe CHMeSPh, CHMeOAc, CHMeOCOEt, CHMeOSO.sub.2 Me, CHMeOSO.sub.2 Et, CHMeOCH.sub.2 CH.sub.2 CN, CMe.sub.2 OH, CMe.sub.2 OMe, CMe.sub.2 OEt, CMe.sub.2 OPr-n, CMe.sub.2 OPr-i, CMe.sub.2 OCH.dbd.CH.sub.2, CMe.sub.2 OCH.sub.2 CH.dbd.CH.sub.2, CMe.sub.2 OCH.sub.2 C.tbd.CH, CMe.sub.2 OCH.sub.2 CH.sub.2 Cl, CMe.sub.2 OCH.sub.2 CH.sub.2 OMe, ##STR14## CMe.sub.2 NHMe, CMe.sub.2 NMe.sub.2, CMe.sub.2 OCH.sub.2 COOMe, CMe.sub.2 CN, CMe.sub.2 SMe, CMe.sub.2 SEt, CMe.sub.2 SO.sub.2 Me, CMe.sub.2 SO.sub.2 Et, CMe.sub.2 OAc, CMe.sub.2 OSO.sub.2 Me, COOH, COOMe, COOEt, COOPr-n, COOPr-i, COOBu-n, COOBu-s, COOBu-i, COOBu-t, COOAm-i, ##STR15## COOCH.sub.2 CH.dbd.CH.sub.2, COOCH.sub.2 C.tbd.CH, COOCH.sub.2 CMe.dbd.CH.sub.2, COOCH.sub.2 CH.sub.2 Br, COOCH.sub.2 CH.sub.2 Cl COOCH.sub.2 CH.sub.2 F, COOCH.sub.2 CCl.sub.3, COOCH.sub.2 CHF.sub.2, COOCH.sub.2 CF.sub.3, ##STR16## COOCH.sub.2 CCl.dbd.CH.sub.2, COOCH.sub.2 CCl.dbd.CHCl, COOCH.sub.2 OMe, COOCH.sub.2 CH.sub.2 OMe, COOCH.sub.2 CH.sub.2 OEt, COOCH.sub.2 OEt, COOCH.sub.2 SMe COOCH.sub.2 CH.sub.2 SMe, COOCH.sub.2 CH.sub.2 SEt, COOCH.sub.2 CH.sub.2 SCH.sub.2 CH.sub.2 Cl, COOCH.sub.2 SOMe, COOCH.sub.2 CH.sub.2 SOMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl, COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Br, COOCH.sub.2 CH.sub.2 OSO.sub.2 Me, COOCH.sub.2 CH.sub.2 OSO.sub.2 Ph-Me-4, COOCH.sub.2 OCH.sub.2 CH.sub.2 OMe, COOCH.sub.2 CH.sub.2 SO.sub.2 Me, COOCH.sub.2 CH.sub.2 SO.sub.2 Et, COOCH.sub.2 SO.sub.2 Me, COOCH.sub.2 CN, COOCH.sub.2 CH.sub.2 CN, COOCH.sub.2 CH.sub.2 CH.sub.2 CN, COOCH.sub.2 CH.sub.2 NHMe, COOCH.sub.2 CH.sub.2 NMe.sub.2, COOCH.sub.2 NMe.sub.2, COOCH.sub.2 CH.sub.2 NO.sub.2, COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2, COOCH.sub.2 OH, ##STR17## COOCH.sub.2 COMe, COOCH.sub.2 COBu-t, COOCh.sub.2 COPr-i, COOCH.sub.2 COPh, COOCH.sub.2 COOMe, COOCH.sub.2 COOEt, COOCHMeCOOMe, COOCMe.sub.2 OOMe, COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.dbd.CH.sub.2, COOCH.sub.2 CH.sub.2 OCH.sub.2 C.tbd.CH, COOCH.sub.2 CH.sub.2 OPh, COOCH.sub.2 OPh, COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph, COOCH.sub.2 SiMe.sub.3, COOSiMe.sub.3, COOSiEt.sub.3, COOPh, COOPh-Cl-4, COOPh-Me-4, COOPh-OMe-4, COOPh-NO.sub.2 -4, COOCH.sub.2 Ph, COOCH.sub.2 Ph-Cl-2, COOCH.sub.2 Ph-Cl-4, COOCHMePh, COOCH.sub.2 CH.sub.2 Ph, ##STR18## C(O)SMe, C(O)SEt, C(O)SPr-i, C(O)SPr-n, C(O)SBu-n, C(O)SBu-t, C(O)SBu-s, C(O)SBu-i, C(S)OMe, C(S)OEt, C(S)OPr-i, C(S)OPr-n, C(S)OBu-n, C(S)OBu-t, C(S)OBu-s, C(S)OBu-i, CSSMe, CSSEt, CSSPr-n, CSSPr-i, CONMe.sub.2, CONHMe, CONEt.sub.2, CONHEt, CONHPr-n, CONHPr-i, CONHBu-t, CONHBu-s, CONHBu-i, CONHBu-n, CONHAm-t, CONPr.sub.2 -i, CONPr.sub.2 -n, CONHPh, CONHPh-Me-4, CONHPh-NO.sub.2 -4, ##STR19## CONMeOMe, CONHCH.sub.2 CH.dbd.CH.sub.2, CON(CH.sub.2 CH.dbd.CH.sub.2).sub.2, CONHCH.sub.2 C.tbd.CH, CON(CH.sub.2 C.tbd.CH).sub.2, CONMePh, CONEtPh, CON(Me)Ph-Me-4, CONHSO.sub.2 Me, CONHSO.sub.2 CF.sub.3, COON.dbd.CMe.sub.2, ##STR20## COOCH.sub.2 OCOMe, COOCH.sub.2 OCOBu-t, Z: F, Cl, Br, I, NO.sub.2, OMe, OEt, OPr-n, OPr-i, CF.sub.3, CN, SMe, SOMe, SO.sub.2 Me, SCF.sub.3, SOCF.sub.3, SO.sub.2 CF.sub.3
Q: H, Me, Et, n-Pr, i-Pr, n-Bu, i-Bu, s-Bu, t-Bu, CH.sub.2 CH.sub.2 Cl, CH.sub.2 CF.sub.3, CHClMe, CH.sub.2 CH.sub.2 Br, CHClCH.sub.2 Cl, CH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 CMe.dbd.CH.sub.2, CH.sub.2 CH.dbd.CHMe, CH.sub.2 C.tbd.CH, CH.sub.2 CCl.dbd.CH.sub.2, CH.sub.2 CN, CH.sub.2 Ph, CH.sub.2 Ph-Cl-2, CH.sub.2 Ph-Cl-3, CH.sub.2 Ph-Me-2, ##STR21## CH.sub.2 Ph-Me.sub.2 -2,4, CH.sub.2 Ph-Me-4, CHMePh, CHEtPh, CH.sub.2 Ph-NO.sub.2 -2, CH.sub.2 Ph-CF.sub.3 -3, CH.sub.2 OMe, CH.sub.2 OEt, CH.sub.2 OH, CHMeOH, CH.sub.2 NHMe, CH.sub.2 NMe.sub.2, CHMeNMe.sub.2, CH.sub.2 COPh, CH.sub.2 COPh-NO.sub.2 -4, CH.sub.2 COPh-Me-4, CH.sub.2 COPh-Cl-4, CH.sub.2 COPh-Me.sub.2 -2,4, CH.sub.2 COPh-CF.sub.3 -4, CH.sub.2 Ac, CH.sub.2 COEt, CHMeAc, CH.sub.2 CO.sub.2 Me, CH.sub.2 CO.sub.2 Et, CH.sub.2 CO.sub.2 Pr-n, CH.sub.2 CO.sub.2 Pr-i, CH.sub.2 CO.sub.2 Bu-t, CH.sub.2 CO.sub.2 H, CHMeCO.sub.2 H, CH.sub.2 CONHMe, CH.sub.2 CONMe.sub.2, CH.sub.2 CONHEt, CH.sub.2 CONEt.sub.2, CH.sub.2 CONPr-n.sub.2, CH.sub.2 OCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 OAc, CH.sub.2 COEt, CH.sub.2 COPr-i, CH.sub.2 COBu-t, CH.sub.2 OCO.sub.2 Me, CH.sub.2 OCO.sub.2 Et, CH.sub.2 OCO.sub.2 Pr-i, CH.sub.2 OCO.sub.2 Bu-t, CH.sub.2 SMe, CH.sub.2 SEt, CH.sub.2 SCH.sub.2 CH.dbd.CH.sub. 2, CH.sub.2 SAc, CH.sub.2 SCOBu-t, CH.sub.2 SO.sub.2 Me, CH.sub.2 SO.sub.2 Et, CH.sub.2 SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 NHCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 NMeCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 NHAc, CH.sub.2 NHCOEt, CH.sub.2 NHCO.sub.2 Me, CH.sub.2 NHCO.sub.2 Et, CH.sub.2 NMeCO.sub.2 Me, COPh, COPh-Me-4, COPh-NO.sub.2 -2, COPh-Cl.sub.2 -2,4, Ac, COEt, COPr-n, COPr-i, COBu-n, COBu-t, COCH.sub.2 Cl, COCHCl.sub.2, COCCl.sub.3, COCF.sub.3, COCH.sub.2 OMe, COCH.sub.2 OPh, COCH.sub.2 CH.dbd.CHCH.sub.3, CO.sub.2 Me, CO.sub.2 Et, CO.sub.2 Bu-t, CO.sub.2 Pr-i, CONHMe, CONMe.sub.w, CONHEt, CONEt.sub.2, CONPr-n.sub.2, CON(CH.sub.2 CH.dbd.CH.sub.2).sub.2, CONMePh, ##STR22## CO.sub.2 CH.sub.2 Ph, CO.sub.2 Ph, SO.sub.2 Me, SO.sub.2 Et, SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2, SO.sub.2 Ph, SO.sub.2 Ph-Me-4, SO.sub.2 Ph-Cl-4, SO.sub.2 Ph-(NO.sub.2).sub.2 -2,4, SO.sub.2 CF.sub.3, P(.dbd.O)(OMe).sub.2, P(.dbd.O)(OEt).sub.2, P(.dbd.O)(OPr-n).sub.2, P(.dbd.O)(OPr-i).sub.2, P(.dbd.S)(OMe).sub.2, P(.dbd.S)(OEt).sub.2, P(.dbd.O)OMeOPh, P(.dbd.O)(OCH.sub.2 CH.dbd.CH.sub.2).sub.2, P(.dbd.O)OPhOCH.sub.2 CH.dbd.CH.sub.2
When Q is a hydrogen atom, the compound may readily form a salt with a metal or with an organic base.
As such a metal, sodium, potassium, calcium, lithium, barium, magnesium, iron, copper, nickel or manganese may be mentioned.
As such an organic base, methylamine, dimethylamine, trimethylamine, ethylamine, diethylamine, triethylamine, n-propylamine, di-n-propylamine, i-propylamine, di-i-propylamine, n-butylamine, i-butylamine, sec-butylamine, tert-butylamine, piperidine, pyrrolidine, morpholine, pyridine, N,N-dimethylaniline or choline may be mentioned.
In the course of researches on the herbicidal properties of various organic compounds with an aim to develop useful herbicides, the present inventors have found that the above-mentioned compound of the present invention exhibits excellent herbicidal activities against narrow leaf weeds (gramineous and cyperaceous weeds) and against broad leaf weeds and no substantial phytotoxicity against useful plants e.g. crop plants such as Zea mays (corn), Sorghum bicolor (sorgo), Triticum spp (wheat) and Hordeum vulgare (barley). The present invetion has been accomplished on the basis of this discovery.
The compound of the present invention exhibits strong herbicidal activities in each of soil treatment, soil incorporaton treatment and foliage treatment. On the other hand, it exhibits no phytotoxicity against crop plants such as Zea mays, Sorghum bicolor, Triticum spp and Hordeum vulgare in a practical application in any of soil treatment, soil incorporation treatment and foliage treatment. Thus, the compound of the present invention has high selectivity and it is extremely effective for controlling weeds during the cultivation of these crop plants. Namely, the compound of the present invention exhibits strong herbicidal activities against noxious weeds such as Setaria viridis (green foxtail), Echinochloa crus-galli (barnyardgrass), Amaranthus lividus (livid amaranth), Polygonum longisetum (persicaria blumei gross), Xanthium strumarium (cocklebur), Abutilon theophrasti (velvet leaf) and Cyperus esculentus (yellow nutsedge), which develop during the cultivation of Zea mays or Sorghum bicolor. The herbicidal activities against gramineous weeds and Cyperus esculentus are remarkably high and extremely unique. Heretofore, during the cultivation of Zea mays or Sorghum bicolor, it has been common to employ atrazine or cyanazine as a triazine-type herbicide, or alachlor or metolachlor as an acid anilide-type herbicide. However, atrazine and cyanazine have poor herbicidal activities against gramineous weeds although they show high activities against broad leaf weeds, and their activities against Cyperus esculentus are very low. On the other hand, alachlor and metolachlor have poor activities against broad leaf weeds although their activities against gramineous weeds are high, and their activities against Cyperus esculentus are very poor. Thus, it has been difficult to eradicate all the weed species by a single application of such herbicides.
As a result of various studies, the present inventors have found the compound of the present invention which exhibits excellent herbicidal effects against a wide range of weeds, and the present invention has been accomplished on the basis of this discovery. The compound of the present invention also has a feature that it exhibits no phytotoxicity against crop plants such as Zea mays, Sorghum bicolor, Triticum spp and Hordeum vulgare and thus can safely be applied to the fields for such crop plants.
Further, the compound of the present invention includes a compound which shows selectivity between Oryza sativa (rice) and Echinochloa crus-galli (barnyardgrass), and it also includes a compound having selectivity for a useful plant such as Gossypium spp (cotton), Beta vulgaris (sugar beat) or Glycine max (soybean).
Heretofore, it has been known that 4-benzoylpyrazole derivatives have excellent herbicidal activities. For example, pyrazolate (common name) is commercially available and widely used for practical application. However, such conventional herbicides are restricted in their application to paddy fields, and their activities are very poor in their application to upland fields. Whereas, as a result of extensive reasearch for many years on 4-benzoylpyrazole derivatives, the present inventors have finally found that the compound of the present invention which simultaneously satisfies the various conditions for substituents in the structure as specified above, exhibits strong herbicidal activities in the application to upland fields in each of soil treatment, soil incorporation and foliage treatment. It has been found that the compound of the present invention exhibits particularly high activities against gramineous weeds and Cyperus esculentus.
The compound of the present invention can readily be prepared by any one of the following reactions. ##STR23##
In the above formulas, A, B, X, Y, Z and Q are as defined above, E is a halogen atom, a methanesulfonyloxy group or a p-toluenesulfonyloxy group. Further, ##STR24## and may be represented by either formula. DCC is N,N'-dicyclohexylcarbodiimide.
Reaction scheme (1) represents a reaction wherein benzoic acid having suitable substituents and 5-hydroxypyrazole are reacted in an inert solvent in the presence of DCC and a base to obtain 4-benzoyl-5-hydroxypyrazole. DCC is used in an amount of from 1.0 to 1.5 mols per mole of the benzoic acid and pyrazole. The solvent may be any solvent so long as it is inert to the reaction. Particularly preferred is tert-butyl alcohol, tert-amyl alcohol or isopropyl alcohol. The base may not necessarily be required. However, in general, the yield can be improved by using a base. There is no particular restriction as to the base, but potassium carbonate or sodium carbonate may preferably be employed. The reaction temperature may range from room temperature to the boiling point of the solvent, but is preferably from 50.degree. to 100.degree. C.
The reaction time is usually from 0.5 to 20 hours.
Reaction scheme (2) shows a reaction wherein benzoyl chloride having suitable substituents and 5-hydroxypyrazole are reacted to form a benzoyl ester, which is then rearranged to a 4-benzoyl compound.
The benzoyl esterification can be accomplished in an inert solvent (such as an aromatic hydrocarbon, a fatty acid ester, a halogenated hydrocarbon, an ether, acetonitrile, dimethylsulfoxide or N,N'-dimethylformamide) or in a two phase system with such a solvent and water or in a mixture of such solvents in the presence of a suitable dehydrochlorinating agent (e.g. an inorganic base such as sodium hydroxide, potassium hydroxide or sodium hydrogencarbonate, or an organic base such as pyridine or triethylamine) at a temperature of from room temperature to 100.degree. C. for from 10 minutes to 5 hours.
The rearrangement reaction can be accomplished by means of a Lewis acid such as anhydrous aluminum chloride or a base. As the base, potassium carbonate, calcium hydroxide or sodium carbonate may be used. The Lewis acid or base is used usually in an amount of from 1 to 10 mol times.
No solvent is required. However, in some cases, it is advantageous to use a solvent having a suitable boiling point to improve the operation efficiency or the yield. As such an advantageous example, use of dioxane or diglyme may be mentioned.
The reaction temperature is usually from 50.degree. to 150.degree. C., and the reaction time is usually from 15 minutes to 10 hours.
Reaction scheme (3) shows a reaction wherein 4-benzoyl-5-hydroxypyrazole is condensed with a halide, a methanesulfonic acid ester or a p-toluenesulfonic acid ester.
For this reaction, it is preferred to employ from 1 to 3 mol times of a dehydrohalogenating agent. As such a dehydrohalogenating agent, an inorganic base such as sodium hydroxide, potassium hydroxide, sodium carbonate, sodium hydrogencarbonate or potassium carbonate, or an organic base such as pyridine or triethylamine, may be mentioned.
There is no particular restriction as to the solvent so long as it is inert to the reaction. A wide range of solvents including an aromatic hydrocarbon, a fatty acid ester, a halogenated hydrocarbon, an ether, a ketone, an aliphatic hydrocarbon, acetonitrile, dimethylsulfoxide and dimethylformamide may be used.
The reaction temperature may be optionally selected within a range of from room temperature to the boiling point of the solvent. The reaction time is usually from 30 minutes to 30 hours.
Reaction scheme (4) shows a reaction wherein 4-benzoyl-5-hydroxypyrazole is converted to a 5-chloro compound by a chlorinating agent, followed by condensation with a suitable alcohol or acid.
As the chlorinating agent, phosphorus oxychloride, phosphorus pentachloride or thionyl chloride may be mentioned.
As the solvent, a wide range of solvents inert to the reaction, such as dimethylformamide, may be employed. However, the reaction can be conducted without any solvent.
The reaction temperature is preferably from 30.degree. to 150.degree. C., and the reaction time is usually from 30 minutes to 10 hours. In some cases, the reaction time may be shortened or the yield may be improved by an addition of a dehydrohalogenating agent.
The condensation reaction with an alcohol or acid is conducted by an addition of a dehydrohalogenating agent.
A such a dehydrohalogenating agent, a base such as sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium alkoxide or sodium hydride may be employed.
The solvent may be any solvent which is inert to the reaction (such as an aromatic hydrocarbon, an ether, a ketone or N,N'-dimethylformamide). The reaction temperature may be selected within a range of from room temperature to the boiling point of the solvent.
The benzoic acids or benzoyl chlorides used as the starting materials for the compounds of the present invention may readily be prepared by a proprer combination of various known syntheses. For instance, compounds wherein the substituent Z in the benzene ring is --S(O).sub.n CH.sub.3 can be prepared in accordance with the following reaction schemes. ##STR25##
In the above formulas, X and Y are as defined above, and Hal is a halogen atom.
Now, the preparation of benzoic acids will be described in detail with reference to Reference Examples. However, it should be understood that the present invention is by no means restricted by such specific Examples.
REFERENCE EXAMPLE 1
Preparation of 4-methanesulfonyl-3-methoxymethyl-2-methyl benzoic acid and 3-methoxymethyl-2-methyl-4-methylthio benzoic acid
(1) 2-Methyl-3-nitrobenzyl alcohol
39.0 g (0.2 mol) of methyl 2-methyl-3-nitrobenzoate was dissolved in 600 ml of tert-butanol, and 19.0 g of sodium borohydride was added thereto. Under refluxing, 150 ml of methanol was dropwise added thereto over a period of 1 hour. The refluxing was continued further for 1 hour to complete the reaction. The reaction mixture was left to cool, and then water was added thereto. The solvent was distilled off under reduced pressure. To the residue, water and chloroform were added, and the organic layer was separated and dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain 30.7 g of 2-methyl-3-nitrobenzyl alcohol.
(2) 2-Methyl-3-nitrobenzyl methyl ether
30.1 g (0.18 mol) of 2-methyl-3-nitrobenzyl alcohol obtained in the preceding step was dissolved in 200 ml of benzene, and 0.2 g of tetra-n-butylammonium bromide and a 50% aqueous solution of 20.1 g of sodium hydroxide were added thereto sequentially. Then, 27.2 g of dimethyl sulfate was dropwise added thereto at room temperature. Further, the reaction was conducted for 3 hours under stirring. Water was added to the reaction solution, and the organic layer was separated and washed sequentially with water, a 2% hydrochloric acid aqueous solution, water and a saturated sodium chloride aqueous solution. Then, the solvent was distilled off to obtain 30.9 g of 2-methyl-3-nitrobenzyl methyl ether as an oily substance.
(3) 3-Methoxymethyl-2-methylaniline
To 30.7 g (0.17 mol) of the above-mentioned 2-methyl-3-nitrobenzyl methyl ether, 200 ml of methanol was added. After the compound was dissolved in methanol, 92 ml of concentrated hydrochloric acid was gradually added thereto. Then 30.4 g of iron powder was gradually added so that the reaction temperature became at a level of not higher than 60.degree. C., and the reaction was continued further for 1 hour.
To the reaction solution, 300 ml of water was added, and sodium hydroxide was added until the pH became higher than 8. To the slurry thus obtained, chloroform was added, and the mixture was thoroughly stirred. Then, the solid was separated by filtration, and an organic layer was separated from the filtrate.
This organic layer was washed sequentially with water and a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Further, the solvent was distilled off under reduced pressure to obtain 23.1 g of 3-methoxymethyl-2-methylaniline as an oily substance.
(4) 3-Methoxymethyl-2-methyl-4-thiocyanoaniline 22.6 g (0.15 mol) of 3-methoxymethyl-2-methylaniline was dissolved in 300 ml of methanol. Then, 36.5 g of sodium thiocyanate was added thereto to obtain a uniform solution. This solution was cooled to 0.degree. C., and 100 ml of a saturated methanol solution of sodium bromide with 25.2 g of bromine was dropwise added thereto so that the reaction temperature did not exceed 5.degree. C. After the dropwise addition, the mixture was stirred at a temperature of not higher than 5.degree. C. for 1 hour and at room temperature for 1 hour to complete the reaction. The reaction solution was poured into 1 liter of water and neutralized with a 5% sodium carbonate aqueous solution. Chloroform was added to extract the oily substance. The chloroform layer was washed with water and a saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure to obtain 29.6 g of the desired product.
(5) 3-Methoxymethyl-2-methyl-4-methylthioaniline
29.1 g (0.14 mol) of 3-methoxymethyl-2-methyl-4-thiocyanoaniline was dissolved in 200 ml of ethanol and mixed with 100 ml of an aqueous solution containing 33.6 g of sodium sulfide nonahydrate at room temperature. Then, 21.9 g of methyl iodide was dropwise added thereto, and the mixture was reacted at room temperature for 3 hours. After completion of the reaction, the solvent was distilled off under reduced pressure, and water and chloroform were added to the residue. Then, the organic layer was separated and washed sequentially with water and a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure to obtain 25.6 g of the desired product as an oily substance.
(6) 3'-Iodo-2'-methyl-6'-methylthiobenzyl methyl ether
To 25.6 g (0.13 mol) of 3-methoxymethyl-2-methyl-4-methylthioaniline, 100 ml of water and 33 ml of concentrated hydrochloric acid were added to convert it to an aniline hydrochloride. This solution was cooled to 0.degree. C., and 30 ml of an aqueous solution containing 9.3 g of sodium nitrite was dropwise added thereto so that the reaction temperature did not exceed 5.degree. C. After completion of dropwise addition, stirring was continued further for 30 minutes to complete diazotization. 100 ml of an aqueous solution containing 33 g of potassium iodide was heated to 70.degree. C., and the aqueous solution of the diazonium salt obtained above was gradually added thereto and decomposed. The reaction solution was stirred further for 1 hour at 70.degree. C. and then left to cool. The oil component was extracted with benzene. The benzene layer was washed sequentially with water, a saturated sodium hydrogensulfite aqueous solution, water and a saturated sodium chloride aqueous solution. Then, the solvent was distilled off under reduced pressure, and the residue was purified by column chromatography (eluent:benzene) to obtain 30.0 g of the desired product. Melting point: 56.0.degree.-59.0.degree. C.
(7) 3-Methoxymethyl-2-methyl-4-methylthiobenzoic acid
27.7 g (0.09 mol) of 3'-iodo-2'-methyl-6'-methylthiobenzyl methyl ether was dissolved in 100 ml of dried tetrahydrofuran, and 63 ml of a 1.5M n-butyllithium n-hexane solution was dropwise added thereto at -70.degree. C. After the dropwise addition, the mixture was stirred for 15 minutes at the same temperature, and then dried carbon dioxide gas was thoroughly blown into the reaction solution until the heat generation of the reaction solution stopped. After the reaction, the temperature of the solution was returned to room temperature, and water and diethyl ether were added for liquid separation. The aqueous layer thus obtained was further washed twice with diethyl ether, and then concentrated hydrochloric acid was added to bring the pH<1. Precipitated crystals were collected by filtration, thoroughly washed with water and dried to obtain 14.4 g of the desired product. Melting point: 192.0.degree.-194.0.degree. C.
(8) 4-Methanesulfonyl-3-methoxymethyl-2-methylbenzoic acid
To 11.3 g (0.05 mol) of 3-methoxymethyl-2-methyl-4-methylthiobenzoic acid, 120 ml of acetic acid and 120 ml of a 35% hydrogen peroxide aqueous solution were added, and the mixture was reacted at 80.degree. C. for 1 hour. After cooling, the reaction solution was poured into ice water, whereupon precipitated crystals were collected by filtration, then washed with water and dried to obtain 12.3 g of the desired product. Melting point: 129.0.degree.-131.0.degree. C.
REFERENCE EXAMPLE 2
Preparation of 3-methoxycarbonyl-2-methyl-b 4-methylthiobenzoic acid and 4-methanesulfonyl-3-methoxycarbonyl-2-methylbenzoic acid
(1) Methyl 3-amino-2-methylbenzoate
40 g of methyl 2-methyl-3-nitrobenzoate was dissolved in 120 ml of methanol, and 157 g of concentrated hydrochloric acid was added thereto. Then, 36.8 g of iron powder was gradually added while maintaining the mixture at a temperature of not higher than 60.degree. C. The mixture was stirred at room temperature for 4 hours and then poured into 1 liter of ice water. The solution was neutralized with sodium carbonate and extracted with chloroform (after filtering off insolubles). The extract was washed with a saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain 27.8 g of the desired product as an oily substance.
(2) Methyl 3-amino-2-methyl-6-thiocyanobenzoate
While maintaining a solution comprising 27.7 g of methyl 3-amino-2-methylbenzoate, 41.5 g of sodium thiocyanate and 250 ml of methanol at a temperature of not higher than 0.degree. C., 100 ml of sodium bromide-saturated methanol with 28.1 g of bromine was slowly dropwise added thereto. The mixture was stirred at room temperature for 3 hours and then poured into 1 liter of ice water. The solution was neutralized with sodium carbonate and then extracted with chloroform. The extract was washed with a saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain 34.0 g of the desired product as an oily substance.
(3) Methyl 3-amino-2-methyl-6-methylthiobenzoate
To a solution comprising 39.5 g of sodium sulfide nonahydrate and 110 ml of water, a solution comprising 32.9 g of methyl 3-amino-2-methyl-6-thiocyanobenzoate and 300 ml of ethanol was dropwise added. The mixture was stirred at room temperature for 1.5 hours, and 24.0 g of methyl iodide was dropwise added under cooling with ice. The mixture was stirred further at room temperature for 2 hours and then concentrated under reduced pressure. A saturated sodium chloride aqueous solution was added thereto, and the mixture was extracted with chloroform. The extract was dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain 30.1 g of the desired product as an oily substance.
(4) Methyl 3-iodo-2methyl-6-methylthiobenzoate 28 g of methyl 3-amino-2-methyl-6-methylthiobenzoate was stirred in 150 ml of concentrated hydrochloric acid at room temperature for 2 hours to convert it to a hydrochloride. Then, while maintaining the mixture at a temperature of not higher than 0.degree. C., a solution comprising 11.9 g of sodium nitrite and 20 ml of water was dropwise added thereto to obtain a diazonium salt solution. The diazonium salt solution was dropwise added to a solution comprising 28.4 g of potassium iodide and 90 ml of water while maintaining the solution at 80.degree. C. After completion of the dropwise addition, the mixture was stirred at 80.degree. C. for 15 minutes and left to cool. Water was added thereto, and the mixture was extracted with chloroform. The extract was washed with an aqueous sodium hydrogensulfite solution and water and then dried over anhydrous sodium sulfate. The solvent was distilled off to obtain 40 g of the desired product as a crude product. The crude product was purified by silica gel column chromatography (eluted with benzene) to obtain 36.0 g of a purified product as an oily substance.
(5) 3-Methoxycarbonyl-2-methyl-4-methylthiobenzoic acid
While maintaining a solution comprising 20.0 g of methyl 3-iodo-2-methyl-6-methylthiobenzoate and 70 ml of dried tetrahydrofuran at a temperature of not higher than -60.degree. C. under a nitrogen atmosphere, 42 ml of a 1.5M n-butyllithium n-hexane solution was dropwise added thereto. Fifteen minutes later, dried carbon dioxide gas was thoroughly blown into the mixture while maintaining it at a temperature of not higher than -50.degree. C. After purging carbon dioxide gas with nitrogen, 12.7 g of diisopropylamine was dropwise added thereto, and the mixture was stirred until the temperature reached room temperature. The mixture was concentrated under reduced pressure. Water was added thereto and the mixture was washed with chloroform. The aqueous solution was acidified with concentrated hydrochloric acid and then extracted with chloroform. The extract was dried over anhydrous sodium sulfate. The solvent was distilled off to obtain 7.5 g of the desired product. Melting point: 178.degree.-178.5.degree. C.
(6) 4-Methanesulfonyl-3-methoxycarbonyl-2-methylbenzoic acid
A solution comprising 5.0 g of 3-methoxycarbonyl-2-methyl-4-methylthiobenzoic acid, 25 ml of acetic acid and 25 ml of hydrogen peroxide (35%) was stirred at 80.degree. C. for 3 hours. After cooling, the mixture was poured into ice water and extracted with chloroform. The extract was dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain 5.1 g of the desired product. Melting point: 151.degree.-152.degree. C.
REFERENCE EXAMPLE 3
Preparation of 2-chloro-3-ethylthiomethyl-4-methanesulfonylbenzoic acid
(1) Methyl 3-bromomethyl-2-chloro-4-methanesulfonylbenzoate
12.1 g of methyl 2-chloro-4-methanesulfonyl-3-methylbenzoate was dissolved in 250 ml of carbon tetrachloride, and the solution was refluxed under stirring. Then, 7.5 g of bromine and 1 g of benzoyl peroxide were gradually added thereto over a period of 30 minutes, and the solution was further refluxed for 4 hours under heating. After cooling, 200 ml of chloroform was added thereto, and the mixture was washed with a 5% sodium hydrogensulfite aqueous solution. The organic layer was separated and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure to obtain a crude product. The crude product was washed with ethyl ether to obtain 13.2 g of crystals of the desired product. Melting point: 77.degree.-78.degree. C.
(2) Methyl 2-chloro-3-ethylthiomethyl-4-methanesulfonylbenzoate
To 100 ml of tetrahydrofuran, 1.3 g of ethanethiol and 1.5 g of potassium carbonate and then 4.4 g of methyl 3-bromomethyl-2-chloro-4-methanesulfonylbenzoate were added, and the mixture was stirred for 1 day at room temperature. Then, the mixture was stirred further for 1 hour at a temperature of from 50.degree. to 60.degree. C. After cooling, chloroform was added thereto, and the mixture was washed with a dilute potassium carbonate aqueous solution. The chloroform layer was separated and dried. Then, the solvent was distilled off to obtain 4.1 g of methyl 2-chloro-3-ethylthiomethyl-4-methanesulfonylbenzoate as an oily substance.
(3) 2-Chloro-3-ethylthiomethyl-4-methanesulfonylbenzoic acid
To a solution mixture comprising 50 ml of a 10% sodium hydroxide aqueous solution and 150 ml of methanol, 3.9 g of methyl 2-chloro-3-ethylthiomethyl-4-methanesulfonylbenzoate was added, and the mixture was stirred at room temperature for 30 minutes. Methanol was distilled off under reduced pressure, and a dilute hydrochloric acid was added to the residue for acid preparation. The mixture was extracted with ethyl acetate, and the extract was dried. Then, the solvent was distilled off to obtain 3.5 g of the desired product. Melting point: 172.degree.-174.degree. C.
REFERENCE EXAMPLE 4
Preparation of 2-chloro-4-methanesulfonyl-3-methoxymethylbenzoic acid
(1) Methyl-2-chloro-4-methanesulfonyl-3-methoxymethylbenzoate
To a solution comprising 12.0 g of methyl 3-bromomethyl-2-chloro-4-methanesulfonylbenzoate prepared in Reference Example 3(1) and 100 ml of methanol, 50 ml of a methanol solution containing 1.7 g of sodium methoxide was added, and the mixture was stirred at room temperature overnight. The solvent was distilled off under reduced pressure. Then, dilute hydrochloric acid was added to the residue, and the mixture was extracted with chloroform. The extract was washed with water and dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain 9.5 g of the desired product as a crude product. The crude product was purified by silica gel column chromatography (eluted with benzene) to obtain 7.5 g of a purified product as an oily substance.
(2) 2-Chloro-4-methanesulfonyl-3-methoxymethylbenzoic acid
To a solution comprising 3.0 g of methyl 2-chloro-4-methanesulfonyl-3-methoxymethylbenzoate and 20 ml of methanol, a solution comprising 0.57 g of sodium hydroxide (93%) and 2 ml of water was added, and the mixture was stirred at room temperature for 30 minutes. After an addition of 10 ml of water, the mixture was concentrated under reduced pressure. Then, dilute hydrochloric acid was added thereto, and the mixture was extracted with chloroform. The extract was dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain 2.6 g of the desired product. Melting point: 137.degree.-141.degree. C.
REFERENCE EXAMPLE 5
Preparation of 2-chloro-4-methanesulfonyl-3-methoxymethylbenzoic acid (alternative method of Reference Example 4)
The desired product was prepared in the same manner as in Reference Example 1. Melting point: 137.degree.-141.degree. C.
The physical properties of the intermediates were as follows:
(1) 2-Chloro-3-nitrobenzyl alcohol: Oily substance
(2) 2'-Chloro-3'-nitrobenzyl methyl ether: Oily substance
(3) 2-Chloro-3-methoxymethylaniline: Oily substance
(4) 2-Chloro-3-methoxymethyl-4-thiocyanoaniline: Melting point: 90.degree.-96.degree. C.
(5) 2-Chloro-3-methoxymethyl-4-methylthioaniline: Oily substance
(6) 2'-Chloro-3'-iodo-6'-methylthiobenzyl methyl ether: Melting point: 53.degree.-56.degree. C.
REFERENCE EXAMPLE 6
Preparation of 2-chloro-4-methanesulfonyl-3-methoxycarbonyl benzoic acid
The desired product was prepared in the same manner as in Reference Example 2. Melting point 160.degree.-162.degree. C.
The physical properties of the intermediates were as follows:
(1) Methyl 3-amino-2-chlorobenzoate: Oily substance
(2) Methyl 3-amino-2-chloro-6-thiocyanobenzoate: Melting point: 80.degree.-83.degree. C.
(3) Methyl 3-amino-2-chloro-6-methylthiobenzoate: Melting point: 70.degree.-72.degree. C.
(4) Methyl 2-chloro-3-iodo-6-methylthiobenzoate: Oily substance
(5) 2-Chloro-3-methoxycarbonyl-4-methylthiobenzoic acid: Melting point: 176.degree.-179.degree. C.
REFERENCE EXAMPLE 7
Preparation of 4-methanesulfonyl-3-[(2-methoxyethyl)oxycarbonyl]-2-methylbenzoic acid
The desired compound was prepared in the same manner as in Reference Example 2. Melting point: 118.degree.-121.degree. C.
The physical properties of the intermediates were as follows:
(1) 2-Methoxyethyl 3-amino-2-methylbenzoate: Oily substance
(2) 2-Methoxyethyl 3-amino-2-methyl-6-thiocyanobenzoate: Melting point: 79.degree.-81.degree. C.
(3) 2-Methoxyethyl 3-amino-2-methyl-6-methylthiobenzoate: Oily substance
(4) 2-Methoxyethyl 3-iodo-2-methyl-6-methylthiobenzoate: Oily substance
(5) 3-[(2-methoxyethyl)oxycarbonyl]-2-methyl-4-methylthiobenzoic acid: Melting point: 90.degree.-93.degree. C.
REFERENCE EXAMPLE 8
Preparation of 2-methyl-4-methylthio-3-n-propoxycarbonylbenzoic acid and 4-methanesulfonyl-2-methyl-3-n-propoxycarbonylbenzoic acid
(1) Methyl 3-bromo-2-methyl-6-methylthiobenzoate
16.1 g of the compound of Reference Example 2(3) was stirred in 150 ml of hydrobromic acid (48%) to convert it into a hydrobromide. While maintaining the solution at a temperature of not higher than 0.degree. C., a solution comprising 7.2 g of sodium nitrite and 20 ml of water was dropwise added to obtain a diazonium salt solution. The diazonium salt solution was dropwise added to a solution comprising 6.0 g of cuprous bromide and 7.7 g of hydrobromic acid (48%) while refluxing the solution under heating. After completion of the dropwise addition, the mixture was further refluxed for 1 hour under heating and then left to cool. Ice water was added thereto, and the mixture was extracted with chloroform. The extract was washed with an aqueous sodium hydrogensulfite solution and water and then dried over anhydrous sodium sulfate. The solvent was distilled off to obtain 19.2 g of the desired product as a crude product. The crude product was purified by silica gel column chromatography (eluted with benzene) to obtain 17.1 g of a purified product as an oily substance.
(2) 3-Bromo-2-methyl-6-methylthiobenzoic acid
To 100 ml of an ethanol solution containing 17.0 g of methyl 3-bromo-2-methyl-6-methylthiobenzoate, 16 g of a 50% sodium hydroxide aqueous solution was added, and the mixture was refluxed for 3 hours under heating. The reaction mixture was concentrated under reduced pressure. Then, water was added thereto, and the mixture was washed with chloroform. The aqueous layer was acidified with concentrated hydrochloric acid and extracted with chloroform. The extract was dried over anhydrous sodium sulfate. The solvent was distilled off to obtain 15.9 g of the desired product. Melting point: 98.degree.-103.degree. C.
(3) n-Propyl 3-bromo-2-methyl-6-methylthiobenzoate
Thionyl chloride was added to 15.8 g of 3-bromo-2-methyl-6-methylthiobenzoic acid, and the mixture was refluxed for 4 hours under heating. Thionyl chloride was distilled off, and 70 ml of n-propanol was added to the residue under cooling with ice. Then, a solution comprising 7.3 g of pyridine and 20 ml of n-propanol was dropwise added thereto. The mixture was stirred at room temperature overnight and then concentrated under reduced pressure. Then, ethyl acetate was added thereto, and the mixture was washed sequentially with a 5% sodium carbonate aqueous solution, 10% hydrochloric acid and water and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure to obtain 18 g of the desired product as a crude product. The crude product was purified by silica gel column chromatography (eluted with benzene) to obtain 16.6 g of a purified product as an oily substance.
(4) 3-Bromo-2-methyl-6-methylthiobenzoic acid
This product was prepared in the same manner as in Reference Example 2(5). Melting point: 138.degree.-142.degree. C.
(5) 3-Bromo-6-methanesulfonyl-2-methylbenzoic acid
This compound was prepared in the same manner as in Reference Example 2(6). Melting point: 142.degree.-146.degree. C.
REFERENCE EXAMPLE 9
Preparation of 2-chloro-3-isopropoxycarbonyl-4-methanesulfonylbenzoic acid
This compound was prepared from the compound of Reference Example 6(4) in the same manner as in Reference Example 8(2)-(5). Melting point: 146.degree.-148.degree. C.
The physical properties of the intermediates were as follows:
(1) 2-Chloro-3-iodo-6-methylthiobenzoic acid: Melting point: 155.degree.-159.degree. C.
(2) Isopropyl 2-chloro-3-iodo-6-methylthiobenzoate: Oily substance
(3) 2-Chloro-3-isopropoxycarbonyl-4-methylthiobenzoic acid: Melting point: 114.degree.-118.degree. C.
REFERENCE EXAMPLE 10
Preparation of 3-(1-methoxyethyl)-2-methyl-4-methylthiobenzoic acid and 4-methanesulfonyl-3-(1-methoxyethyl)-2-methylbenzoic acid
(1) 2'-Methyl-3'-nitroacetophenone
To 5.4 g of metal magnesium, 5 ml of absolute ethanol and 0.5 ml of carbon tetrachloride were dropwise added under a dry nitrogen stream. Further, 130 ml of dried diethyl ether was added under refluxing, and then a solution comprising 25 ml of a diethyl ether, 35.2 g of diethyl malonate and 20 ml of ethanol was dropwise added at a rate to maintain the refluxing. After completion of the dropwise addition, refluxing was continued for 3 hours to prepare diethyl ethoxymagnesiomalonate. To the solution of diethyl ethoxymagnesiomalonate thus obtained, 150 ml of a diethyl ether solution of 40.0 g of 2-methyl-3-nitrobenzoic acid chloride prepared from 2-methyl-3-nitrobenzoic acid and thionyl chloride, was dropwise added over a period of 20 minutes under refluxing, and the reaction was continued for 2 hours. After cooling, dilute sulfuric acid was added thereto for hydrolysis. The diethyl ether layer was washed sequentially with water and a saturated sodium chloride aqueous solution. Then, the solvent was distilled off under reduced pressure, and the residue was dried to obtain a crude product of diethyl 2-(2-methyl-3-nitrobenzoyl)malonate. To this crude product, a mixture comprising 7.5 ml of concentrated sulfuric acid, 60 ml of acetic acid and 40 ml of water was added, and the mixture was refluxed for 6 hours under heating. Then, the mixture was adjusted to pH>10 with a 20% sodium hydroxide aqueous solution. Precipitated oil component was extracted with chloroform. This chloroform layer was washed sequentially with water and a sodium chloride aqueous solution. Then, the solvent was distilled off under reduced pressure to obtain 34.0 g of the desired product. (Yield: 95%) Melting point: 53.0.degree.-54.0.degree. C.
(2) Preparation of 1-methyl-2'-methyl-3'-nitrobenzyl alcohol
To 50 ml of a methanol solution of 0.5 g of sodium hydroxide, 0.9 g of sodium borohydride was added at 0.degree. C., and then 100 ml of a methanol solution of 14.3 g of 2'-methyl-3'-nitroacetophenone was dropwise added thereto. The temperature of the mixture was returned to room temperature and reacted for 1 hour. After the reaction, the reaction mixture was poured into water and extracted with benzene. The subsequent operation was conducted in a usual manner to obtain 14.3 g of the desired product as an oily substance. (Yield: 99%)
Subsequently, the synthesis was conducted in the same manner as in Reference Example 1 to obtain intermediates (3) to (9).
(3) 1-Methyl-2'-methyl-3'-nitrobenzyl methyl ether: Oily substance
(4) 1-Methyl-3'-amino-2'-methylbenzyl methyl ether: Oily substance
(5) 1-Methyl-3'-amino-2'-methyl-6'-thiocyanobenzyl methyl ether: Solid
(6) 1-Methyl-3'-amino-2'-methyl-6'-methylthiobenzyl methyl ether: Oily substance
(7) 1-Methyl-3'-iodo-2'-methyl-6'-methylthiobenzyl: Oily substance
(8) 3-(1-Methoxyethyl)-2-methyl-4-methylthiobenzoic acid: Oily substance
(9) 4-Methanesulfonyl-3-(1-methoxyethyl)-2-methylbenzoic acid: Melting point: 106.degree.-109.degree. C.
The physical properties of benzoic acids prepared in accordance with the preceding Reference Examples will be given in Tables 1 and 2 including those of the preceding Reference Examples.
TABLE 1______________________________________ ##STR26##X Y Z Melting point (.degree.C.)______________________________________Me CH.sub.2 OMe SMe 192.about.194Me CH.sub.2 OMe SO.sub.2 Me 129.about.131Me CO.sub.2 Me SMe 178.about.178.5Me CO.sub.2 Me SO.sub.2 Me 151.about.152Me CH.sub.2 OEt SMe 172.about.175Me CH.sub.2 OEt SO.sub.2 Me 160.about.162Cl CO.sub.2 Me Cl 183.about.185Me CHMeOMe SMe Oily substanceMe CHMeOMe SO.sub.2 Me 106.about.109Me CO.sub.2 Pri SMe 151.about.153Me CO.sub.2 Pri SO.sub.2 Me 153.about.155Cl CH.sub.2 OMe SO.sub.2 Me 137.about.141Me CH.sub.2 OPri SMe 134.about.138Me CH.sub.2 OPri SO.sub.2 Me 159.about.161Me CO.sub.2 CH.sub.2 CH.sub.2 OMe SMe 90.about.93Me CO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me 118.about.121Cl CH.sub.2 SEt SO.sub.2 Me 172.about.174Me CO.sub.2 Et SMe 114.about.120Me CO.sub.2 Et SO.sub.2 Me 119.7.about. 127.9Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me 93.about.95Cl ##STR27## SO.sub.2 Me Oily substanceMe ##STR28## SMe 169.about.172Me ##STR29## SO.sub.2 Me 129.about.134Me CO.sub.2 Prn SMe 138.about.142Me CO.sub.2 Prn SO.sub.2 Me 142.about.146Cl CH.sub.2 OH SO.sub.2 Me 240.about.245Cl CO.sub.2 Me SMe 176.about.179Cl CO.sub.2 Me SO.sub.2 Me 160.about.162Cl CO.sub.2 Pri SMe 114.about.118Cl CO.sub.2 Pri SO.sub.2 Me 146.about.148OMe CO.sub.2 Me SMe 107.about.109OMe CO.sub.2 Me SO.sub.2 Me 113.about.119Me CHEtOMe SMe Oily substanceMe CHEtOMe SO.sub.2 Me Oily substanceMe CHMeOEt SMe Oily substanceMe CHMeOEt SO.sub.2 Me Oily substanceCl CH.sub.2 OCH.sub.2 CCH SO.sub.2 Me 166.about.169Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 SO.sub.2 Me 118.about.119Cl CH.sub.2 OAmn SO.sub.2 Me Oily substanceMe CO.sub.2 Ami SMe 98.about.105Me CO.sub.2 Ami SO.sub.2 Me 107.about.113Cl CH.sub.2 OCH.sub.2 CF.sub.3 SO.sub.2 Me 155.about.157OMe CH.sub.2 OMe SMe 157.about.161OMe CH.sub.2 OMe SO.sub.2 Me Oily substanceMe CO.sub.2 CH.sub.2 CH.sub.2 Cl SMe 138.about.144Me CO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me 121.about.126______________________________________
TABLE 2______________________________________X Y Z .sup.1 H--NMR (.delta., ppm) [Solvent]______________________________________Me CHEtOMe SO.sub.2 Me 1.19(3H,t), 1.63(3H,d), 2.78(3H,s), 3.18(3H,s), 3.35(2H,q), 5.63(1H,q), 7.81(2H, A-B q), 10.20(1H,s) [CDCl.sub.3 ]Me CHMeOEt SMe 1.00(3H,t), 1.67.about.2.26(2H,m), 2.46(3H,s), 2.69(3H,s), 3.21(3H,s), 4.91(1H,d-d) 7.48(2H, A-Bq), 10.2(1H,s) [CDCl.sub.3 ]Me CHMeOEt SO.sub.2 Me 1.04(3H,t), 1.60.about.2.20(2H,m), 2.66(3H,s), 3.23(6H,s), 5.26(1H,d-d), 7.79(2H, A-B q) 9.0(1H, Broad s) [CDCl.sub.3 + DMSO-d.sub.6 ]OMe CH.sub.2 OMe SO.sub.2 Me 3.04(3H,s), 3.24(3H,s), 3.71(3H,s), 4.71(2H,s), 7.71(2H,s), 8.88(1H,Broad s) [CDCl.sub.3 + DMSO-d.sub.6 ]______________________________________
These benzoic acids can readily be led to benzoyl chlorides by chlorinating agents such as phosphorus pentachloride, thionyl chloride and sulfuryl chloride.
By using such benzoic acids or benzoyl chlorides, compounds of the present invention can be readily prepared in accordance with reaction schemes (1) to (4).
The present invention will be described in further detail with reference to Examples. However, it should be understood that the present invention is by no means restricted to such specific Examples.

EXAMPLE 1
Preparation of 1-ethyl-5-hydroxy-4-(4-methanesulfonyl-3-methoxymethyl-2-methylbenzoyl)pyrazole
1.12 g (0.01 mol) of 1-ethyl-5-hydroxypyrazole is dissolved in 30 ml of t-amyl alcohol, and then 2.59 g (0.01 mol) of 4-methanesulfonyl-3-methoxymethyl-2-methylbenzoic acid, 2.06 g (0.01 mol) of N,N'-dicyclohexylcarbodiimide and 0.69 g (0.005 mol) of anhydrous potassium carbonate were sequentially added thereto. The mixture was reacted at a temperature of from 80.degree. to 90.degree. C. for 8 hours under stirring. After completion of the reaction, t-amyl alcohol was distilled off under reduced pressure, and 30 ml of water was added to the residue to dissolve the soluble components. The mixture was subjected to filtration to separate out the insolubles. The aqueous solution thus obtained was washed with chloroform, and concentrated hydrochloric acid was added to adjust pH<1. The precipitated oil component was extracted with chloroform. The solvent was distilled off under reduced pressure, and the residue was purified with silica gel column chromatography (eluent: ethyl acetate/ethanol=9/1) to obtain 2.3 g of the desired product. (Yield: 66%, melting point: 116.degree.-118.degree. C.)
EXAMPLE 2
Preparation of 1-ethyl-5-hydroxy-4-(4-methanesulfonyl-3-methoxycarbonyl-2-methylbenzoyl)pyrazole
1.12 g (0.01 mol) of 1-ethyl-5-hydroxypyrazole was dissolved in 30 ml of t-amyl alcohol, and 2.72 g (0.01 mol) of 4-methanesulfonyl-3-methoxycarbonyl-2-methylbenzoic acid, 2.27 g (0.011 mol) of N,N'-dicyclohexylcarbodiimide and 0.76 g (0.0055 mol) of anhydrous potassium carbonate were sequentially added thereto. The mixture was reacted at 80.degree. C. for 6 hours under stirring. After completion of the reaction, t-amyl alcohol was distilled off under reduced pressure, and then water was added to the residue to dissolve the soluble component. The mixture was subjected to filtration to separate out the insolubles. The aqueous solution thus obtained was washed twice with chloroform, and then concentrated hydrochloric acid was added to adjust pH<1. The precipitated oil component was extracted with chloroform. The chloroform layer was washed sequentially with water and a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure, and the residue thus obtained was recrystallized from water/ethanol to obtain 2.26 g of the desired product. (Yield: 62%, melting point: 150.degree.-152.degree. C.)
EXAMPLE 3
Preparation of 5-hydroxy-(3-isopropoxycarbonyl-4-methanesulfonyl-2-methylbenzoyl)-1-methylpyrazole
The operation and treatment were conducted in the same manner as in Example 1 except that 1.12 g of 1-ethyl-5-hydroxypyrazole was changed to 0.98 g of 5-hydroxy-1-methylpyrazole, and 2.72 g of 4-methanesulfonyl-3-methoxycarbonyl-2-methylbenzoic acid was changed to 3.00 g of 3-isopropoxycarbonyl-4-methanesulfonyl-2-methylbenzoic acid, to obtain 1.71 g of the desired product. (Yield: 45%, melting point: 192.degree.-194.degree. C.)
EXAMPLE 4
Preparation of 4-(2-chloro-3-ethylthiomethyl-4-methanesulfonylbenzoyl)-1-ethyl-5-hydroxypyrazole
3 g of 2-chloro-3-ethylthiomethyl-4-methanesulfonylbenzoic acid, 0.72 g of potassium carbonate, 50 ml of t-amyl alcohol, 1.95 g of N,N'-dicyclohexylcarbodiimide and 4.5 g of a 25% t-amyl alcohol solution of 1-ethyl-5-pyrazolone were mixed and heated under stirring for 4 hours at a temperature of from 70.degree. to 80.degree. C. After cooling, the mixture was distilled under reduced pressure, and 200 ml of water was added to the residue. After filtering off the insolubles, the filtrate was washed with chloroform. Hydrochloric acid was added to the aqueous layer, and the mixture was extracted with chloroform. The extract was dried, and the solvent was distilled off to obtain the desired product as a crude product. The crude product was recrystallized from ethanol to obtain 1.88 g of the purified product. (Melting pont: 142.degree.-145.degree. C.)
EXAMPLE 5
Preparation of 4-(2-chloro-5-ethanesulfonylmethyl-4-methanesulfonylbenzoyl)-1-ethyl-5-hydroxypyrazole
0.5 g of the compound obtained in Example 4 was dissolved in a solution comprising 30 ml of CHCl.sub.3 and 30 ml of THF at room temperature, and 2.2 equivalent of m-chloroperbenzoic acid was added thereto under cooling in ice bath. The mixture was gradually returned to room temperature and stirred for 1 day. The solvent was distilled off, and crystals thus obtained were collected by filtration and washed with ethyl ether to obtain 2.2 g of the desired product. (Melting poing: 133.degree.-135.degree. C.)
EXAMPLE 6
Preparation of 4-(2-chloro-3-ethanesulfinyl-4-methanesulfonylbenzoyl)-1-ethyl-5-hydroxypyrazole
0.45 g of the compound obtained in Example 4 was dissolved in 30 ml of dioxane, and 0.21 g of sodium bromite trihydrate was added thereto. The mixture was stirred at room temperature for 30 minutes, and then water was added thereto. The mixture was extracted with chloroform. The extract was dried, and the solvent was distilled off to obtain a crude product. The crude product was purified by column chromatography (eluted with chloroform/ethanol) to obtain 0.2 g of the desired product as an oily substance.
The physical properties of the compounds prepared in the same manner as the preceding Examples will be given in Tables 3 and 4 including those of the preceding Examples.
TABLE 3__________________________________________________________________________ ##STR30##CompoundNo. A B X Y Z Q Melting point (.degree.C.)__________________________________________________________________________1 Me H Me CH.sub.2 OMe SO.sub.2 Me H Oily substance2 Me H Me CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Oily substance3 Et H Me CH.sub.2 OMe SO.sub.2 Me H 116.about.1184 i-Pr H Me CH.sub.2 OMe SO.sub.2 Me H Oily substance5 Me H Me CO.sub.2 H SO.sub.2 Me H 274.about.274.56 Me H Me CO.sub.2 Me SO.sub.2 Me H 199.about.2017 Et H Me CO.sub.2 Me SO.sub.2 Me H 150.about.1528 Me H Me CO.sub.2 Et SO.sub.2 Me H 174.about.174.59 Et H Me CO.sub.2 Et SO.sub.2 Me H 78.about.8110 Me H Me CO.sub.2 Pri SO.sub.2 Me H 192.about.19411 Et H Me CO.sub.2 Pri SO.sub.2 Me H 125.about.12812 Me H Cl CO.sub.2 Me Cl H 123.about.12613 Me H Cl CO.sub.2 Me Cl p-TS Oily substance14 Me H Me CH.sub.2 OEt SO.sub.2 Me H 178.about.17915 Et H Me CH.sub.2 OEt SO.sub.2 Me H Oily substance16 i-Pr H Me CH.sub.2 OEt SO.sub.2 Me H Oily substance17 Me Me Me CH.sub.2 OEt SO.sub.2 Me H Oily substance18 Me H Me CHMeOMe SO.sub.2 Me H 238.about.24019 Et H Me CHMeOMe SO.sub.2 Me H 138.about.14120 Me H Cl CH.sub.2 OMe SO.sub.2 Me H 189.about.19021 Et H Cl CH.sub.2 OMe SO.sub.2 Me H 151.about.15422 i-Pr H Cl CH.sub.2 OMe SO.sub.2 Me H 142.about.14423 Et H Me CH.sub.2 OPri SO.sub.2 Me H 125.about.12724 Me H Me CO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H 114.about.11725 Et H Me CO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H 122.about.12426 Me H Cl CO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H 157.about.16127 Et H Cl CH.sub.2 SEt SO.sub.2 Me H 142.about.14528 Et H Cl CH.sub.2 SOEt SO.sub.2 Me H Oily substance29 Et H Cl CH.sub.2 SO.sub.2 Et SO.sub.2 Me H 133.about.13530 Et H Me CO.sub.2 Prn SO.sub.2 Me H Oily substance31 Me H Cl ##STR31## SO.sub.2 Me H Oily substance32 Me H Me ##STR32## SO.sub.2 Me H 220.about.22233 Et H Me ##STR33## SO.sub.2 Me H 179.about.18334 Me H Cl CO.sub.2 Me SO.sub.2 Me H 183.about.18535 Et H Cl CO.sub.2 Me SO.sub.2 Me H 174.about.17636 Pri H Cl CO.sub.2 Me SO.sub.2 Me H 138.about.14037 Et H Cl CH.sub.2 OCH.sub.2 C CH SO.sub.2 Me H 161.about.16438 Me H Cl CH.sub.2 OAmn SO.sub.2 Me H Oily substance39 Et H Me CH.sub.2 OMe SO.sub.2 Me K 180.about.19040 Et H Me CH.sub.2 OMe SO.sub.2 Me Na 210.about.21641 Et H Me CH.sub.2 OMe SO.sub.2 Me NH.sub.3.sup.+ Pri 95.about.10242 Me H OMe CO.sub.2 Me SO.sub.2 Me H 195.about.19843 Me H Cl CO.sub.2 Pri SO.sub.2 Me H 117.about.11944 Et H Cl CO.sub.2 Pri SO.sub.2 Me H 141.about.14345 Me H Cl CH.sub.2 OCH.sub.2 CF.sub.3 SO.sub.2 Me H 167.about.17046 Et H Me CH.sub.2 OMe SO.sub.2 Me 1/2 Ca 232.about.24247 Pri H Me CO.sub.2 Me SO.sub.2 Me H 116.about.12148 Me H OMe CH.sub.2 OMe SO.sub.2 Me H 154.about.15749 Et H Me CO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H 149.about.15250 Et H OMe CO.sub.2 Me SO.sub.2 Me H 172.about.175__________________________________________________________________________
The compounds represented by the Compound Nos. in the following Table are the same as represented by the corresponding Compound Nos. in Table 3.
TABLE 4______________________________________CompoundNo. .sup.1 H--NMR (.delta., ppm) [Solvent]______________________________________1 2.47(3H,s), 3.22(3H,s), 3.50 (3H,s), 3.69(3H,s), 4.96(2H,s), 7.30(1H,s), 7.78(2H,A-Bq), 10.9(1H) [CDCl.sub.3 ]2 2.41(3H,s), 3.17(3H,s), 3.50 (3H,s), 4.94(2H,s), 5.53(2H,s), 7.30.about.8.12 (8H,m) [CDCl.sub.3 ]3 1.44(3H,t), 2.48(3H,s), 3.23 (3H,s), 3.51(3H,s), 4.07(2H,q), 4.98(2H,s), 7.36(1H,s), 7.82(2H,A-Bq) [CDCl.sub.3 ]4 1.48(6H,d), 2.47(3H,s), 3.19 (3H,s), 3.48(3H,s), 4.53(1H,m), 4.92(2H,s), 7.18(1H,s), 7.69(2H,A-Bq), 9.57(1H) [CDCl.sub.3 ]13 2.43(3H,s), 3.78(3H,s), 3.94 (3H,s), 7.24.about.7.81(7H,m) [CDCl.sub.3 ]15 1.07(3H,t), 2.27(3H,s), 3.01 (3H,s), 3.30.about.3.65(5H,m), 4.77(2H,s), 6.99(1H,s), 7.48(2H, A-B q), 8.22(1H,s) [CDCl.sub.3 ]28 1.45(3H,t), 3.04(2H,q), 4.05 (2H,q), 4.91(2H,q), 7.29(1H,s), 7.70 (1H,s), 7.85(2H,q) [CDCl.sub.3 ]30 0.91.about.2.03(8H,m), 2.41(3H,s), 3.20(3H,s), 3.91.about.4.47(4H,m), 7.36.about.8.08(4H,m), [CDCl .sub.3 ]16 1.26(3H,t), 1.49(3H,d), 2.49 (3H,s), 3.24(3H,s), 3.69(2H,q), 4.59 (1H,m), 5.00(2H,s), 7.28.about.8.14(4H,m), [CDCl.sub.3 ]17 1.27(3H,t), 1.67(3H,s), 2.42 (3H,s), 3.23(3H,s), 3.63(3H,s), 3.68 (2H,q), - 5.02(2H,s), 7.7 (1H,s), 7.75 (2H,A-B q) [CDCl.sub.3 ]______________________________________
Compounds which can be prepared in the same manner as the preceding Examples will be given in Table 5 including those of the preceding Examples. However, the present invention is not restricted to such compounds.
Various symbols used in Table 5 has the following meanings. ##STR34##
TABLE 5__________________________________________________________________________A B X Y Z Q__________________________________________________________________________Me H Cl COOMe MeS HMe H Cl COOMe MeSO HMe H Cl COOMe Ms HMe H Cl COOMe Ms Q1Me H Cl COOMe Ms Q2Me H Cl COOMe Ms Q3Me H Cl COOMe Ms Q4Me H Cl COOMe Ms Q5Me H Cl COOMe Ms Q6Me H Cl COOMe Ms Q20Me Me Cl COOMe Ms HMe Cl Cl COOMe Ms HMe CF.sub.3 Cl COOMe Ms HMe OMe Cl COOMe Ms HMe SMe Cl COOMe Ms HMe H Cl COOEt MeS HMe H Cl COOEt MeSO HMe H Cl COOEt Ms HMe H Cl COOEt Ms Q1Me H Cl COOEt Ms Q18Me H Cl COOEt Ms Q13Me H Cl COOEt Ms Q4Me H Cl COOEt Ms Q5Me H Cl COOEt Ms Q6Me H Cl COOEt Ms Q22Me Me Cl COOEt Ms HMe Cl Cl COOEt Ms HMe CF.sub.3 Cl COOEt Ms HMe OMe Cl COOEt Ms HMe SMe Cl COOEt Ms HMe H Cl COOCH(CH.sub.3).sub.2 MeS HMe H Cl COOCH(CH.sub.3).sub.2 MeSO HMe H Cl COOCH(CH.sub.3).sub.2 Ms HMe H Cl COOCH(CH.sub.3).sub.2 Ms Q7Me H Cl COOCH(CH.sub.3).sub.2 Ms Q12Me H Cl COOCH(CH.sub.3).sub.2 Ms Q9Me H Cl COOCH(CH.sub.3).sub.2 Ms Q4Me H Cl COOCH(CH.sub.3).sub.2 Ms Q5Me H Cl COOCH(CH.sub.3).sub.2 Ms Q6Me H Cl COOCH(CH.sub.3).sub.2 Ms Q17Me Me Cl COOCH(CH.sub.3).sub.2 Ms HMe Cl Cl COOCH(CH.sub.3).sub.2 Ms HMe CF.sub.3 Cl COOCH(CH.sub.3).sub.2 Ms HMe OMe Cl COOCH(CH.sub.3).sub.2 Ms HMe SMe Cl COOCH(CH.sub.3).sub.2 Ms HMe H Cl COOMe Cl HMe H Cl COOMe Cl Q1Me H Cl COOMe Cl Q2Me H Cl COOMe Cl Q3Me H Cl COOEt Cl HMe H Cl COOEt Cl Q1Me H Cl COOEt Cl Q2Me H Cl COOEt Cl Q3Me H Cl COOCH(CH.sub.3).sub.2 Cl HMe H Cl COOCH(CH.sub.3).sub.2 Cl Q1Me H Cl COOCH(CH.sub.3).sub.2 Cl Q2Me H Cl COOCH(CH.sub.3).sub.2 Cl Q3Me H Cl CON(CH.sub.3).sub.2 MeS HMe H Cl CON(CH.sub.3).sub.2 MeSO HMe H Cl CON(CH.sub.3).sub.2 Ms HMe H Cl CON(CH.sub.3).sub.2 Ms Q1Me H Cl CON(CH.sub.3).sub.2 Ms Q18Me H Cl CON(CH.sub.3).sub.2 Ms Q13Me H Cl CON(CH.sub.3).sub.2 Ms Q4Me H Cl CON(CH.sub.3).sub.2 Ms Q5Me H Cl CON(CH.sub.3).sub.2 Ms Q6Me H Cl CON(CH.sub.3).sub.2 Ms Q22Me Me Cl CON(CH.sub.3).sub.2 Ms HMe Cl Cl CON(CH.sub.3).sub.2 Ms HMe CF.sub.3 Cl CON(CH.sub.3).sub.2 Ms HMe OMe Cl CON(CH.sub. 3).sub.2 Ms HMe SMe Cl CON(CH.sub.3).sub.2 Ms HMe H Cl CON(CH.sub.3).sub.2 Cl HMe H Cl CON(CH.sub.3).sub.2 Cl Q1Me H Cl CON(CH.sub.3).sub.2 Cl Q2Me H Cl CON(CH.sub.3).sub.2 Cl Q3Me H Cl COOC.sub.4 H.sub.9 Ms HMe H Cl COOC.sub.4 H.sub.9 Cl HMe H Cl COOCH.sub.2 CH(CH.sub.3).sub.2 Ms HMe H Cl COOCH.sub.2 CH(CH.sub.3).sub.2 Cl HMe H Cl COOCH(CH.sub.3)C.sub.2 H.sub.5 Ms HMe H Cl COOCH(CH.sub.3)C.sub.2 H.sub.5 Cl HMe H Cl COOC(CH.sub.3).sub.3 Ms HMe H Cl COOC(CH.sub.3).sub.3 Cl HMe H Cl CONHMe Ms HMe H Cl CONHMe Cl HMe H Cl CONHEt Ms HMe H Cl CONHEt Cl HMe H Cl CONHCH(CH.sub.3).sub.2 Ms HMe H Cl CONHCH(CH.sub.3).sub.2 Cl HMe H Cl CONHC(CH.sub.3).sub.3 Ms HMe H Cl CONHC(CH.sub.3).sub.3 Cl HMe H Cl CONHC.sub.4 H.sub.9 Ms HMe H Cl CONHC.sub.4 H.sub.9 Cl HMe H Cl CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms HMe H Cl CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl HMe H Cl CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms HMe H Cl CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl HMe H Cl CONEt.sub.2 Ms HMe H Cl CONEt.sub.2 Cl HMe H Cl CON [CH(CH.sub.3).sub.2 ].sub.2 Ms HMe H Cl CON [CH(CH.sub.3).sub.2 ].sub.2 Cl HMe H Cl Y1 Ms HMe H Cl Y1 Cl HMe H Cl Y2 Ms HMe H Cl Y2 Cl HMe H Cl Y3 Ms HMe H Cl Y3 Cl HMe H Cl COOPh Ms HMe H Cl COOPh Cl HMe H Cl COOCH.sub.2 Ph Ms HMe H Cl COOCH.sub.2 Ph Cl HMe H Cl COOCH.sub.2 CHCH.sub.2 Ms HMe H Cl COOCH.sub.2 CHCH.sub.2 Cl HMe H Cl COOCH.sub.2 CCH.sub.2 Ms HMe H Cl COOCH.sub.2 CCH.sub.2 Cl HMe H Cl C(O)SMe Ms HMe H Cl C(O)SMe Cl HMe H Cl C(O)SEt Ms HMe H Cl C(O)SEt Cl HMe H Cl C(O)SCH(CH.sub.3).sub.2 Ms HMe H Cl C(O)SCH(CH.sub.3).sub.2 Cl HMe H Cl C(O)SC.sub.3 H.sub.7 Ms HMe H Cl C(O)SC.sub.3 H.sub.7 Cl HMe H Cl C(S)OMe Ms HMe H Cl C(S)OMe Cl HMe H Cl C(S)OEt Ms HMe H Cl C(S)OEt Cl HMe H Cl C(S)OCH(CH.sub.3).sub.2 Ms HMe H Cl C(S)OCH(CH.sub.3).sub.2 Cl HMe H Cl C(S)SC.sub.3 H.sub.7 Ms HMe H Cl C(S)SC.sub.3 H.sub.7 Cl HMe H Cl C(S)SMe Ms HMe H Cl C(S)SMe Cl HMe H Cl C(S)SEt Ms HMe H Cl C(S)SEt Cl HMe H Cl C(S)SCH(CH.sub.3).sub.2 Ms HMe H Cl C(S)SCH(CH.sub.3).sub.2 Cl HMe H Cl C(S)SC.sub.3 H.sub.7 Ms HMe H Cl C(S)SC.sub.3 H.sub.7 Cl HMe H Me COOMe MeS HMe H Me COOMe MeSO HMe H Me COOMe Ms HMe H Me COOMe Ms Q1Me H Me COOMe Ms Q2Me H Me COOMe Ms Q3Me H Me COOMe Ms Q4Me H Me COOMe Ms Q5Me H Me COOMe Ms Q6Me H Me COOMe Ms Q20Me Me Me COOMe Ms HMe Cl Me COOMe Ms HMe CF.sub.3 Me COOMe Ms HMe OMe Me COOMe Ms HMe SMe Me COOMe Ms HMe H Me COOEt MeS HMe H Me COOEt MeSO HMe H Me COOEt Ms Q1Me H Me COOEt Ms Q18Me H Me COOEt Ms Q13Me H Me COOEt Ms Q4Me H Me COOEt Ms Q5Me H Me COOEt Ms Q6Me H Me COOEt Ms Q22Me Me Me COOEt Ms HMe Cl Me COOEt Ms HMe CF.sub.3 Me COOEt Ms HMe OMe Me COOEt Ms HMe SMe Me COOEt Ms HMe H Me COOCH(CH.sub.3).sub.2 MeS HMe H Me COOCH(CH.sub.3).sub.2 MeSO HMe H Me COOCH(CH.sub.3).sub.2 Ms HMe H Me COOCH(CH.sub.3).sub.2 Ms Q7Me H Me COOCH(CH.sub.3).sub.2 Ms Q12Me H Me COOCH(CH.sub.3).sub.2 Ms Q9Me H Me COOCH(CH.sub.3).sub.2 Ms Q4Me H Me COOCH(CH.sub.3).sub.2 Ms Q5Me H Me COOCH(CH.sub.3).sub.2 Ms Q6Me H Me COOCH(CH.sub.3).sub.2 Ms Q17Me Me Me COOCH(CH.sub.3).sub.2 Ms HMe Cl Me COOCH(CH.sub.3).sub.2 Ms HMe CF.sub.3 Me COOCH(CH.sub.3).sub.2 Ms HMe OMe Me COOCH(CH.sub.3).sub.2 Ms HMe SMe Me COOCH(CH.sub.3).sub.2 Ms HMe H Me COOMe Cl HMe H Me COOMe Cl Q1Me H Me COOMe Cl Q2Me H Me COOMe Cl Q3Me H Me COOEt Cl HMe H Me COOEt Cl Q1Me H Me COOEt Cl Q2Me H Me COOEt Cl Q3Me H Me COOCH(CH.sub.3).sub.2 Cl HMe H Me COOCH(CH.sub.3).sub.2 Cl Q1Me H Me COOCH(CH.sub.3).sub.2 Cl Q2Me H Me COOCH(CH.sub.3).sub.2 Cl Q3Me H Me CON(CH.sub.3).sub.2 MeS HMe H Me CON(CH.sub.3).sub.2 MeSO HMe H Me CON(CH.sub.3).sub.2 Ms HMe H Me CON(CH.sub.3).sub.2 Ms Q1Me H Me CON(CH.sub.3).sub.2 Ms Q18Me H Me CON(CH.sub.3).sub.2 Ms Q13Me H Me CON(CH.sub.3).sub.2 Ms Q4Me H Me CON(CH.sub.3).sub.2 Ms Q5Me H Me CON(CH.sub.3).sub.2 Ms Q6Me H Me CON(CH.sub.3).sub.2 Ms Q22Me Me Me CON(CH.sub.3).sub.2 Ms HMe Cl Me CON(CH.sub.3).sub.2 Ms HMe CF.sub.3 Me CON(CH.sub.3).sub.2 Ms HMe OMe Me CON(CH.sub.3).sub.2 Ms HMe SMe Me CON(CH.sub.3).sub.2 Ms HMe H Me CON(CH.sub.3).sub.2 Cl HMe H Me CON(CH.sub.3).sub.2 Cl Q1Me H Me CON(CH.sub.3).sub.2 Cl Q2Me H Me CON(CH.sub.3).sub.2 Cl Q3Me H Me COOC.sub.4 H.sub.9 Ms HMe H Me COOC.sub.4 H.sub.9 Cl HMe H Me COOCH.sub.2 CH(CH.sub.3).sub.2 Ms HMe H Me COOCH.sub.2 CH(CH.sub.3 ).sub.2 Cl HMe H Me COOCH(CH.sub.3)C.sub.2 H.sub.5 Ms HMe H Me COOCH(CH.sub.3)C.sub.2 H.sub.5 Cl HMe H Me COO(CH.sub.3).sub.3 Ms HMe H Me COO(CH.sub.3).sub.3 Cl HMe H Me CONHMe Ms HMe H Me CONHMe Cl HMe H Me CONHEt Ms HMe H Me CONHEt Cl HMe H Me CONHCH(CH.sub.3).sub.2 Ms HMe H Me CONHCH(CH.sub.3).sub.2 Cl HMe H Me CONHC(CH.sub.3).sub.3 Ms HMe H Me CONHC(CH.sub.3).sub.3 Cl HMe H Me CONHC.sub.4 H.sub.9 Ms HMe H Me CONHC.sub.4 H.sub.9 Cl HMe H Me CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms HMe H Me CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl HMe H Me CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms HMe H Me CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl HMe H Me CONEt.sub.2 Ms HMe H Me CONEt.sub.2 Cl HMe H Me CON [CH(CH.sub.3).sub.2 ].sub.2 Ms HMe H Me CON [CH(CH.sub. 3).sub.2 ].sub.2 Cl HMe H Me Y1 Ms HMe H Me Y1 Cl HMe H Me Y2 Ms HMe H Me Y2 Cl HMe H Me Y3 Ms HMe H Me Y3 Cl HMe H Me COOPh Ms HMe H Me COOPh Cl HMe H Me COOCH.sub.2 Ph Ms HMe H Me COOCH.sub.2 Ph Cl HMe H Me COOCH.sub.2 CHCH.sub.2 Ms HMe H Me COOCH.sub.2 CHCH.sub.2 Cl HMe H Me COOCH.sub.2 CCH Ms HMe H Me COOCH.sub.2 CCH Cl HMe H Me C(O)SMe Ms HMe H Me C(O)SMe Cl HMe H Me C(O)SEt Ms HMe H Me C(O)SEt Cl HMe H Me C(O)SCH(CH.sub.3).sub.2 Ms HMe H Me C(O)SCH(CH.sub.3).sub.2 Cl HMe H Me C(O)SC.sub.3 H.sub.7 Ms HMe H Me C(O)SC.sub.3 H.sub.7 Cl HMe H Me C(S)OMe Ms HMe H Me C(S)OMe Cl HMe H Me C(S)OEt Ms HMe H Me C(S)OEt Cl HMe H Me C(S)OCH(CH.sub.3).sub.2 Ms HMe H Me C(S)OCH(CH.sub.3).sub.2 Cl HMe H Me C(S)SC.sub.3 H.sub.7 Ms HMe H Me C(S)SC.sub.3 H.sub.7 Cl HMe H Me C(S)SMe Ms HMe H Me C(S)SMe Cl HMe H Me C(S)SEt Ms HMe H Me C(S)SEt Cl HMe H Me C(S)SCH(CH.sub.3).sub.2 Ms HMe H Me C(S)SCH(CH.sub.3).sub.2 Cl HMe H Me C(S)SC.sub.3 H.sub.7 Ms HMe H Me C(S)SC.sub.3 H.sub.7 Cl HMe H OMe COOMe MeS HMe H OMe COOMe MeSO HMe H OMe COOMe Ms HMe H OMe COOMe Ms Q1Me H OMe COOMe Ms Q2Me H OMe COOMe Ms Q3Me H OMe COOMe Ms Q4Me H OMe COOMe Ms Q5Me H OMe COOMe Ms Q6Me H OMe COOMe Ms Q20Me Me OMe COOMe Ms HMe Cl OMe COOMe Ms HMe CF.sub.3 OMe COOMe Ms HMe OMe OMe COOMe Ms HMe SMe OMe COOMe Ms HMe H OMe COOEt MeS HMe H OMe COOEt MeSO HMe H OMe COOEt Ms HMe H OMe COOEt Ms Q1Me H OMe COOEt Ms Q18Me H OMe COOEt Ms Q13Me H OMe COOEt Ms Q4Me H OMe COOEt Ms Q5Me H OMe COOEt Ms Q6Me H OMe COOEt Ms Q22Me Me OMe COOEt Ms HMe Cl OMe COOEt Ms HMe CF.sub.3 OMe COOEt Ms HMe OMe OMe COOEt Ms HMe SMe OMe COOEt Ms HMe H OMe COOCH(CH.sub.3).sub.2 MeS HMe H OMe COOCH(CH.sub.3).sub.2 MeSO HMe H OMe COOCH(CH.sub.3).sub.2 Ms HMe H OMe COOCH(CH.sub.3).sub.2 Ms Q7Me H OMe COOCH(CH.sub.3).sub.2 Ms Q12Me H OMe COOCH(CH.sub.3).sub.2 Ms Q9Me H OMe COOCH(CH.sub.3).sub.2 Ms Q4Me H OMe COOCH(CH.sub.3).sub.2 Ms Q5Me H OMe COOCH(CH.sub.3).sub.2 Ms Q6Me H OMe COOCH(CH.sub.3).sub.2 Ms Q17Me Me OMe COOCH(CH.sub.3).sub.2 Ms HMe Cl OMe COOCH(CH.sub.3).sub.2 Ms HMe CF.sub. 3 OMe COOCH(CH.sub.3).sub.2 Ms HMe OMe OMe COOCH(CH.sub.3).sub.2 Ms HMe SMe OMe COOCH(CH.sub.3).sub.2 Ms HMe H OMe COOMe Cl HMe H OMe COOMe Cl Q1Me H OMe COOMe Cl Q2Me H OMe COOMe Cl Q3Me H OMe COOEt Cl HMe H OMe COOEt Cl Q1Me H OMe COOEt Cl Q2Me H OMe COOEt Cl Q3Me H OMe COOCH(CH.sub.3).sub.2 Cl HMe H OMe COOCH(CH.sub.3).sub.2 Cl Q1Me H OMe COOCH(CH.sub.3).sub.2 Cl Q2Me H OMe COOCH(CH.sub.3).sub.2 Cl Q3Me H OMe CON(CH.sub.3).sub.2 MeS HMe H OMe CON(CH.sub.3).sub.2 MeSO HMe H OMe CON(CH.sub.3).sub.2 Ms HMe H OMe CON(CH.sub.3).sub.2 Ms Q1Me H OMe CON(CH.sub.3).sub.2 Ms Q18Me H OMe CON(CH.sub.3).sub.2 Ms Q13Me H OMe CON(CH.sub.3).sub.2 Ms Q4Me H OMe CON(CH.sub.3).sub.2 Ms Q5Me H OMe CON(CH.sub.3).sub.2 Ms Q6Me H OMe CON(CH.sub.3).sub.2 Ms Q22Me Me OMe CON(CH.sub.3).sub.2 Ms HMe Cl OMe CON(CH.sub.3).sub.2 Ms HMe CF.sub.3 OMe CON(CH.sub.3).sub.2 Ms HMe OMe OMe CON(CH.sub.3).sub.2 Ms HMe SMe OMe CON(CH.sub.3).sub.2 Ms HMe H OMe CON(CH.sub.3).sub.2 Cl HMe H OMe CON(CH.sub.3).sub.2 Cl Q1Me H OMe CON(CH.sub.3).sub.2 Cl Q2Me H OMe CON(CH.sub.3).sub.2 Cl Q3Me H OMe COOC.sub.4 H.sub.9 Ms HMe H OMe COOC.sub.4 H.sub.9 Cl HMe H OMe COOCH.sub.2 CH(CH.sub.3).sub.2 Ms HMe H OMe COOCH.sub.2 CH(CH.sub.3).sub.2 Cl HMe H OMe COOCH(CH.sub.3)C.sub.2 H.sub.5 Ms HMe H OMe COOCH(CH.sub.3)C.sub.2 H.sub.5 Cl HMe H OMe COOC(CH.sub.3).sub.3 Ms HMe H OMe COOC(CH.sub.3).sub.3 Cl HMe H OMe CONHMe Ms HMe H OMe CONHMe Cl HMe H OMe CONHEt Ms HMe H OMe CONHEt Cl HMe H OMe CONHCH(CH.sub.3).sub.2 Ms HMe H OMe CONHCH(CH.sub.3 ).sub.2 Cl HMe H OMe CONHC(CH.sub.3).sub.3 Ms HMe H OMe CONHC(CH.sub.3).sub.3 Cl HMe H OMe CONHC.sub.4 H.sub.9 Ms HMe H OMe CONHC.sub.4 H.sub.9 Cl HMe H OMe CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms HMe H OMe CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl HMe H OMe CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms HMe H OMe CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl HMe H OMe CONEt.sub.2 Ms HMe H OMe CONEt.sub.2 Cl HMe H OMe CON [CH(CH.sub.3).sub.2 ].sub.2 Ms HMe H OMe CON [CH(CH.sub.3).sub.2 ].sub.2 Cl HMe H OMe Y1 Ms HMe H OMe Y1 Cl HMe H OMe Y2 Ms HMe H OMe Y2 Cl HMe H OMe Y3 Ms HMe H OMe Y3 Cl HMe H OMe COOPh Ms HMe H OMe COOPh Cl HMe H OMe COOCH.sub.2 Ph Ms HMe H OMe COOCH.sub.2 Ph Cl HMe H OMe COOCH.sub.2 CHCH.sub.2 Ms HMe H OMe COOCH.sub.2 CHCH.sub.2 Cl HMe H OMe COOCH.sub.2 CCH Ms HMe H OMe COOCH.sub.2 CCH Cl HMe H OMe C(O)SMe Ms HMe H OMe C(O)SMe Cl HMe H OMe C(O)SEt Ms HMe H OMe C(O)SEt Cl HMe H OMe C(O)SCH(CH.sub.3).sub.2 Ms HMe H OMe C(O)SCH(CH.sub.3).sub.2 Cl HMe H OMe C(O)SC.sub.3 H.sub.7 Ms HMe H OMe C(O)SC.sub.3 H.sub.7 Cl HMe H OMe C(S)OMe Ms HMe H OMe C(S)OMe Cl HMe H OMe C(S)OEt Ms HMe H OMe C(S)OEt Cl HMe H OMe C(S)OCH(CH.sub.3).sub.2 Ms HMe H OMe C(S)OCH(CH.sub.3).sub.2 Cl HMe H OMe C(S)SC.sub.3 H.sub.7 Ms HMe H OMe C(S)SC.sub.3 H.sub.7 Cl HMe H OMe C(S)SMe Ms HMe H OMe C(S)SMe Cl HMe H OMe C(S)SEt Ms HMe H OMe C(S)SEt Cl HMe H OMe C(S)SCH(CH.sub.3).sub.2 Ms HMe H OMe C(S)SCH(CH.sub.3).sub.2 Cl HMe H OMe C(S)SC.sub.3 H.sub.7 Ms HMe H OMe C(S)SC.sub.3 H.sub.7 Cl HMe H Br COOMe Ms HMe H Br COOMe Cl HMe H Br COOEt Ms HMe H Br COOEt Cl HMe H Br COOCH(CH.sub.3).sub.2 Ms HMe H Br COOCH(CH.sub.3).sub.2 Cl HMe H Br CON(CH.sub.3).sub.2 Ms HMe H Br CON(CH.sub.3).sub.2 Cl HMe H Br CONHMe Ms HMe H Br CONHEt Ms HMe H Br CONHC.sub.3 H.sub.7 Ms HMe H Br CONHCH(CH.sub.3).sub.2 Ms HMe H Br CONHC(CH.sub.3).sub.3 Ms HMe H Br CONEt.sub.2 Ms HMe H Br CONHC(CH.sub.3).sub.3 Ms HMe H Br CONHC.sub.4 H.sub.9 Ms HMe H Br CONHC.sub.4 H.sub.9 Ms HMe H Br CON [CH(CH.sub.3).sub.2 ].sub.2 Ms HMe H Br Y1 Ms HMe H Br Y2 Ms HMe H Br COOPh Ms HMe H Br COOCH.sub.2 Ph Ms HMe H Br COOCH.sub.2 CHCH.sub.2 Ms HMe H Br COOCH.sub.2 CCH Ms HMe H OEt COOMe Ms HMe H OEt COOMe Cl HMe H OEt COOEt Ms HMe H OEt COOEt Cl HMe H OEt COOCH(CH.sub.3).sub.2 Ms HMe H OEt COOCH(CH.sub.3).sub.2 Cl HMe H OEt CON(CH.sub.3).sub.2 Ms HMe H OEt CON(CH.sub.3).sub.2 Cl HMe H OEt CONHMe Ms HMe H OEt CONHEt Ms HMe H OEt CONHC.sub.3 H.sub.7 Ms HMe H OEt CONHCH(CH.sub.3).sub.2 Ms HMe H OEt CONHC(CH.sub.3).sub.3 Ms HMe H OEt CONEt.sub.2 Ms HMe H OEt CONHC(CH.sub.3).sub.3 Ms HMe H OEt CONHC.sub.4 H.sub.9 Ms HMe H OEt CONHC.sub.4 H.sub.9 Ms HMe H OEt CON [CH(CH.sub.3).sub.2 ].sub.2 Ms HMe H OEt Y1 Ms HMe H OEt Y2 Ms HMe H OEt COOPh Ms HMe H OEt COOCH.sub.2 Ph Ms HMe H OEt COOCH.sub.2 CHCH.sub.2 Ms HMe H OEt COOCH.sub.2 CCH Ms HMe H OCH(CH.sub.3).sub.2 COOMe Ms HMe H OCH(CH.sub.3).sub.2 COOMe Cl HMe H OCH(CH.sub.3).sub.2 COOEt Ms HMe H OCH(CH.sub.3).sub.2 COOEt Cl HMe H OCH(CH.sub.3).sub.2 COOCH(CH.sub.3).sub.2 Ms HMe H OCH(CH.sub.3).sub.2 COOCH(CH.sub.3).sub.2 Cl HMe H OCH(CH.sub.3).sub.2 CON(CH.sub.3).sub.2 Ms HMe H OCH(CH.sub.3).sub.2 CON(CH.sub.3).sub.2 Cl HMe H OCH(CH.sub.3).sub.2 CONHMe Ms HMe H OCH(CH.sub.3).sub.2 CONHEt Ms HMe H OCH(CH.sub.3).sub.2 CONHC.sub.3 H.sub.7 Ms HMe H OCH(CH.sub.3).sub.2 CONHCH(CH.sub.3).sub.2 Ms HMe H OCH(CH.sub.3).sub.2 CONHC(CH.sub.3).sub.3 Ms HMe H OCH(CH.sub.3).sub.2 CONEt.sub.2 Ms HMe H OCH(CH.sub.3).sub.2 CONHC(CH.sub.3).sub.3 Ms HMe H OCH(CH.sub.3).sub.2 CONHC.sub.4 H.sub.9 Ms HMe H OCH(CH.sub.3).sub.2 CONHC.sub.4 H.sub.9 Ms HMe H OCH(CH.sub.3).sub.2 CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HMe H OCH(CH.sub.3).sub.2 Y1 Ms HMe H OCH(CH.sub.3).sub.2 Y2 Ms HMe H OCH(CH.sub.3).sub.2 COOPh Ms HMe H OCH(CH.sub.3).sub.2 COOCH.sub.2 Ph Ms HMe H OCH(CH.sub.3).sub.2 COOCH.sub.2 CHCH.sub.2 Ms HMe H OCH(CH.sub.3).sub.2 COOCH.sub.2 CCH Ms HMe H CH.sub.2 OCH.sub.3 COOMe Ms HMe H CH.sub.2 OCH.sub.3 COOMe Cl HMe H CH.sub.2 OCH.sub.3 COOEt Ms HMe H CH.sub.2 OCH.sub.3 COOEt Cl HMe H CH.sub.2 OCH.sub.3 COOCH(CH.sub.3).sub.2 Ms HMe H CH.sub.2 OCH.sub.3 COOCH(CH.sub.3).sub.2 Cl HMe H CH.sub.2 OCH.sub.3 CON(CH.sub.3).sub.2 Ms HMe H CH.sub.2 OCH.sub.3 CON(CH.sub.3).sub.2 Cl HMe H CH.sub.2 OCH.sub.3 CONHMe Ms HMe H CH.sub.2 OCH.sub.3 CONHEt Ms HMe H CH.sub.2 OCH.sub.3 CONHC.sub.3 H.sub.7 Ms HMe H CH.sub.2 OCH.sub.3 CONHCH(CH.sub.3).sub.2 Ms HMe H CH.sub.2 OCH.sub.3 CONHC(CH.sub.3).sub.3 Ms HMe H CH.sub.2 OCH.sub.3 CONEt.sub.2 Ms HMe H CH.sub.2 OCH.sub.3 CONHC(CH.sub.3).sub.3 Ms HMe H CH.sub.2 OCH.sub.3 CONHC.sub.4 H.sub.9 Ms HMe H CH.sub.2 OCH.sub.3 CONHC.sub.4 H.sub.9 Ms HMe H CH.sub.2 OCH.sub.3 CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HMe H CH.sub.2 OCH.sub.3 Y1 Ms HMe H CH.sub.2 OCH.sub.3 Y2 Ms HMe H CH.sub.2 OCH.sub.3 COOPh Ms HMe H CH.sub.2 OCH.sub.3 COOCH.sub.2 Ph Ms HMe H CH.sub.2 OCH.sub.3 COOCH.sub.2 CHCH.sub.2 Ms HMe H CH.sub.2 OCH.sub.3 COOCH.sub.2 CCH Ms HEt H Cl COOMe MeS HEt H Cl COOMe MeSO HEt H Cl COOMe Ms HEt H Cl COOMe Ms Q1Et H Cl COOMe Ms Q2Et H Cl COOMe Ms Q3Et H Cl COOMe Ms Q4Et H Cl COOMe Ms Q5Et H Cl COOMe Ms Q6Et H Cl COOMe Ms Q20Et Me Cl COOMe Ms HEt Cl Cl COOMe Ms HEt CF.sub.3 Cl COOMe Ms HEt OMe Cl COOMe Ms HEt SMe Cl COOMe Ms HEt H Cl COOEt MeS HEt H Cl COOEt MeSO HEt H Cl COOEt Ms HEt H Cl COOEt Ms Q1Et H Cl COOEt Ms Q18Et H Cl COOEt Ms Q13Et H Cl COOEt Ms Q4Et H Cl COOEt Ms Q5Et H Cl COOEt Ms Q6Et H Cl COOEt Ms Q22Et Me Cl COOEt Ms HEt Cl Cl COOEt Ms HEt CF.sub.3 Cl COOEt Ms HEt OMe Cl COOEt Ms HEt SMe Cl COOEt Ms HEt H Cl COOCH(CH.sub.3).sub.2 MeS HEt H Cl COOCH(CH.sub.3).sub.2 MeSO HEt H Cl COOCH(CH.sub.3).sub.2 Ms HEt H Cl COOCH(CH.sub.3).sub.2 Ms Q7Et H Cl COOCH(CH.sub.3).sub.2 Ms Q12Et H Cl COOCH(CH.sub.3).sub.2 Ms Q9Et H Cl COOCH(CH.sub.3).sub.2 Ms Q4Et H Cl COOCH(CH.sub.3).sub.2 Ms Q5Et H Cl COOCH(CH.sub.3).sub.2 Ms Q6Et H Cl COOCH(CH.sub.3).sub.2 Ms Q17Et Me Cl COOCH(CH.sub.3).sub.2 Ms HEt Cl Cl COOCH(CH.sub.3).sub.2 Ms HEt CF.sub.3 Cl COOCH(CH.sub.3).sub.2 Ms HEt OMe Cl COOCH(CH.sub.3).sub.2 Ms H__________________________________________________________________________
TABLE 5__________________________________________________________________________ ##STR35##A B X Y Z Q__________________________________________________________________________Et SMe Cl COOCH(CH.sub.3).sub.2 Ms HEt H Cl COOMe Cl HEt H Cl COOMe Cl Q1Et H Cl COOMe Cl Q2Et H Cl COOMe Cl Q3Et H Cl COOEt Cl HEt H Cl COOEt Cl Q1Et H Cl COOEt Cl Q2Et H Cl COOEt Cl Q3Et H Cl COOCH(CH.sub.3).sub.2 Cl HEt H Cl COOCH(CH.sub.3).sub.2 Cl Q1Et H Cl COOCH(CH.sub.3).sub.2 Cl Q2Et H Cl COOCH(CH.sub.3).sub.2 Cl Q3Et H Cl CON(CH.sub.3).sub.2 MeS HEt H Cl CON(CH.sub.3).sub.2 MeSO HEt H Cl CON(CH.sub.3).sub.2 Ms HEt H Cl CON(CH.sub. 2).sub.2 Ms Q1Et H Cl CON(CH.sub.3).sub.2 Ms Q18Et H Cl CON(CH.sub.3).sub.2 Ms Q13Et H Cl CON(CH.sub.3).sub.2 Ms Q4Et H Cl CON(CH.sub.3).sub.2 Ms Q5Et H Cl CON(CH.sub.3).sub.2 Ms Q6Et H Cl CON(CH.sub.3).sub.2 Ms Q22Et Me Cl CON(CH.sub.3).sub.2 Ms HEt Cl Cl CON(CH.sub.3).sub.2 Ms HEt CF.sub.3 Cl CON(CH.sub.3).sub.2 Ms HEt OMe Cl CON(CH.sub.3).sub.2 Ms HEt SMe Cl CON(CH.sub.3).sub.2 Ms HEt H Cl CON(CH.sub.3).sub.2 Cl HEt H Cl CON(CH.sub.3).sub.2 Cl Q1Et H Cl CON(CH.sub.3).sub.2 Cl Q2Et H Cl CON(CH.sub.3).sub.2 Cl Q3Et H Cl COOC.sub.4 H.sub.9 Ms HEt H Cl COOC.sub.4 H.sub.9 Cl HEt H Cl COOCH.sub.2 CH(CH.sub.3).sub.2 Ms HEt H Cl COOCH.sub.2 CH(CH.sub.3).sub.2 Cl HEt H Cl COOCH.sub.2 CH(CH.sub.3)C.sub.2 H.sub.5 Ms HEt H Cl COOCH(CH.sub.3)C.sub. 2 H.sub.5 Cl HEt H Cl COOC(CH.sub.3).sub.3 Ms HEt H Cl COOC(CH.sub.3).sub.3 Cl HEt H Cl CONHMe Ms HEt H Cl CONHMe Cl HEt H Cl CONHEt Ms HEt H Cl CONHEt Cl HEt H Cl CONHCH(CH.sub.3).sub.2 Ms HEt H Cl CONHCH(CH.sub.3).sub.2 Cl HEt H Cl CONHC(CH.sub.3).sub.3 Ms HEt H Cl CONHC(CH.sub.3).sub.3 Cl HEt H Cl CONHC.sub.4 H.sub.9 Ms HEt H Cl CONHC.sub.4 H.sub.9 Cl HEt H Cl CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms HEt H Cl CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl HEt H Cl CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms HEt H Cl CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl HEt H Cl CONEt.sub.2 Ms HEt H Cl CONEt.sub.2 Cl HEt H Cl CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HEt H Cl CON[CH(CH.sub.3).sub.2 ].sub.2 Cl HEt H Cl Y1 Ms HEt H Cl Y1 Cl HEt H Cl Y2 Ms HEt H Cl Y2 Cl HEt H Cl Y3 Ms HEt H Cl Y3 Cl HEt H Cl COOPh Ms HEt H Cl COOPh Cl HEt H Cl COOCH.sub.2 Ph Ms HEt H Cl COOCH.sub.2 Ph Cl HEt H Cl COOCH.sub.2 CHCH.sub.2 Ms HEt H Cl COOCH.sub.2 CHCH.sub.2 Cl HEt H Cl COOCH.sub.2 CCH Ms HEt H Cl COOCH.sub.2 CCH Cl HEt H Cl C(O)SMe Ms HEt H Cl C(O)SMe Cl HEt H Cl C(O)SEt Ms HEt H Cl C(O)SEt Cl HEt H Cl C(O)SCH(CH.sub.3).sub.2 Ms HEt H Cl C(O)SCH(CH.sub.3).sub.2 Cl HEt H Cl C(O)SC.sub.3 H.sub.7 Ms HEt H Cl C(O)SC.sub.3 H.sub.7 Cl HEt H Cl C(S)OMe Ms HEt H Cl C(S)OMe Cl HEt H Cl C(S)OEt Ms HEt H Cl C(S)OEt Cl HEt H Cl C(S)OCH(CH.sub.3).sub.2 Ms HEt H Cl C(S)OCH(CH.sub.3).sub.2 Cl HEt H Cl C(S)SC.sub.3 H.sub.7 Ms HEt H Cl C(S)SC.sub.3 H.sub.7 Cl HEt H Cl C(S)SMe Ms HEt H Cl C(S)SMe Cl HEt H Cl C(S)SEt Ms HEt H Cl C(S)SEt Cl HEt H Cl C(S)SCH(CH.sub.3).sub.2 Ms HEt H Cl C(S)SCH(CH.sub.3).sub.2 Cl HEt H Cl C(S)SC.sub.3 H.sub.7 Ms HEt H Cl C(S)SC.sub.3 H.sub.7 Cl HEt H Me COOMe MeS HEt H Me COOMe MeSO HEt H Me COOMe Ms HEt H Me COOMe Ms HEt H Me COOMe Ms Q2Et H Me COOMe Ms Q3Et H Me COOMe Ms Q4Et H Me COOMe Ms Q5Et H Me COOMe Ms Q6Et H Me COOMe Ms Q20Et Me Me COOMe Ms HEt Cl Me COOMe Ms HEt CF.sub.3 Me COOMe Ms HEt OMe Me COOMe Ms HEt SMe Me COOMe Ms HEt H Me COOEt MeS HEt H Me COOEt MeSO HEt H Me COOEt Ms HEt H Me COOEt Ms Q1Et H Me COOEt Ms Q18Et H Me COOEt Ms Q13Et H Me COOEt Ms Q4Et H Me COOEt Ms Q5Et H Me COOEt Ms Q6Et H Me COOEt Ms Q22Et Me Me COOEt Ms HEt Cl Me COOEt Ms HEt CF.sub.3 Me COOEt Ms HEt OMe Me COOEt Ms HEt SMe Me COOEt Ms HEt H Me COOCH(CH.sub.3).sub.2 MeS HEt H Me COOCH(CH.sub.3).sub.2 MeSO HEt H Me COOCH(CH.sub.3).sub.2 Ms HEt H Me COOCH(CH.sub.3).sub.2 Ms Q7Et H Me COOCH(CH.sub.3).sub.2 Ms Q12Et H Me COOCH(CH.sub.3).sub.2 Ms Q9Et H Me COOCH(CH.sub.3).sub.2 Ms Q4Et H Me COOCH(CH.sub.3).sub.2 Ms Q5Et H Me COOCH(CH.sub.3).sub.2 Ms Q6Et H Me COOCH(CH.sub.3).sub.2 Ms Q17Et Me Me COOCH(CH.sub.3).sub.2 Ms HEt Cl Me COOCH(CH.sub.3).sub.2 Ms HEt CF.sub.3 Me COOCH(CH.sub.3).sub.2 Ms HEt OMe Me COOCH(CH.sub.3).sub.2 Ms HEt SMe Me COOCH(CH.sub.3).sub. 2 Ms HEt H Me COOMe Cl HEt H Me COOMe Cl Q1Et H Me COOMe Cl Q2Et H Me COOMe Cl Q3Et H Me COOEt Cl HEt H Me COOEt Cl Q1Et H Me COOEt Cl Q2Et H Me COOEt Cl Q3Et H Me COOCH(CH.sub.3).sub.2 Cl HEt H Me COOCH(CH(CH.sub.3).sub.2 Cl Q1Et H Me COOCH(CH.sub.3).sub.2 Cl Q2Et H Me COOCH(CH.sub.3).sub.2 Cl Q3Et H Me CON(CH.sub.3).sub.2 MeS HEt H Me CON(CH.sub.3).sub.2 MeSO HEt H Me CON(CH.sub.3).sub.2 Ms HEt H Me CON(CH.sub.3).sub.2 Ms Q1Et H Me CON(CH.sub.3).sub.2 Ms Q18Et H Me CON(CH.sub.3).sub.2 Ms Q13Et H Me CON(CH.sub.3).sub.2 Ms Q4Et H Me CON(CH.sub.3).sub.2 Ms Q5Et H Me CON(CH.sub.3).sub.2 Ms Q6Et H Me CON(CH.sub.3).sub.2 Ms Q22Et Me Me CON(CH.sub.3).sub.2 Ms HEt Cl Me CON(CH.sub.3).sub.2 Ms HEt CF.sub.3 Me CON(CH.sub. 3).sub.2 Ms HEt OMe Me CON(CH.sub.3).sub.2 Ms HEt SMe Me CON(CH.sub.3).sub.2 Ms HEt H Me CON(CH.sub.3).sub.2 Cl HEt H Me CON(CH.sub.3).sub.2 Cl Q1Et H Me CON(CH.sub.3).sub.2 Cl Q2Et H Me CON(CH.sub.3).sub.2 Cl Q3Et H Me COOC.sub.4 H.sub.9 Ms HEt H Me COOC.sub.4 H.sub.9 Cl HEt H Me COOCH.sub.2 CH(CH.sub.3).sub.2 Ms HEt H Me COOCH.sub.2 CH(CH.sub.3).sub.2 Cl HEt H Me COOCH(CH.sub.3)C.sub.2 H.sub.5 Ms HEt H Me COOCH(CH.sub.3)C.sub.2 H.sub.5 Cl HEt H Me COOC(CH.sub.3).sub.3 Ms HEt H Me COOC(CH.sub.3).sub.3 Cl HEt H Me CONHMe Ms HEt H Me CONHMe Cl HEt H Me CONHEt Ms HEt H Me CONHEt Cl HEt H Me CONHCH(CH.sub.3).sub.2 Ms HEt H Me CONHCH(CH.sub.3).sub.2 Cl HEt H Me CONHC(CH.sub.3).sub.3 Ms HEt H Me CONHC(CH.sub.3).sub.3 Cl HEt H Me CONHC.sub.4 H.sub.9 Ms HEt H Me CONHC.sub.4 H.sub.9 Cl HEt H Me CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms HEt H Me CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl HEt H Me CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms HEt H Me CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl HEt H Me CONEt.sub.2 Ms HEt H Me CONEt.sub.2 Cl HEt H Me CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HEt H Me CON[CH(CH.sub.3).sub.2 ].sub.2 Cl HEt H Me Y1 Ms HEt H Me Y1 Cl HEt H Me Y2 Ms HEt H Me Y2 Cl HEt H Me Y3 Ms HEt H Me Y3 Cl HEt H Me COOPh Ms HEt H Me COOPh Cl HEt H Me COOCH.sub.2 Ph Ms HEt H Me COOCH.sub.2 Ph Cl HEt H Me COOCH.sub.2 CHCH.sub.2 Ms HEt H Me COOCH.sub.2 CHCH.sub.2 Cl HEt H Me COOCH.sub.2 C CH Ms HEt H Me COOCH.sub.2 CCH Cl HEt H Me C(O)SMe Ms HEt H Me C(O)SMe Cl HEt H Me C(O)SEt Cl HEt H Me C(O)SCH(CH.sub.3).sub.2 Ms HEt H Me C(O)SCH(CH.sub.3).sub.2 Cl HEt H Me C(O)SC.sub.3 H.sub.7 Ms HEt H Me C(O)SC.sub.3 H.sub.7 Cl HEt H Me C(S)OMe Ms HEt H Me C(S)OMe Cl HEt H Me C(S)OEt Ms HEt H Me C(S)OEt Cl HEt H Me C(S)OCH(CH.sub.3).sub.2 Ms HEt H Me C(S)OCH(CH.sub.3).sub.2 Cl HEt H Me C(S)SC.sub.3 H.sub.7 Ms HEt H Me C(S)SC.sub.3 H.sub.7 Cl HEt H Me C(S)SMe Ms HEt H Me C(S)SMe Cl HEt H Me C(S)SEt Ms HEt H Me C(S)SEt Cl HEt H Me C(S)SCH(CH.sub.3).sub.2 Ms HEt H Me C(S)SCH(CH.sub.3).sub.2 Cl HEt H Me C(S)SC.sub.3 H.sub.7 Ms HEt H Me C(S)SC.sub.3 H.sub.7 Cl HEt H OMe COOMe MeS HEt H OMe COOMe MeSO HEt H OMe COOMe Ms HEt H OMe COOMe Ms Q1Et H OMe COOMe Ms Q2Et H OMe COOMe Ms Q3Et H OMe COOMe Ms Q4Et H OMe COOMe Ms Q5Et H OMe COOMe Ms Q6Et H OMe COOMe Ms Q20Et Me OMe COOMe Ms HEt Cl OMe COOMe Ms HEt CF.sub.3 OMe COOMe Ms HEt OMe OMe COOMe Ms HEt SMe OMe COOMe Ms HEt H OMe COOEt MeS HEt H OMe COOEt MeSO HEt H OMe COOEt Ms HEt H OMe COOEt Ms Q1Et H OMe COOEt Ms Q18Et H OMe COOEt Ms Q13Et H OMe COOEt Ms Q4Et H OMe COOEt Ms Q5Et H OMe COOEt Ms Q6Et H OMe COOEt Ms Q22Et Me OMe COOEt Ms HEt Cl OMe COOEt Ms HEt CF.sub.3 OMe COOEt Ms HEt OMe OMe COOEt Ms HEt SMe OMe COOEt Ms HEt H OMe COOCH(CH.sub.3).sub.2 MeS HEt H OMe COOCH(CH.sub.2).sub.2 MeSO HEt H OMe COOCH(CH.sub.3).sub. 2 Ms HEt H OMe COOCH(CH.sub.3).sub.2 Ms Q7Et H OMe COOCH(CH.sub.3).sub.2 Ms Q12Et H OMe COOCH(CH.sub.3).sub.2 Ms Q9Et H OMe COOCH(CH.sub.3).sub.2 Ms Q4Et H OMe COOCH(CH.sub.3).sub.2 Ms Q5Et H OMe COOCH(CH.sub.3).sub.2 Ms Q6Et H OMe COOCH(CH.sub.3).sub.2 Ms Q17Et Me OMe COOCH(CH.sub.3).sub.2 Ms HEt Cl OMe COOCH(CH.sub.3).sub.2 Ms HEt CF.sub.3 OMe COOCH(CH.sub.3).sub.2 Ms HEt OMe OMe COOCH(CH.sub.3).sub.2 Ms HEt SMe OMe COOCH(CH.sub.3).sub.2 Ms HEt H OMe COOMe Cl HEt H OMe COOMe Cl Q1Et H OMe COOMe Cl Q2Et H OMe COOMe Cl Q3Et H OMe COOEt Cl HEt H OMe COOEt Cl Q1Et H OMe COOEt Cl Q2Et H OMe COOEt Cl Q3Et H OMe COOCH(CH.sub.3).sub.2 Cl HEt H OMe COOCH(CH.sub.3).sub.2 Cl Q1Et H OMe COOCH(CH.sub.3).sub.2 Cl Q2Et H OMe COOCH(CH.sub.3).sub.2 Cl Q3Et H OMe CON(CH.sub. 3).sub.2 MeS HEt H OMe CON(CH.sub.3).sub.2 MeSO HEt H OMe CON(CH.sub.3).sub.2 Ms HEt H OMe CON(CH.sub.3).sub.2 Ms Q1Et H OMe CON(CH.sub.3).sub.2 Ms Q18Et H OMe CON(CH.sub.3).sub.2 Ms Q13Et H OMe CON(CH.sub.3).sub.2 Ms Q4Et H OMe CON(CH.sub.3).sub.2 Ms Q5Et H OMe CON(CH.sub.3).sub.2 Ms Q6Et H OMe CON(CH.sub.3).sub.2 Ms Q22Et Me OMe CON(CH.sub.3).sub.2 Ms HEt Cl OMe CON(CH.sub.3).sub.2 Ms HEt CF.sub.3 OMe CON(CH.sub.3).sub.2 Ms HEt OMe OMe CON(CH.sub.3).sub.2 Ms HEt SMe OMe CON(CH.sub.3).sub.2 Ms HEt H OMe CON(CH.sub.3).sub.2 Cl HEt H OMe CON(CH.sub.3).sub.2 Cl Q1Et H OMe CON(CH.sub.3).sub.2 Cl Q2Et H OMe CON(CH.sub.3).sub.2 Cl Q3Et H OMe COOC.sub.4 H.sub.9 Ms HEt H OMe COOC.sub.4 H.sub.9 Cl HEt H OMe COOCH.sub.2 CH(CH.sub.3).sub.2 Ms HEt H OMe COOCH.sub.2 CH(CH.sub.3).sub.2 Cl HEt H OMe COOCH(CH.sub.3)C.sub.2 H.sub.5 Ms HEt H OMe COOCH(CH.sub.3)C.sub.2 H.sub.5 Cl HEt H OMe COOC(CH.sub.3).sub.3 Ms HEt H OMe COOC(CH.sub.3).sub.3 Cl HEt H OMe CONHMe Ms HEt H OMe CONHMe Cl HEt H OMe CONHEt Ms HEt H OMe CONHEt Cl HEt H OMe CONHCH(CH.sub.3).sub.2 Ms HEt H OMe CONHCH(CH.sub.3).sub.2 Cl HEt H OMe CONHC(CH.sub.3).sub.3 Ms HEt H OMe CONHC(CH.sub.3).sub.3 Cl HEt H OMe CONHC.sub.4 H.sub.9 Ms HEt H OMe CONHC.sub.4 H.sub.9 Cl HEt H OMe CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms HEt H OMe CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl HEt H OMe CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms HEt H OMe CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl HEt H OMe CONEt.sub.2 Ms HEt H OMe CONEt.sub.2 Cl HEt H OMe CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HEt H OMe CON[CH(CH.sub.3).sub.2 ].sub.2 Cl HEt H OMe Y1 Ms HEt H OMe Y1 Cl HEt H OMe Y2 Ms HEt H OMe Y2 Cl HEt H OMe Y3 Ms HEt H OMe Y3 Cl HEt H OMe COOPh Ms HEt H OMe COOPh Cl HEt H OMe COOCH.sub.2 Ph Ms HEt H OMe COOCH.sub.2 Ph Cl HEt H OMe COOCH.sub.2 CHCH.sub.2 Ms HEt H OMe COOCH.sub.2 CHCH.sub.2 Cl HEt H OMe COOCH.sub.2 CCH Ms HEt H OMe COOCH.sub.2 CCH Cl HEt H OMe C(O)SMe Ms HEt H OMe C(O)SMe Cl HEt H OMe C(O)SEt Ms HEt H OMe C(O)SEt Cl HEt H OMe C(O)SCH(CH.sub.3).sub.2 Ms HEt H OMe C(O)SCH(CH.sub.3).sub.2 Cl HEt H OMe C(O)SC.sub.3 H.sub.7 Ms HEt H OMe C(O)SC.sub.3 H.sub.7 Cl HEt H OMe C(S)OMe Ms HEt H OMe C(S)OMe Cl HEt H OMe C(S)OEt Ms HEt H OMe C(S)OEt Cl HEt H OMe C(S)OCH(CH.sub.3).sub.2 Ms HEt H OMe C(S)OCH(CH.sub.3).sub.2 Cl HEt H OMe C(S)SC.sub.3 H.sub.7 Ms HEt H OMe C(S)SC.sub.3 H.sub.7 Cl HEt H OMe C(S)SMe Ms HEt H OMe C(S)SMe Cl HEt H OMe C(S)SEt Ms HEt H OMe C(S)SEt Cl HEt H OMe C(S)SCH(CH.sub.3).sub.2 Ms HEt H OMe C(S)SCH(CH.sub.3).sub.2 Cl HEt H OMe C(S)SC.sub.3 H.sub.7 Ms HEt H OMe C(S)SC.sub.3 H.sub.7 Cl HEt H Br COOMe Ms HEt H Br COOMe Cl HEt H Br COOEt Ms HEt H Br COOEt Cl HEt H Br COOCH(CH.sub.3).sub.2 Ms HEt H Br COOCH(CH.sub.3).sub.2 Cl HEt H Br CON(CH.sub.3).sub.2 Ms HEt H Br CON(CH.sub.3).sub.2 Cl HEt H Br CONHMe Ms HEt H Br CONHEt Ms HEt H Br CONHC.sub.3 H.sub.7 Ms HEt H Br CONHCH(CH.sub.3).sub.2 Ms HEt H Br CONHC(CH.sub.3).sub.3 Ms HEt H Br CONEt.sub.2 Ms HEt H Br CONHC(CH.sub.3).sub.3 Ms HEt H Br CONHC.sub.4 H.sub.9 Ms HEt H Br CONHC.sub.4 H.sub.9 Ms HEt H Br CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HEt H Br Y1 Ms HEt H Br Y2 Ms HEt H Br COOPh Ms HEt H Br COOCH.sub.2 Ph Ms HEt H Br COOCH.sub.2 CHCH.sub.2 Ms HEt H Br COOCH.sub.2 CCH Ms HEt H OEt COOMe Ms HEt H OEt COOMe Cl HEt H OEt COOEt Ms HEt H OEt COOEt Cl HEt H OEt COOCH(CH.sub.3)hd 2 Ms HEt H OEt COOCH(CH.sub.3).sub.2 Cl HEt H OEt CON(CH.sub.3).sub.2 Ms HEt H OEt CON(CH.sub.3).sub.2 Cl HEt H OEt CONHMe Ms HEt H OEt CONHEt Ms HEt H OEt CONHC.sub.3 H.sub.7 Ms HEt H OEt CONHCH(CH.sub.3).sub.2 Ms HEt H OEt CONHC(CH.sub.3).sub.3 Ms HEt H OEt CONEt.sub.2 Ms HEt H OEt CONHC(CH.sub.3).sub.3 Ms HEt H OEt CONHC.sub.4 H.sub.9 Ms HEt H OEt CONHC.sub.4 H.sub.9 Ms HEt H OEt CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HEt H OEt Y1 Ms HEt H OEt Y2 Ms HEt H OEt COOPh Ms HEt H OEt COOCH.sub.2 Ph Ms HEt H OEt COOCH.sub.2 CHCH.sub.2 Ms HEt H OEt COOCH.sub.2 CCH Ms HEt H OCH(CH.sub.3).sub.2 COOMe Ms HEt H OCH(CH.sub.3).sub.2 COOMe Cl HEt H OCH(CH.sub.3).sub.2 COOEt Ms HEt H OCH(CH.sub.3).sub.2 COOEt Cl HEt H OCH(CH.sub.3).sub.2 COOCH(CH.sub.3).sub.2 Ms HEt H OCH(CH.sub.3).sub.2 COOCH(CH.sub.3).sub.2 Cl HEt H OCH(CH.sub.3).sub.2 CON(CH.sub.3).sub.2 Ms HEt H OCH(CH.sub.3).sub.2 CON(CH.sub.3).sub.2 Cl HEt H OCH(CH.sub.3).sub. 2 CONHMe Ms HEt H OCH(CH.sub.3).sub.2 CONHEt Ms HEt H OCH(CH.sub.3).sub.2 CONHC.sub.3 H.sub.7 Ms HEt H OCH(CH.sub.3).sub.2 CONHCH(CH.sub.3).sub.2 Ms HEt H OCH(CH.sub.3).sub.2 CONHC(CH.sub.3).sub.3 Ms HEt H OCH(CH.sub.3).sub.2 CONEt.sub.2 Ms HEt H OCH(CH.sub.3).sub.2 CONHC(CH.sub.3).sub.3 Ms HEt H OCH(CH.sub.3).sub.2 CONHC.sub.4 H.sub.9 Ms HEt H OCH(CH.sub.3).sub.2 CONHC.sub.4 H.sub.9 Ms HEt H OCH(CH.sub.3).sub.2 CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HEt H OCH(CH.sub.3).sub.2 Y1 Ms HEt H OCH(CH.sub.3).sub.2 Y2 Ms HEt H OCH(CH.sub.3).sub.2 COOPh Ms HEt H OCH(CH.sub.3).sub.2 COOCH.sub.2 Ph Ms HEt H OCH(CH.sub.3).sub.2 COOCH.sub.2 CHCH.sub.2 Ms HEt H OCH(CH.sub.3).sub.2 COOCH.sub.2 C CH Ms HEt H CH.sub.2 OCH.sub.3 COOMe Ms HEt H CH.sub.2 OCH.sub.3 COOMe Cl HEt H CH.sub.2 OCH.sub.3 COOEt Ms HEt H CH.sub.2 OCH.sub.3 COOEt Cl HEt H CH.sub.2 OCH.sub.3 COOCH(CH.sub.3).sub.2 Ms HEt H CH.sub.2 OCH.sub.3 COOCH(CH.sub.3).sub.2 Cl HEt H CH.sub.2 OCH.sub.3 CON(CH.sub.3).sub.2 Ms HEt H CH.sub.2 OCH.sub.3 CON(CH.sub.3).sub.2 Cl HEt H CH.sub.2 OCH.sub.3 CONHMe Ms HEt H CH.sub.2 OCH.sub.3 CONHEt Ms HEt H CH.sub.2 OCH.sub.3 CONHC.sub.3 H.sub.7 Ms HEt H CH.sub.2 OCH.sub.3 CONHCH(CH.sub.3).sub.2 Ms HEt H CH.sub.2 OCH.sub.3 CONHC(CH.sub.3).sub.3 Ms HEt H CH.sub.2 OCH.sub.3 CONEt.sub.2 Ms HEt H CH.sub.2 OCH.sub.3 CONHC(CH.sub.3).sub.3 Ms HEt H CH.sub.2 OCH.sub.3 CONHC.sub.4 H.sub.9 Ms HEt H CH.sub.2 OCH.sub.3 CONHC.sub.4 H.sub.9 Ms HEt H CH.sub.2 OCH.sub.3 CON[CH(CH.sub.3).sub.2 ].sub.2 Ms HEt H CH.sub.2 OCH.sub.3 Y1 Ms HEt H CH.sub.2 OCH.sub.3 Y2 Ms HEt H CH.sub.2 OCH.sub.3 COOPh Ms HEt H CH.sub.2 OCH.sub.3 COOCH.sub.2 Ph Ms HEt H CH.sub.2 OCH.sub.3 COOCH.sub.2 CHCH.sub.2 Ms HEt H CH.sub.2 OCH.sub.3 COOCH.sub.2 CCH Ms Hi-Pr H Cl COOMe MeS Hi-Pr H Cl COOMe MeSO Hi-Pr H Cl COOMe Ms Hi-Pr H Cl COOMe Ms Q1i-Pr H Cl COOMe Ms Q2i-Pr H Cl COOMe Ms Q3i-Pr H Cl COOMe Ms Q4i-Pr H Cl COOMe Ms Q5i-Pr H Cl COOMe Ms Q6i-Pr H Cl COOMe Ms Q20i-Pr Me Cl COOMe Ms Hi-Pr Cl Cl COOMe Ms Hi-Pr CF.sub.3 Cl COOMe Ms Hi-Pr OMe Cl COOMe Ms Hi-Pr SMe Cl COOMe Ms Hi-Pr H Cl COOEt MeS Hi-Pr H Cl COOEt MeSO Hi-Pr H Cl COOEt Ms Hi-Pr H Cl COOEt Ms Q1i-Pr H Cl COOEt Ms Q18i-Pr H Cl COOEt Ms Q13i-Pr H Cl COOEt Ms Q4i-Pr H Cl COOEt Ms Q5i-Pr H Cl COOEt Ms Q6i-Pr H Cl COOEt Ms Q22i-Pr Me Cl COOEt Ms Hi-Pr Cl Cl COOEt Ms Hi-Pr CF.sub.3 Cl COOEt Ms Hi-Pr OMe Cl COOEt Ms Hi-Pr SMe Cl COOEt Ms Hi-Pr H Cl COOCH(CH.sub.3).sub.2 MeS Hi-Pr H Cl COOCH(CH.sub.3).sub.2 MeSO Hi-Pr H Cl COOCH(CH.sub.3 .sub.2 Ms Hi-Pr H Cl COOCH(CH.sub.3).sub.2 Ms Q7i Pr H Cl COOCH(CH.sub.3).sub.2 Ms Q12i-Pr H Cl COOCH(CH.sub.3).sub.2 Ms Q9i-Pr H Cl COOCH(CH.sub.3).sub.2 Ms Q4i-Pr H Cl COOCH(CH.sub.3).sub.2 Ms Q5i-Pr H Cl COOCH(CH.sub.3).sub.2 Ms Q6i-Pr H Cl COOCH(CH.sub.3).sub.2 Ms Q17i-Pr Me Cl COOCH(CH.sub.3).sub.2 Ms Hi-Pr Cl Cl COOCH(CH.sub.3).sub.2 Ms Hi-Pr CF.sub.3 Cl COOCH(CH.sub.3).sub.2 Ms Hi-Pr OMe Cl COOCH(CH.sub.3).sub.2 Ms Hi-Pr SMe Cl COOCH(CH.sub.3).sub.2 Ms Hi-Pr H Cl COOMe Cl Hi-Pr H Cl COOMe Cl Q1i-Pr H Cl COOMe Cl Q2i-Pr H Cl COOMe Cl Q3i-Pr H Cl COOEt Cl Hi-Pr H Cl COOEt Cl Q1i-Pr H Cl COOEt Cl Q2i-Pr H Cl COOEt Cl Q3i-Pr H Cl COOCH(CH.sub.3).sub.2 Cl Hi-Pr H Cl COOCH(CH.sub.3).sub.2 Cl Q1i-Pr H Cl COOCH(CH.sub.3).sub.2 Cl Q2i-Pr H Cl COOCH(CH.sub.3).sub.2 Cl Q3i-Pr H Cl CON(CH.sub.3).sub.2 MeS Hi-Pr H Cl CON(CH.sub.3).sub.2 MeSO Hi-Pr H Cl CON(CH.sub.3).sub.2 Ms Hi-Pr H Cl CON(CH.sub.3).sub.2 Ms Q1i-Pr H Cl CON(CH.sub.3).sub.2 Ms Q18i-Pr H Cl CON(CH.sub.3).sub.2 Ms Q13i-Pr H Cl CON(CH.sub.3).sub.2 Ms Q4i-Pr H Cl CON(CH.sub.3).sub.2 Ms Q5i-Pr H Cl CON(CH.sub.3).sub.2 Ms Q6i-Pr H Cl CON(CH.sub.3).sub.2 Ms Q22i-Pr Me Cl CON(CH.sub.3).sub.2 Ms Hi-Pr Cl Cl CON(CH.sub.3).sub.2 Ms Hi-Pr CF.sub.3 Cl CON(CH.sub.3).sub.2 Ms Hi-Pr OMe Cl CON(CH.sub.3).sub.2 Ms Hi-Pr SMe Cl CON(CH.sub.3).sub.2 Ms Hi-Pr H Cl CON(CH.sub.3).sub.2 Cl Hi-Pr H Cl CON(CH.sub.3).sub.2 Cl Q1i-Pr H Cl CON(CH.sub.3).sub.2 Cl Q2i-Pr H Cl CON(CH.sub.3).sub.2 Cl Q3i-Pr H Cl COOC.sub.4 H.sub.9 Ms Hi-Pr H Cl COOC.sub.4 H.sub.9 Cl Hi-Pr H Cl COOCH.sub.2 CH(CH.sub.3).sub.2 Ms Hi-Pr H Cl COOCH.sub.2 CH(CH.sub.3).sub.2 Cl Hi-Pr H Cl COOCH(CH.sub.3)C.sub.2 H.sub.5 Ms Hi-Pr H Cl COOCH(CH.sub.3)C.sub.2 H.sub.5 Cl Hi-Pr H Cl COOC(CH.sub.3).sub.3 Ms Hi-Pr H Cl COOC(CH.sub.3).sub.3 Cl Hi-Pr H Cl CONHMe Ms Hi-Pr H Cl CONHMe Cl Hi-Pr H Cl CONHEt Ms Hi-Pr H Cl CONHEt Cl Hi-Pr H Cl CONHCH(CH.sub.3).sub.2 Ms Hi-Pr H Cl CONHCH(CH.sub.3).sub.2 Cl Hi-Pr H Cl CONHC(CH.sub.3).sub.3 Ms Hi-Pr H Cl CONHC(CH.sub.3).sub.3 Cl Hi-Pr H Cl CONHC.sub.4 H.sub.9 Ms Hi-Pr H Cl CONHC.sub.4 H.sub.9 Cl Hi-Pr H Cl CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms Hi-Pr H Cl CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl Hi-Pr H Cl CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms Hi-Pr H Cl CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl Hi-Pr H Cl CONEt.sub.2 Ms Hi-Pr H Cl CONEt.sub.2 Cl Hi-Pr H Cl CON[CH(CH.sub.3).sub.2 ].sub.2 Ms Hi-Pr H Cl CON[CH(CH.sub.3).sub.2 ].sub.2 Cl Hi-Pr H Cl Y1 Ms Hi-Pr H Cl Y1 Cl Hi-Pr H Cl Y2 Ms Hi-Pr H Cl Y2 Cl Hi-Pr H Cl Y3 Ms Hi-Pr H Cl Y3 Cl Hi-Pr H Cl COOPh Ms Hi-Pr H Cl COOPh Cl Hi-Pr H Cl COOCH.sub.2 Ph Ms Hi-Pr H Cl COOCH.sub.2 Ph Cl Hi-Pr H Cl COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H Cl COOCH.sub.2 CHCH.sub.2 Cl Hi-Pr H Cl COOCH.sub.2 CCH Ms Hi-Pr H Cl COOCH.sub.2 CCH Cl Hi-Pr H Cl C(O)SME Ms Hi-Pr H Cl C(O)SMe Cl Hi-Pr H Cl C(O)SEt Ms Hi-Pr H Cl C(O)SEt Cl Hi-Pr H Cl C(O)SCH(CH.sub.3).sub.2 Ms Hi-Pr H Cl C(O)SCH(CH.sub.3).sub.2 Cl Hi-Pr H Cl C(O)SC.sub.3 H.sub.7 Ms HPr H Cl C(O)SC.sub.3 H.sub.7 Cl HPr H Cl C(S)OMe Ms Hi-Pr H Cl C(S)OMe Cl Hi-Pr H CL C(S)OEt Ms Hi-Pr H Cl C(S)OEt Cl H
TABLE 5__________________________________________________________________________ ##STR36##A B X Y Z Q__________________________________________________________________________i-Pr H Cl C(S)OCH(CH.sub.3).sub.2 Ms Hi-Pr H Cl C(S)OCH(CH.sub.3).sub.2 Cl Hi-Pr H Cl C(S)SC.sub.3 H.sub.7 Ms Hi-Pr H Cl C(S)SC.sub.3 H.sub.7 Cl Hi-Pr H Cl C(S)SMe Ms Hi-Pr H Cl C(S)SMe Cl Hi-Pr H Cl C(S)SEt Ms Hi-Pr H Cl C(S)SEt Cl Hi-Pr H Cl C(S)SCH(CH.sub.3).sub.2 Ms Hi-Pr H Cl C(S)SCH(CH.sub.3).sub.2 Cl Hi-Pr H Cl C(S)SC.sub.3 H.sub.7 Ms Hi-Pr H Cl C(S)SC.sub.3 H.sub.7 Cl Hi-Pr H Me COOMe MeS Hi-Pr H Me COOMe MeSO Hi-Pr H Me COOMe Ms Hi-Pr H Me COOMe Ms Q1i-Pr H Me COOMe Ms Q2i-Pr H Me COOMe Ms Q3i-Pr H Me COOMe Ms Q4i-Pr H Me COOMe Ms Q5i-Pr H Me COOMe Ms Q6i-Pr H Me COOMe Ms Q20i-Pr Me Me COOMe Ms Hi-Pr Cl Me COOMe Ms Hi-Pr CF.sub.3 Me COOMe Ms Hi-Pr OMe Me COOMe Ms Hi-Pr SMe Me COOMe Ms Hi-Pr H Me COOEt MeS Hi-Pr H Me COOEt MeSO Hi-Pr H Me COOEt Ms Hi-Pr H Me COOEt Ms Q1i-Pr H Me COOEt Ms Q18i-Pr H Me COOEt Ms Q13i-Pr H Me COOEt Ms Q4i-Pr H Me COOEt Ms Q5i-Pr H Me COOEt Ms Q6i-Pr H Me COOEt Ms Q22i-Pr Me Me COOEt Ms Hi-Pr Cl Me COOEt Ms Hi-Pr CF.sub.3 Me COOEt Ms Hi-Pr OMe Me COOEt Ms Hi-Pr SMe Me COOEt Ms Hi-Pr H Me COOCH(CH.sub.3).sub.2 MeS Hi-Pr H Me COOCH(CH.sub.3).sub.2 MeSO Hi-Pr H Me COOCH(CH.sub.3).sub.2 Ms Hi-Pr H Me COOCH(CH.sub.3).sub.2 Ms Q7i-Pr H Me COOCH(CH.sub.3).sub.2 Ms Q12i-Pr H Me COOCH(CH.sub.3).sub.2 Ms Q9i-Pr H Me COOCH(CH.sub.3).sub.2 Ms Q4i-Pr H Me COOCH(CH.sub.3).sub.2 Ms Q5i-Pr H Me COOCH(CH.sub.3).sub.2 Ms Q6i-Pr H Me COOCH(CH.sub.3).sub.2 Ms Q17i-Pr Me Me COOCH(CH.sub.3).sub.2 Ms Hi-Pr Cl Me COOCH(CH.sub.3).sub.2 Ms Hi-Pr CF.sub.3 Me COOCH(CH.sub.3).sub.2 Ms Hi-Pr OMe Me COOCH(CH.sub.3).sub.2 Ms Hi-Pr SMe Me COOCH(CH.sub.3).sub.2 Ms Hi-Pr H Me COOMe Cl Hi-Pr H Me COOMe Cl Q1i-Pr H Me COOMe Cl Q2i-Pr H Me COOMe Cl Q3i-Pr H Me COOEt Cl Hi-Pr H Me COOEt Cl Q1i-Pr H Me COOEt Cl Q2i-Pr H Me COOEt Cl Q3i-Pr H Me COOCH(CH.sub.3).sub.2 Cl Hi-Pr H Me COOCH(CH.sub.3).sub.2 Cl Q1i-Pr H Me COOCH(CH.sub.3).sub.2 Cl Q2i-Pr H Me COOCH(CH.sub.3).sub.2 Cl Q3i-Pr H Me CON(CH.sub.3).sub.2 MeS Hi-Pr H Me CON(CH.sub.3).sub.2 MeSO Hi-Pr H Me CON(CH.sub.3).sub.2 Ms Hi-Pr H Me CON(CH.sub.3).sub.2 Ms Q1i-Pr H Me CON(CH.sub.3).sub.2 Ms Q18i-Pr H Me CON(CH.sub.3).sub.2 Ms Q13i-Pr H Me CON(CH.sub.3).sub.2 Ms Q4i-Pr H Me CON(CH.sub.3).sub.2 Ms Q5i-Pr H Me CON(CH.sub.3).sub.2 Ms Q6i-Pr H Me CON(CH.sub.3).sub.2 Ms Q22i-Pr Me Me CON(CH.sub.3).sub.2 Ms Hi-Pr Cl Me CON(CH.sub.3).sub.2 Ms Hi-Pr CF.sub.3 Me CON(CH.sub.3).sub.2 Ms Hi-Pr OMe Me CON(CH.sub.3).sub.2 Ms Hi-Pr SMe Me CON(CH.sub.3).sub.2 Ms Hi-Pr H Me CON(CH.sub.3).sub.2 Cl Hi-Pr H Me CON(CH.sub.3).sub.2 Cl Q1i-Pr H Me CON(CH.sub.3).sub.2 Cl Q2i-Pr H Me CON(CH.sub.3).sub.2 Cl Q3i-Pr H Me COOC.sub.4 H.sub.9 Ms Hi-Pr H Me COOC.sub.4 H.sub.9 Cl Hi-Pr H Me COOCH.sub.2 CH(CH.sub.3).sub.2 Ms Hi-Pr H Me COOCH.sub.2 CH(CH.sub.3).sub.2 Cl Hi-Pr H Me COOCH(CH.sub.3)C.sub.2 H.sub.5 Ms Hi-Pr H Me COOCH(CH.sub.3)C.sub.2 H.sub.5 Cl Hi-Pr H Me COOC(CH.sub.3).sub.3 Ms Hi-Pr H Me COOC(CH.sub.3).sub.3 Cl Hi-Pr H Me CONHMe Ms Hi-Pr H Me CONHMe Cl Hi-Pr H Me CONHEt Ms Hi-Pr H Me CONHEt Cl Hi-Pr H Me CONHCH(CH.sub.3).sub.2 Ms Hi-Pr H Me CONHCH(CH.sub.3).sub.2 Cl Hi-Pr H Me CONHC(CH.sub.3).sub.3 Ms Hi-Pr H Me CONHC(CH.sub.3).sub.3 Cl Hi-Pr H Me CONHC.sub.4 H.sub.9 Ms Hi-Pr H Me CONHC.sub.4 H.sub.9 Cl Hi-Pr H Me CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms Hi-Pr H Me CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl Hi-Pr H Me CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms Hi-Pr H Me CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl Hi-Pr H Me CONEt.sub.2 Ms Hi-Pr H Me CONEt.sub.2 Cl Hi-Pr H Me CON[CH(CH.sub.3).sub.2 ].sub.2 Ms Hi-Pr H Me CON[CH(CH.sub.3).sub.2 ].sub.2 Cl Hi-Pr H Me Y1 Ms Hi-Pr H Me Y1 Cl Hi-Pr H Me Y2 Ms Hi-Pr H Me Y2 Cl Hi-Pr H Me Y3 Ms Hi-Pr H Me Y3 Cl Hi-Pr H Me COOPh Ms Hi-Pr H Me COOPh Cl Hi-Pr H Me COOCH.sub.2 Ph Ms Hi-Pr H Me COOCH.sub.2 Ph Cl Hi-Pr H Me COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H Me COOCH.sub.2 CHCH.sub.2 Cl Hi-Pr H Me COOCH.sub.2 CCH Ms Hi-Pr H Me COOCH.sub.2 CCH Cl Hi-Pr H Me C(O)SMe Ms Hi-Pr H Me C(O)SMe Cl Hi-Pr H Me C(O)SEt Ms Hi-Pr H Me C(O)SEt Cl Hi-Pr H Me C(O)SCH(CH.sub.3).sub.2 Ms Hi-Pr H Me C(O)SCH(CH.sub.3).sub.2 Cl Hi-Pr H Me C(O)SC.sub.3 H.sub.7 Ms Hi-Pr H Me C(O)SC.sub.3 H.sub.7 Cl Hi-Pr H Me C(S)OMe Ms Hi-Pr H Me C(S)OMe Cl Hi-Pr H Me C(S)OEt Ms Hi-Pr H Me C(S)OEt Cl Hi-Pr H Me C(S)OCH(CH.sub.3).sub.2 Ms Hi-Pr H Me C(S)OCH(CH.sub.3).sub.2 Cl Hi-Pr H Me C(S)SC.sub.3 H.sub.7 Ms Hi-Pr H Me C(S)SC.sub.3 H.sub.7 Cl Hi-Pr H Me C(S)SMe Ms Hi-Pr H Me C(S)SMe Cl Hi-Pr H Me C(S)SEt Ms Hi-Pr H Me C(S)SEt Cl Hi-Pr H Me C(S)SCH(CH.sub.3).sub.2 Ms Hi-Pr H Me C(S)SCH(CH.sub.3).sub.2 Cl Hi-Pr H Me C(S)SC.sub.3 H.sub.7 Ms Hi-Pr H Me C(S)SC.sub.3 H.sub.7 Cl Hi-Pr H OMe COOMe MeS Hi-Pr H OMe COOMe MeSO Hi-Pr H OMe COOMe Ms Hi-Pr H OMe COOMe Ms Q1i-Pr H OMe COOMe Ms Q2i-Pr H OMe COOMe Ms Q3i-Pr H OMe COOMe Ms Q4i-Pr H OMe COOMe Ms Q5i-Pr H OMe COOMe Ms Q6i-Pr H OMe COOMe Ms Q20i-Pr Me OMe COOMe Ms Hi-Pr Cl OMe COOMe Ms Hi-Pr CF.sub.3 OMe COOMe Ms Hi-Pr OMe OMe COOMe Ms Hi-Pr SMe OMe COOMe Ms Hi-Pr H OMe COOEt MeS Hi-Pr H OMe COOEt MeSO Hi-Pr H OMe COOEt Ms Hi-Pr H OMe COOEt Ms Q1i-Pr H OMe COOEt Ms Q18i-Pr H OMe COOEt Ms Q13i-Pr H OMe COOEt Ms Q4i-Pr H OMe COOEt Ms Q5i-Pr H OMe COOEt Ms Q6i-Pr H OMe COOEt Ms Q22i-Pr Me OMe COOEt Ms Hi-Pr Cl OMe COOEt Ms Hi-Pr CF.sub.3 OMe COOEt Ms Hi-Pr OMe OMe COOEt Ms Hi-Pr SMe OMe COOEt Ms Hi-Pr H OMe COOCH(CH.sub.3).sub.2 MeS Hi-Pr H OMe COOCH(CH.sub.3).sub.2 MeSO Hi-Pr H OMe COOCH(CH.sub.3).sub.2 Ms Hi-Pr H OMe COOCH(CH.sub.3).sub.2 Ms Q7i-Pr H OMe COOCH(CH.sub.3).sub.2 Ms Q12i-Pr H OMe COOCH(CH.sub.3).sub.2 MS Q9i-Pr H OMe COOCH(CH.sub.3).sub.2 Ms Q4i-Pr H OMe COOCH(CH.sub.3).sub.2 Ms Q5i-Pr H OMe COOCH(CH.sub.3).sub.2 Ms Q6i-Pr H OMe COOCH(CH.sub.3).sub.2 Ms Q17i-Pr Me OMe COOCH(CH.sub.3).sub.2 Ms Hi-Pr Cl OMe COOCH(CH.sub.3).sub.2 Ms Hi-Pr CF.sub.3 OMe COOCH(CH.sub.3).sub.2 Ms Hi-Pr OMe OMe COOCH(CH.sub.3).sub.2 Ms Hi-Pr SMe OMe COOCH(CH.sub.3).sub.2 Ms Hi-Pr H OMe COOMe Cl Hi-Pr H OMe COOMe Cl Q1i-Pr H OMe COOMe Cl Q2i-Pr H OMe COOMe Cl Q3i-Pr H OMe COOEt Cl Hi-Pr H OMe COOEt Cl Q1i-Pr H OMe COOEt Cl Q2i-Pr H OMe COOEt Cl Q3i-Pr H OMe COOCH(CH.sub.3).sub.2 Cl Hi-Pr H OMe COOCH(CH.sub.3).sub.2 Cl Q1i-Pr H OMe COOCH(CH.sub.3).sub.2 Cl Q2i-Pr H OMe COOCH(CH.sub.3).sub.2 Cl Q3i-Pr H OMe CON(CH.sub.3).sub.2 MeS Hi-Pr H OMe CON(CH.sub.3).sub.2 MeSO Hi-Pr H OMe CON(CH.sub.3).sub.2 Ms Hi-Pr H OMe CON(CH.sub.3).sub.2 Ms Q1i-Pr H OMe CON(CH.sub.3).sub.2 Ms Q18i-Pr H OMe CON(CH.sub.3).sub.2 Ms Q13i-Pr H OMe CON(CH.sub.3).sub.2 Ms Q4i-Pr H OMe CON(CH.sub.3).sub.2 Ms Q5i-Pr H OMe CON(CH.sub.3).sub.2 Ms Q6i-Pr H OMe CON(CH.sub.3).sub.2 Ms Q22i-Pr Me OMe CON(CH.sub.3).sub.2 Ms Hi-Pr Cl OMe CON(CH.sub.3).sub.2 Ms Hi-Pr CF.sub. 3 OMe CON(CH.sub.3).sub.2 Ms Hi-Pr OMe OMe CON(CH.sub.3).sub.2 Ms Hi-Pr SMe OMe CON(CH.sub.3).sub.2 Ms Hi-Pr H OMe CON(CH.sub.3).sub.2 Cl Hi-Pr H OMe CON(CH.sub.3).sub.2 Cl Q1i-Pr H OMe CON(CH.sub.3).sub.2 Cl Q2i-Pr H OMe CON(CH.sub.3).sub.2 Cl Q3i-Pr H OMe COOC.sub.4 H.sub.9 Ms Hi-Pr H OMe COOC.sub.4 H.sub.9 Cl Hi-Pr H OMe COOCH.sub.2 CH(CH.sub.3).sub.2 Ms Hi-Pr H OMe COOCH.sub.2 CH(CH.sub.3).sub.2 Cl Hi-Pr H OMe COOCH(CH.sub.3)C.sub.2 H.sub.5 Ms Hi-Pr H OMe COOCH(CH.sub.3)C.sub.2 H.sub.5 Cl Hi-Pr H OMe COOC(CH.sub.3).sub.3 Ms Hi-Pr H OMe COOC(CH.sub.3).sub.3 Cl Hi-Pr H OMe CONHMe Ms Hi-Pr H OMe CONHMe Cl Hi-Pr H OMe CONHEt Ms Hi-Pr H OMe CONHEt Cl Hi-Pr H OMe CONHCH(CH.sub.3).sub.2 Ms Hi-Pr H OMe CONHCH(CH.sub.3).sub.2 Cl Hi-Pr H OMe CONHC(CH.sub.3).sub.3 Ms Hi-Pr H OMe CONHC(CH.sub.3).sub.3 Cl Hi-Pr H OMe CONHC.sub.4 H.sub.9 Ms Hi-Pr H OMe CONHC.sub.4 H.sub.9 Cl Hi-Pr H OMe CONHCH.sub.2 CH(CH.sub.3).sub.2 Ms Hi-Pr H OMe CONHCH.sub.2 CH(CH.sub.3).sub.2 Cl Hi-Pr H OMe CONHCH(CH.sub.3)C.sub.2 H.sub.5 Ms Hi-Pr H OMe CONHCH(CH.sub.3)C.sub.2 H.sub.5 Cl Hi-Pr H OMe CONEt.sub.2 Ms Hi-Pr H OMe CONEt.sub.2 Cl Hi-Pr H OMe CON[CH(CH.sub.3).sub.2 ].sub.2 Ms Hi-Pr H OMe CON[CH(CH.sub.3).sub.2 ].sub.2 Cl Hi-Pr H OMe Y1 Ms Hi-Pr H OMe Y1 Cl Hi-Pr H OMe Y2 Ms Hi-Pr H OMe Y2 Cl Hi-Pr H OMe Y3 Ms Hi-Pr H OMe Y3 Cl Hi-Pr H OMe COOPh Ms Hi-Pr H OMe COOPh Cl Hi-Pr H OMe COOCH.sub.2 Ph Ms Hi-Pr H OMe COOCH.sub.2 Ph Cl Hi-Pr H OMe COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H OMe COOCH.sub.2 CHCH.sub.2 Cl Hi-Pr H OMe COOCH.sub.2 C CH Ms Hi-Pr H OMe COOCH.sub.2 CCH Cl Hi-Pr H OMe C(O)SMe Ms Hi-Pr H OMe C(O)SMe Cl Hi-Pr H OMe C(O)SEt Ms Hi-Pr H OMe C(O)SEt Cl Hi-Pr H OMe C(O)SCH(CH.sub.3).sub.2 Ms Hi-Pr H OMe C(O)SCH(CH.sub.3).sub.2 Cl Hi-Pr H OMe C(O)SC.sub.3 H.sub.7 Ms Hi-Pr H OMe C(O)SC.sub.3 H.sub.7 Cl Hi-Pr H OMe C(S)OMe Ms Hi-Pr H OMe C(S)OMe Cl Hi-Pr H OMe C(S)OEt Ms Hi-Pr H OMe C(S)OEt Cl Hi-Pr H OMe C(S)OCH(CH.sub.3).sub.2 Ms Hi-Pr H OMe C(S)OCH(CH.sub.3).sub.2 Cl Hi-Pr H OMe C(S)SC.sub.3 H.sub.7 Ms Hi-Pr H OMe C(S)SC.sub.3 H.sub.7 Cl Hi-Pr H OMe C(S)SMe Ms Hi-Pr H OMe C(S)SMe Cl Hi-Pr H OMe C(S)SEt Ms Hi-Pr H OMe C(S)SEt Cl Hi-Pr H OMe C(S)SCH(CH.sub.3).sub.2 Ms Hi-Pr H OMe C(S)SCH(CH.sub.3).sub.2 Cl Hi-Pr H OMe C(S)SC.sub.3 H.sub.7 Ms Hi-Pr H OMe C(S)SC.sub.3 H.sub.7 Cl Hi-Pr H Br COOMe Ms Hi-Pr H Br COOMe Cl Hi-Pr H Br COOEt Ms Hi-Pr H Br COOEt Cl Hi-Pr H Br COOCH(CH.sub.3).sub.2 Ms Hi-Pr H Br COOCH(CH.sub.3).sub.2 Cl Hi-Pr H Br CON(CH.sub.3).sub.2 Ms Hi-Pr H Br CON(CH.sub.3).sub.2 Cl Hi-Pr H Br CONHMe Ms Hi-Pr H Br CONHEt Ms Hi-Pr H Br CONHC.sub.3 H.sub.7 Ms Hi-Pr H Br CONHCH(CH.sub.3).sub.2 Ms Hi-Pr H Br CONHC(CH.sub.3).sub.3 Ms Hi-Pr H Br CONEt.sub.2 Ms Hi-Pr H Br CONHC(CH.sub.3).sub.2 Ms Hi-Pr H Br CONHC.sub.4 H.sub.9 Ms Hi-Pr H Br CONHC.sub.4 H.sub.9 Ms Hi-Pr H Br CON[CH(CH.sub.3).sub.2 ].sub.2 Ms Hi-Pr H Br Y1 Ms Hi-Pr H Br Y2 Ms Hi-Pr H Br COOPh Ms Hi-Pr H Br COOCH.sub.2 Ph Ms Hi-Pr H Br COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H Br COOCH.sub.2 C CH Ms Hi-Pr H OEt COOMe Ms Hi-Pr H OEt COOMe Cl Hi-Pr H OEt COOEt Ms Hi-Pr H OEt COOEt Cl Hi-Pr H OEt COOCH(CH.sub.3).sub.2 Ms Hi-Pr H OEt COOCH(CH.sub.3).sub.2 Cl Hi-Pr H OEt CON(CH.sub.3).sub.2 Ms Hi-Pr H OEt CON(CH.sub.3).sub.2 Cl Hi-Pr H OEt CONHMe Ms Hi-Pr H OEt CONHEt Ms Hi-Pr H OEt CONHC.sub.3 H.sub.7 Ms Hi-Pr H OEt CONHCH(CH.sub.3).sub.2 Ms Hi-Pr H OEt CONHC(CH.sub.3).sub.3 Ms Hi-Pr H OEt CONEt.sub.2 Ms Hi-Pr H OEt CONHC(CH.sub.3).sub.3 Ms Hi-Pr H OEt CONHC.sub.4 H.sub.9 Ms Hi-Pr H OEt CONHC.sub.4 H.sub.9 Ms Hi-Pr H OEt CON[CH(CH.sub.3).sub.2 ].sub.2 Ms Hi-Pr H OEt Y1 Ms Hi-Pr H OEt Y2 Ms Hi-Pr H OEt COOPh Ms Hi-Pr H OEt COOCH.sub.2 Ph Ms Hi-Pr H OEt COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H OEt COOCH.sub.2 C CH Ms Hi-Pr H OCH(CH.sub.3).sub.2 COOMe Ms Hi-Pr H OCH(CH.sub.3).sub.2 COOMe Cl Hi-Pr H OCH(CH.sub.3).sub.2 COOEt Ms Hi-Pr H OCH(CH.sub.3).sub.2 COOEt Cl Hi-Pr H OCH(CH.sub.3).sub.2 COOCH(CH.sub.3).sub.2 Ms Hi-Pr H OCH(CH.sub.3).sub.2 COOCH(CH.sub.3).sub.2 Cl Hi-Pr H OCH(CH.sub.3).sub.2 CON(CH.sub.3).sub.2 Ms Hi-Pr H OCH(CH.sub.3).sub.2 CON(CH.sub.3).sub.2 Cl Hi-Pr H OCH(CH.sub.3).sub.2 CONHMe Ms Hi-Pr H OCH(CH.sub.3).sub.2 CONHEt Ms Hi-Pr H OCH(CH.sub.3).sub.2 CONHC.sub.3 H.sub.7 Ms Hi-Pr H OCH(CH.sub.3).sub.2 CONHCH(CH.sub.3).sub.2 Ms Hi-Pr H OCH(CH.sub.3).sub.2 CONHC(CH.sub.3).sub.3 Ms Hi-Pr H OCH(CH.sub.3).sub.2 CONEt.sub.2 Ms Hi-Pr H OCH(CH.sub.3).sub.2 CONHC(CH.sub.3).sub.3 Ms Hi-Pr H OCH(CH.sub.3).sub.2 CONHC.sub.4 H.sub.9 Ms Hi-Pr H OCH(CH.sub.3).sub.2 CONHC.sub.4 H.sub.9 Ms Hi-Pr H OCH(CH.sub.3).sub.2 CON[CH(CH.sub.3).sub.2 ] .sub.2 Ms Hi-Pr H OCH(CH.sub.3).sub.2 Y1 Ms Hi-Pr H OCH(CH.sub.3).sub.2 Y2 Ms Hi-Pr H OCH(CH.sub.3).sub.2 COOPh Ms Hi-Pr H OCH(CH.sub.3).sub.2 COOCH.sub.2 Ph Ms Hi-Pr H OCH(CH.sub.3).sub.2 COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H OCH(CH.sub.3).sub.2 COOCH.sub.2 CCH Ms Hi-Pr H CH.sub.2 OCH.sub.3 COOMe Ms Hi-Pr H CH.sub.2 OCH.sub.3 COOMe Cl Hi-Pr H CH.sub.2 OCH.sub.3 COOEt Ms Hi-Pr H CH.sub.2 OCH.sub.3 COOEt Cl Hi-Pr H CH.sub.2 OCH.sub.3 COOCH(CH.sub.3).sub.2 Ms Hi-Pr H CH.sub.2 OCH.sub.3 COOCH(CH.sub.3).sub.2 Cl Hi-Pr H CH.sub.2 OCH.sub.3 CON(CH.sub.3).sub.2 Ms Hi-Pr H CH.sub.2 OCH.sub.3 CON(CH.sub.3).sub.2 Cl Hi-Pr H CH.sub.2 OCH.sub.3 CONHMe Ms Hi-Pr H CH.sub.2 OCH.sub.3 CONHEt Ms Hi-Pr H CH.sub.2 OCH.sub.3 CONHC.sub.3 H.sub.7 Ms Hi-Pr H CH.sub.2 OCH.sub.3 CONHCH(CH.sub.3).sub.2 Ms Hi-Pr H CH.sub.2 OCH.sub.3 CONHC(CH.sub.3).sub.3 Ms Hi-Pr H CH.sub.2 OCH.sub.3 CONEt.sub.2 Ms Hi-Pr H CH.sub.2 OCH.sub.3 CONHC(CH.sub.3).sub.3 Ms Hi-Pr H CH.sub.2 OCH.sub.3 CONHC.sub.4 H.sub.9 Ms Hi-Pr H CH.sub.2 OCH.sub.3 CONHC.sub.4 H.sub.9 MS Hi-Pr H CH.sub.2 OCH.sub.3 CON[CH(CH.sub.3).sub.2 ].sub.2 Ms Hi-Pr H CH.sub.2 OCH.sub.3 Y1 Ms Hi-Pr H CH.sub.2 OCH.sub.3 Y2 Ms Hi-Pr H CH.sub.2 OCH.sub.3 COOPh Ms Hi-Pr H CH.sub.2 OCH.sub.3 COOCH.sub.2 Ph Ms Hi-Pr H CH.sub.2 OCH.sub.3 COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H CH.sub.2 OCH.sub.3 COOCH.sub.2 CCH Ms HMe H NO.sub.2 COOMe Ms HMe H NO.sub.2 COOEt Ms HMe H NO.sub.2 COOCH(CH.sub.3).sub.2 Ms HMe H NO.sub.2 CONMe.sub.2 Ms HMe H NO.sub.2 CONEt.sub.2 Ms HMe H NO.sub.2 COOC.sub.3 H.sub.7 Ms HMe H NO.sub.2 Y1 Ms HMe H NO.sub.2 Y2 Ms HMe H NO.sub.2 Y3 Ms HMe H NO.sub.2 COOPh Ms HMe H NO.sub.2 COOCH.sub.2 Ph Ms HMe H NO.sub.2 COOCH.sub.2 CHCH.sub.2 Ms HMe H CF.sub.3 COOMe Ms HMe H CF.sub.3 COOEt Ms HMe H CF.sub.3 COOCH(CH.sub.3).sub.2 Ms HMe H CF.sub.3 CONMe.sub.2 Ms HMe H CF.sub.3 CONEt.sub.2 Ms HMe H CF.sub.3 COOC.sub.3 H.sub.7 Ms HMe H CF.sub.3 Y1 Ms HMe H CF.sub.3 Y2 Ms HMe H CF.sub.3 Y3 Ms HMe H CF.sub.3 COOPh Ms HMe H CF.sub.3 COOCH.sub.2 Ph Ms HMe H CF.sub.3 COOCH.sub.2 CHCH.sub.2 Ms HMe H CN COOMe Ms HMe H CN COOEt Ms HMe H CN COOCH(CH.sub.3).sub.2 Ms HMe H CN CONMe.sub.2 Ms HMe H CN CONEt.sub.2 Ms HMe H CN COOC.sub.3 H.sub.7 Ms HMe H CN Y1 Ms HMe H CN Y2 Ms HMe H CN Y3 Ms HMe H CN COOPh Ms HMe H CN COOCH.sub.2 Ph Ms HMe H CN COOCH.sub.2 CHCH.sub.2 Ms HMe H CH.sub.2 OEt COOMe Ms HMe H CH.sub.2 OEt COOEt Ms HMe H CH.sub.2 OEt COOCH(CH.sub.3).sub.2 Ms HMe H CH.sub.2 OEt CONMe.sub.2 Ms HMe H CH.sub.2 OEt CONEt.sub.2 Ms HMe H CH.sub.2 OEt COOC.sub.3 H.sub.7 Ms HMe H CH.sub.2 OEt Y1 Ms HMe H CH.sub.2 OEt Y2 Ms HMe H CH.sub.2 OEt Y3 Ms HMe H CH.sub.2 OEt COOPh Ms HMe H CH.sub.2 OEt COOCH.sub.2 Ph Ms HMe H CH.sub.2 OEt COOCH.sub.2 CHCH.sub.2 Ms HMe H Et COOMe Ms HMe H Et COOEt Ms HMe H Et COOCH(CH.sub.3).sub.2 Ms HMe H Et CONMe.sub.2 Ms HMe H Et CONEt.sub.2 Ms HMe H Et COOC.sub.3 H.sub.7 Ms HMe H Et Y1 Ms HMe H Et Y2 Ms HMe H Et Y3 Ms HMe H Et COOPh Ms HMe H Et COOCH.sub.2 Ph Ms HMe H Et COOCH.sub.2 CHCH.sub.2 Ms HMe H i-Pr COOMe Ms HMe H i-Pr COOEt Ms HMe H i-Pr COOCH(CH.sub.3).sub.2 Ms HMe H i-Pr CONMe.sub.2 Ms HMe H i-Pr CONEt.sub.2 Ms HMe H i-Pr COOC.sub.3 H.sub.7 Ms HMe H i-Pr Y1 Ms HMe H i-Pr Y2 Ms HMe H i-Pr Y3 Ms HMe H i-Pr COOPh Ms HMe H i-Pr COOCH.sub.2 Ph Ms HMe H i-Pr COOCH.sub.2 CHCH.sub.2 Ms HMe H n-Pr COOMe Ms HMe H n-Pr COOEt Ms HMe H n-Pr COOCH(CH.sub.3).sub.2 Ms HMe H n-Pr CONMe.sub.2 Ms HMe H n-Pr CONEt.sub.2 Ms HMe H n-Pr COOC.sub.3 H.sub.7 Ms HMe H n-Pr Y1 Ms HMe H n-Pr Y2 Ms HMe H n-Pr Y3 Ms HMe H n-Pr COOPh Ms HMe H n-Pr COOCH.sub.2 Ph Ms HMe H n-Pr COOCH.sub.2 CHCH.sub.2 Ms HMe H I COOMe Ms HMe H I COOEt Ms HMe H I COOCH(CH.sub.3).sub.2 Ms HMe H I CONMe.sub.2 Ms HMe H I CONEt.sub.2 Ms HMe H I COOC.sub.3 H.sub.7 Ms HMe H I Y1 Ms HMe H I Y2 Ms HMe H I Y3 Ms HMe H I COOPh Ms HMe H I COOCH.sub.2 Ph Ms HMe H I COOCH.sub.2 CHCH.sub.2 Ms HEt H NO.sub.2 COOMe Ms HEt H NO.sub.2 COOEt Ms HEt H NO.sub.2 COOCH(CH.sub.3).sub.2 Ms HEt H NO.sub.2 CONMe.sub.2 Ms HEt H NO.sub.2 CONEt.sub.2 Ms HEt H NO.sub.2 COOC.sub.3 H.sub.7 Ms HEt H NO.sub.2 Y1 Ms HEt H NO.sub.2 Y2 Ms HEt H NO.sub.2 Y3 Ms HEt H NO.sub.2 COOPh Ms HEt H NO.sub.2 COOCH.sub.2 Ph Ms HEt H NO.sub.2 COOCH.sub.2 CHCH.sub.2 Ms HEt H CF.sub.3 COOMe Ms HEt H CF.sub.3 COOEt Ms HEt H CF.sub.3 COOCH(CH.sub.3).sub.2 Ms HEt H CF.sub.3 CONMe.sub.2 Ms HEt H CF.sub.3 CONEt.sub.2 Ms HEt H CF.sub.3 COOC.sub.3 H.sub.7 Ms HEt H CF.sub.3 Y1 Ms HEt H CF.sub.3 Y2 Ms HEt H CF.sub.3 Y3 Ms HEt H CF.sub.3 COOPh Ms HEt H CF.sub.3 COOCH.sub.2 Ph Ms HEt H CF.sub.3 COOCH.sub.2 CHCH.sub.2 Ms HEt H CN COOMe Ms HEt H CN COOEt Ms HEt H CN COOCH(CH.sub.3).sub.2 Ms HEt H CN CONMe.sub.2 Ms HEt H CN CONEt.sub.2 Ms HEt H CN COOC.sub.3 H.sub.7 Ms HEt H CN Y1 Ms HEt H CN Y2 Ms HEt H CN Y3 Ms HEt H CN COOPh Ms HEt H CN COOCH.sub.2 Ph Ms HEt H CN COOCH.sub.2 CHCH.sub.2 Ms HEt H CH.sub.2 OEt COOMe Ms HEt H CH.sub.2 OEt COOEt Ms HEt H CH.sub.2 OEt COOCH(CH.sub.3).sub.2 Ms HEt H CH.sub.2 OEt CONMe.sub.2 Ms HEt H CH.sub.2 OEt CONEt.sub.2 Ms HEt H CH.sub.2 OEt COOC.sub.3 H.sub.7 Ms HEt H CH.sub.2 OEt Y1 Ms HEt H CH.sub.2 OEt Y2 Ms HEt H CH.sub.2 OEt Y3 Ms HEt H CH.sub.2 OEt COOPh Ms HEt H CH.sub.2 OEt COOCH.sub.2 Ph Ms HEt H CH.sub.2 OEt COOCH.sub.2 CHCH.sub.2 Ms HEt H Et COOMe Ms HEt H Et COOEt Ms HEt H Et COOCH(CH.sub.3).sub.2 Ms HEt H Et CONMe.sub.2 Ms HEt H Et CONEt.sub.2 Ms HEt H Et COOC.sub.3 H.sub.7 Ms HEt H Et Y1 Ms HEt H Et Y2 Ms HEt H Et Y3 Ms HEt H Et COOPh Ms HEt H Et COOCH.sub.2 Ph Ms HEt H Et COOCH.sub.2 CHCH.sub.2 Ms HEt H i-Pr COOMe Ms HEt H i-Pr COOEt Ms HEt H i-Pr COOCH(CH.sub.3).sub.2 Ms HEt H i-Pr CONMe.sub.2 Ms HEt H i-Pr CONEt.sub.2 Ms HEt H i-Pr COOC.sub.3 H.sub.7 Ms HEt H i-Pr Y1 Ms HEt H i-Pr Y2 Ms HEt H i-Pr Y3 Ms HEt H i-Pr COOPh Ms HEt H i-Pr COOCH.sub.2 Ph Ms HEt H i-Pr COOCH.sub.2 CHCH.sub.2 Ms HEt H n-Pr COOMe Ms HEt H n-Pr COOEt Ms HEt H n-Pr COOCH(CH.sub.3).sub.2 Ms HEt H n-Pr CONMe.sub.2 Ms HEt H n-Pr CONEt.sub.2 Ms HEt H n-Pr COOC.sub.3 H.sub.7 Ms HEt H n-Pr Y1 Ms HEt H n-Pr Y2 Ms HEt H n-Pr Y3 Ms HEt H n-Pr COOPh Ms HEt H n-Pr COOCH.sub.2 Ph Ms HEt H n-Pr COOCH.sub.2 CHCH.sub.2 Ms HEt H I COOMe Ms HEt H I COOEt Ms HEt H I COOCH(CH.sub.3).sub.2 Ms HEt H I CONMe.sub.2 Ms HEt H I CONEt.sub.2 Ms HEt H I COOC.sub.3 H.sub.7 Ms HEt H I Y1 Ms HEt H I Y2 Ms HEt H I Y3 Ms HEt H I COOPh Ms HEt H I COOCH.sub.2 Ph Ms HEt H I COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H NO.sub.2 COOMe Ms Hi-Pr H NO.sub.2 COOEt Ms Hi-Pr H NO.sub.2 COOCH(CH.sub.3).sub.2 Ms Hi-Pr H NO.sub.2 CONMe.sub.2 Ms Hi-Pr H NO.sub.2 CONEt.sub.2 Ms Hi-Pr H NO.sub.2 COOC.sub.3 H.sub.7 Ms Hi-Pr H NO.sub.2 Y1 Ms Hi-Pr H NO.sub.2 Y2 Ms Hi-Pr H NO.sub.2 Y3 Ms Hi-Pr H NO.sub.2 COOPh Ms Hi-Pr H NO.sub.2 COOCH.sub.2 Ph Ms Hi-Pr H NO.sub.2 COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H CF.sub.3 COOMe Ms Hi-Pr H CF.sub.3 COOEt Ms Hi-Pr H CF.sub.3 COOCH(CH.sub.3).sub.2 Ms Hi-Pr H CF.sub.3 CONMe.sub.2 Ms Hi-Pr H CF.sub.3 CONEt.sub.2 Ms Hi-Pr H CF.sub.3 COOC.sub.3 H.sub.7 Ms Hi-Pr H CF.sub.3 Y1 Ms Hi-Pr H CF.sub.3 Y2 Ms H
TABLE 5__________________________________________________________________________ ##STR37##A B X Y Z Q__________________________________________________________________________i-Pr H CF.sub.3 Y3 Ms Hi-Pr H CF.sub.3 COOPh Ms Hi-Pr H CF.sub.3 COOCH.sub.2 Ph Ms Hi-Pr H CF.sub.3 COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H CN COOMe Ms Hi-Pr H CN COOEt Ms Hi-Pr H CN COOCH(CH.sub.3).sub.2 Ms Hi-Pr H CN CONMe.sub.2 Ms Hi-Pr H CN CONEt.sub.2 Ms Hi-Pr H CN COOC.sub.3 H.sub.7 Ms Hi-Pr H CN Y1 Ms Hi-Pr H CN Y2 Ms Hi-Pr H CN Y3 Ms Hi-Pr H CN COOPh Ms Hi-Pr H CN COOCH.sub.2 Ph Ms Hi-Pr H CN COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H CH.sub.2 OEt COOMe Ms Hi-Pr H CH.sub.2 OEt COOEt Ms Hi-Pr H CH.sub.2 OEt COOCH(CH.sub.3).sub.2 Ms Hi-Pr H CH.sub.2 OEt CONMe.sub.2 Ms Hi-Pr H CH.sub.2 OEt CONEt.sub.2 Ms Hi-Pr H CH.sub.2 OEt COOC.sub.3 H.sub.7 Ms Hi-Pr H CH.sub.2 OEt Y1 Ms Hi-Pr H CH.sub.2 OEt Y2 Ms Hi-Pr H CH.sub.2 OEt Y3 Ms Hi-Pr H CH.sub.2 OEt COOPh Ms Hi-Pr H CH.sub.2 OEt COOCH.sub.2 Ph Ms Hi-Pr H CH.sub.2 OEt COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H Et COOMe Ms Hi-Pr H Et COOEt Ms Hi-Pr H Et COOCH(CH.sub.3).sub.2 Ms Hi-Pr H Et CONMe.sub.2 Ms Hi-Pr H Et CONEt.sub.2 Ms Hi-Pr H Et COOC.sub.3 H.sub.7 Ms Hi-Pr H Et Y1 Ms Hi-Pr H Et Y2 Ms Hi-Pr H Et Y3 Ms Hi-Pr H Et COOPh Ms Hi-Pr H Et COOCH.sub.2 Ph Ms Hi-Pr H Et COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H i-Pr COOMe Ms Hi-Pr H i-Pr COOEt Ms Hi-Pr H i-Pr COOCH(CH.sub.3).sub.2 Ms Hi-Pr H i-Pr CONMe.sub.2 Ms Hi-Pr H i-Pr CONEt.sub.2 Ms Hi-Pr H i-Pr COOC.sub.3 H.sub.7 Ms Hi-Pr H i-Pr Y1 Ms Hi-Pr H i-Pr Y2 Ms Hi-Pr H i-Pr Y3 Ms Hi-Pr H i-Pr COOPh Ms Hi-Pr H i-Pr COOCH.sub.2 Ph Ms Hi-Pr H i-Pr COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H n-Pr COOMe Ms Hi-Pr H n-Pr COOEt Ms Hi-Pr H n-Pr COOCH(CH.sub.3).sub.2 Ms Hi-Pr H n-Pr CONMe.sub.2 Ms Hi-Pr H n-Pr CONEt.sub.2 Ms Hi-Pr H n-Pr COOC.sub.3 H.sub.7 Ms Hi-Pr H n-Pr Y1 Ms Hi-Pr H n-Pr Y2 Ms Hi-Pr H n-Pr Y3 Ms Hi-Pr H n-Pr COOPh Ms Hi-Pr H n-Pr COOCH.sub.2 Ph Ms Hi-Pr H n-Pr COOCH.sub.2 CHCH.sub.2 Ms Hi-Pr H I COOMe Ms Hi-Pr H I COOEt Ms Hi-Pr H I COOCH(CH.sub.3).sub.2 Ms Hi-Pr H I CONMe.sub.2 Ms Hi-Pr H I CONEt.sub.2 Ms Hi-Pr H I COOC.sub.3 H.sub.7 Ms Hi-Pr H I Y1 Ms Hi-Pr H I Y2 Ms Hi-Pr H I Y3 Ms Hi-Pr H I COOPh Ms Hi-Pr H I COOCH.sub.2 Ph Ms Hi-Pr H I COOCH.sub.2 CHCH.sub.2 Ms Hallyl H NO.sub.2 COOMe Ms Hallyl H NO.sub.2 COOEt Ms Hallyl H NO.sub.2 COOCH(CH.sub.3).sub.2 Ms Hallyl H NO.sub.2 CONMe.sub.2 Ms Hallyl H NO.sub.2 CONEt.sub.2 Ms Hallyl H NO.sub.2 COOC.sub.3 H.sub.7 Ms Hallyl H NO.sub.2 Y1 Ms Hallyl H NO.sub.2 Y2 Ms Hallyl H NO.sub.2 Y3 Ms Hallyl H NO.sub.2 COOPh Ms Hallyl H NO.sub.2 COOCH.sub.2 Ph Ms Hallyl H NO.sub.2 COOCH.sub.2 CHCH.sub.2 Ms Hallyl H CF.sub.3 COOMe Ms Hallyl H CF.sub.3 COOEt Ms Hallyl H CF.sub.3 COOCH(CH.sub.3).sub.2 Ms Hallyl H CF.sub.3 CONMe.sub.2 Ms Hallyl H CF.sub.3 CONEt.sub.2 Ms Hallyl H CF.sub.3 COOC.sub.3 H.sub.7 Ms Hallyl H CF.sub.3 Y1 Ms Hallyl H CF.sub.3 Y2 Ms Hallyl H CF.sub.3 Y3 Ms Hallyl H CF.sub.3 COOPh Ms Hallyl H CF.sub.3 COOCH.sub.2 Ph Ms Hallyl H CF.sub.3 COOCH.sub.2 CHCH.sub.2 Ms Hallyl H CN COOMe Ms Hallyl H CN COOEt Ms Hallyl H CN COOCH(CH.sub.3).sub.2 Ms Hallyl H CN CONMe.sub.2 Ms Hallyl H CN CONEt.sub.2 Ms Hallyl H CN COOC.sub.3 H.sub.7 Ms Hallyl H CN Y1 Ms Hallyl H CN Y2 Ms Hallyl H CN Y3 Ms Hallyl H CN COOPh Ms Hallyl H CN COOCH.sub.2 Ph Ms Hallyl H CN COOCH.sub.2 CHCH.sub.2 Ms Hallyl H CH.sub.2 OEt COOMe Ms Hallyl H CH.sub.2 OEt COOEt Ms Hallyl H CH.sub.2 OEt COOCH(CH.sub.3).sub.2 Ms Hallyl H CH.sub.2 OEt CONMe.sub.2 Ms Hallyl H CH.sub.2 OEt CONEt.sub.2 Ms Hallyl H CH.sub.2 OEt COOC.sub.3 H.sub.7 Ms Hallyl H CH.sub.2 OEt Y1 Ms Hallyl H CH.sub.2 OEt Y2 Ms Hallyl H CH.sub.2 OEt Y3 Ms Hallyl H CH.sub.2 OEt COOPh Ms Hallyl H CH.sub.2 OEt COOCH.sub.2 Ph Ms Hallyl H CH.sub.2 OEt COOCH.sub.2 CHCH.sub.2 Ms Hallyl H Et COOMe Ms Hallyl H Et COOEt Ms Hallyl H Et COOCH(CH.sub.3).sub.2 Ms Hallyl H Et CONMe.sub.2 Ms Hallyl H Et CONEt.sub.2 Ms Hallyl H Et COOC.sub.3 H.sub.7 Ms Hallyl H Et Y1 Ms Hallyl H Et Y2 Ms Hallyl H Et Y3 Ms Hallyl H Et COOPh Ms Hallyl H Et COOCH.sub.2 Ph Ms Hallyl H Et COOCH.sub.2 CHCH.sub.2 Ms Hallyl H i-Pr COOMe Ms Hallyl H i-Pr COOEt Ms Hallyl H i-Pr COOCH(CH.sub.3).sub.2 Ms Hallyl H i-Pr CONMe.sub.2 Ms Hallyl H i-Pr CONEt.sub.2 Ms Hallyl H i-Pr COOC.sub.3 H.sub.7 Ms Hallyl H i-Pr Y1 Ms Hallyl H i-Pr Y2 Ms Hallyl H i-Pr Y3 Ms Hallyl H i-Pr COOPh Ms Hallyl H i-Pr COOCH.sub. 2 Ph Ms Hallyl H i-Pr COOCH.sub.2 CHCH.sub.2 Ms Hallyl H n-Pr COOMe Ms Hallyl H n-Pr COOEt Ms Hallyl H n-Pr COOCH(CH.sub.3).sub.2 Ms Hallyl H n-Pr CONMe.sub.2 Ms Hallyl H n-Pr CONEt.sub.2 Ms Hallyl H n-Pr COOC.sub.3 H.sub.7 Ms Hallyl H n-Pr Y1 Ms Hallyl H n-Pr Y2 Ms Hallyl H n-Pr Y3 Ms Hallyl H n-Pr COOPh Ms Hallyl H n-Pr COOCH.sub.2 Ph Ms Hallyl H n-Pr COOCH.sub.2 CHCH.sub.2 Ms Hallyl H I COOMe Ms Hallyl H I COOEt Ms Hallyl H I COOCH(CH.sub.3).sub.2 Ms Hallyl H I CONMe.sub.2 Ms Hallyl H I CONEt.sub.2 Ms Hallyl H I COOC.sub.3 H.sub.7 Ms Hallyl H I Y1 Ms Hallyl H I Y2 Ms Hallyl H I Y3 Ms Hallyl H I COOPh Ms Hallyl H I COOCH.sub.2 Ph Ms Hallyl H I COOCH.sub.2 CHCH.sub.2 Ms Hallyl H Me COOH Ms Hallyl H Cl COOH Ms HMe H Me COOH Ms HMe H Cl COOH Ms HEt H Me COOH Ms HEt H Cl COOH Ms Hi-Pr H Me COOH Ms Hi-Pr H Cl COOH Ms HMe H COOMe CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H COOMe CH.sub.2 OCH.sub.2 CCH Ms HMe H COOMe SCH.sub.3 Ms HMe H COOMe CH.sub.2 OH Ms HMe H COOMe CH.sub.2 SCH.sub.3 Ms HEt H COOMe CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H COOMe CH.sub.2 OCH.sub.2 CCH Ms HEt H COOMe SCH.sub.3 Ms HEt H COOMe CH.sub.2 OH Ms HEt H COOMe CH.sub.2 SCH.sub.3 Ms Hi-Pr H COOMe CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms Hi-Pr H COOMe CH.sub.2 OCH.sub.2 CCH Ms Hi-Pr H COOMe SCH.sub.3 Ms Hi-Pr H COOMe CH.sub.2 OH Ms Hi-Pr H COOMe CH.sub.2 SCH.sub.3 Ms HMe H COOEt CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H COOEt CH.sub.2 OCH.sub.2 CCH Ms HMe H COOEt SCH.sub.3 Ms HMe H COOEt CH.sub.2 OH Ms HMe H COOEt CH.sub.2 SCH.sub.3 Ms HEt H COOEt CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H COOEt CH.sub.2 OCH.sub.2 CCH Ms HEt H COOEt SCH.sub.3 Ms HEt H COOEt CH.sub.2 OH Ms HEt H COOEt CH.sub.2 SCH.sub.3 Ms Hi-Pr H COOEt CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms Hi-Pr H COOEt CH.sub.2 OCH.sub.2 CCH Ms Hi-Pr H COOEt SCH.sub.3 Ms Hi-Pr H COOEt CH.sub.2 OH Ms Hi-Pr H COOEt CH.sub.2 SCH.sub.3 Ms HMe H Me COOY4 Ms HMe H Me COOY5 Ms HMe H Me COOY6 Ms HMe H Me COOCH.sub.2 CH.sub.2 Cl Ms HMe H Me COOCH.sub.2 CF.sub.3 Ms HMe H Me COOCH.sub.2 CClCH.sub.2 Ms HMe H Me COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms HMe H Me COOCH.sub.2 SCH.sub.3 Ms HMe H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H Me COOCH.sub.2 CH.sub.2 OMs Ms HMe H Me COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms HMe H Me COOCH.sub.2 CH.sub.2 Ms Ms HMe H Me COOCH.sub.2 CH.sub.2 CN Ms HMe H Me COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms HMe H Me COOCH.sub.2 CH.sub.2 OH Ms HMe H Me COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms HMe H Me COOY7 Ms HMe H Me COOCH.sub.2 COCH.sub.3 Ms HMe H Me COOCH.sub.2 CO.sub.2 CH.sub.3 Ms HMe H Me COOCH(CH.sub.3)COOEt Ms HMe H Me COOCH.sub.2 CH.sub.2 OPh Ms HMe H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms HMe H Me COOPh4-CH.sub.3 Ms HMe H Me COOPh4-Cl Ms HMe H Me COOPh4-NO.sub.2 Ms HMe H Me COOCH.sub.2 SiMe.sub.3 Ms HMe H Me COOY8 Ms HMe H Me COOCH.sub.2 Y8 Ms HMe H Me COOY9 Ms HMe H Me COOY10 Ms HMe H Me CONHSO.sub.2 CH.sub.3 Ms HMe H Me CONHSO.sub.2 CF.sub.3 Ms HMe H Cl COOY4 Ms HMe H Cl COOY5 Ms HMe H Cl COOY6 Ms HMe H Cl COOCH.sub.2 CH.sub.2 Cl Ms HMe H Cl COOCH.sub.2 CF.sub.3 Ms HMe H Cl COOCH.sub.2 CClCH.sub.2 Ms HMe H Cl COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms HMe H Cl COOCH.sub.2 SCH.sub.3 Ms HMe H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H Cl COOCH.sub.2 CH.sub.2 OMs Ms HMe H Cl COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms HMe H Cl COOCH.sub.2 CH.sub.2 Ms Ms HMe H Cl COOCH.sub.2 CH.sub.2 CN Ms HMe H Cl COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms HMe H Cl COOCH.sub.2 CH.sub.2 OH Ms HMe H Cl COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms HMe H Cl COOY7 Ms HMe H Cl COOCH.sub.2 COCH.sub.3 Ms HMe H Cl COOCH.sub.2 CO.sub.2 CH.sub.3 Ms HMe H Cl COOCH(CH.sub.3)COOEt Ms HMe H Cl COOCH.sub.2 CH.sub.2 OPh Ms HMe H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms HMe H Cl COOPh4-CH.sub.3 Ms HMe H Cl COOPh4-Cl Ms HMe H Cl COOPh4-NO.sub.2 Ms HMe H Cl COOCH.sub.2 SiMe.sub.3 Ms HMe H Cl COOY8 Ms HMe H Cl COOCH.sub.2 Y8 Ms HMe H Cl COOY9 Ms HMe H Cl COOY10 Ms HMe H Cl CONHSO.sub.2 CH.sub.3 Ms HMe H Cl CONHSO.sub.2 CF.sub.3 Ms HMe H OMe COOY4 Ms HMe H OMe COOY5 Ms HMe H OMe COOY6 Ms HMe H OMe COOCH.sub.2 CH.sub.2 Cl Ms HMe H OMe COOCH.sub.2 CF.sub.3 Ms HMe H OMe COOCH.sub.2 CClCH.sub.2 Ms HMe H OMe COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms HMe H OMe COOCH.sub.2 SCH.sub.3 Ms HMe H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H OMe COOCH.sub.2 CH.sub.2 OMs Ms HMe H OMe COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms HMe H OMe COOCH.sub.2 CH.sub.2 Ms Ms HMe H OMe COOCH.sub.2 CH.sub.2 CN Ms HMe H OMe COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms HMe H OMe COOCH.sub.2 CH.sub.2 OH Ms HMe H OMe COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms HMe H OMe COOY7 Ms HMe H OMe COOCH.sub.2 COCH.sub.3 Ms HMe H OMe COOCH.sub.2 CO.sub.2 CH.sub.3 Ms HMe H OMe COOCH(CH.sub.3)COOEt Ms HMe H OMe COOCH.sub.2 CH.sub.2 OPh Ms HMe H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms HMe H OMe COOPh4-CH.sub.3 Ms HMe H OMe COOPh4-Cl Ms HMe H OMe COOPh4-NO.sub.2 Ms HMe H OMe COOCH.sub.2 SiMe.sub.3 Ms HMe H OMe COOY8 Ms HMe H OMe COOCH.sub.2 Y8 Ms HMe H OMe COOY9 Ms HMe H OMe COOY10 Ms HMe H OMe CONHSO.sub.2 CH.sub.3 Ms HMe H OMe CONHSO.sub.2 CF.sub.3 Ms HEt H Me COOY4 Ms HEt H Me COOY5 Ms HEt H Me COOY6 Ms HEt H Me COOCH.sub.2 CH.sub.2 Cl Ms HEt H Me COOCH.sub.2 CF.sub.3 Ms HEt H Me COOCH.sub.2 CClCH.sub.2 Ms HEt H Me COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms HEt H Me COOCH.sub.2 SCH.sub.3 Ms HEt H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H Me COOCH.sub.2 CH.sub.2 OMs Ms HEt H Me COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms HEt H Me COOCH.sub.2 CH.sub.2 Ms Ms HEt H Me COOCH.sub.2 CH.sub.2 CN Ms HEt H Me COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms HEt H Me COOCH.sub.2 CH.sub.2 OH Ms HEt H Me COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms HEt H Me COOY7 Ms HEt H Me COOCH.sub.2 COCH.sub.3 Ms HEt H Me COOCH.sub.2 CO.sub.2 CH.sub.3 Ms HEt H Me COOCH(CH.sub.3)COOEt Ms HEt H Me COOCH.sub.2 CH.sub.2 OPh Ms HEt H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms HEt H Me COOPh4-CH.sub.3 Ms HEt H Me COOPh4-Cl Ms HEt H Me COOPh4-NO.sub.2 Ms HEt H Me COOCH.sub.2 SiMe.sub.3 Ms HEt H Me COOY8 Ms HEt H Me COOCH.sub.2 Y8 Ms HEt H Me COOY9 Ms HEt H Me COOY10 Ms HEt H Me CONHSO.sub.2 CH.sub.3 Ms HEt H Me CONHSO.sub.2 CF.sub.3 Ms HEt H Cl COOY4 Ms HEt H Cl COOY5 Ms HEt H Cl COOY6 Ms HEt H Cl COOCH.sub.2 CH.sub.2 Cl Ms HEt H Cl COOCH.sub.2 CF.sub.3 Ms HEt H Cl COOCH.sub.2 CClCH.sub.2 Ms HEt H Cl COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms HEt H Cl COOCH.sub.2 SCH.sub.3 Ms HEt H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H Cl COOCH.sub.2 CH.sub.2 OMs Ms HEt H Cl COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms HEt H Cl COOCH.sub.2 CH.sub.2 Ms Ms HEt H Cl COOCH.sub.2 CH.sub.2 CN Ms HEt H Cl COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms HEt H Cl COOCH.sub.2 CH.sub.2 OH Ms HEt H Cl COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms HEt H Cl COOY7 Ms HEt H Cl COOCH.sub.2 COCH.sub.3 Ms HEt H Cl COOCH.sub.2 CO.sub.2 CH.sub.3 Ms HEt H Cl COOCH(CH.sub.3)COOEt Ms HEt H Cl COOCH.sub.2 CH.sub.2 OPh Ms HEt H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms HEt H Cl COOPh4-CH.sub.3 Ms HEt H Cl COOPh4-Cl Ms HEt H Cl COOPh4-NO.sub.2 Ms HEt H Cl COOCH.sub.2 SiMe.sub.3 Ms HEt H Cl COOY8 Ms HEt H Cl COOCH.sub.2 Y8 Ms HEt H Cl COOY9 Ms HEt H Cl COOY10 Ms HEt H Cl CONHSO.sub.2 CH.sub.3 Ms HEt H Cl CONHSO.sub.2 CF.sub.3 Ms HEt H OMe COOY4 Ms HEt H OMe COOY5 Ms HEt H OMe COOY6 Ms HEt H OMe COOCH.sub.2 CH.sub.2 Cl Ms HEt H OMe COOCH.sub.2 CF.sub.3 Ms HEt H OMe COOCH.sub.2 CClCH.sub.2 Ms HEt H OMe COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms HEt H OMe COOCH.sub.2 SCH.sub.3 Ms HEt H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H OMe COOCH.sub.2 CH.sub.2 OMs Ms HEt H OMe COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms HEt H OMe COOCH.sub.2 CH.sub.2 Ms Ms HEt H OMe COOCH.sub.2 CH.sub.2 CN Ms HEt H OMe COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms HEt H OMe COOCH.sub.2 CH.sub.2 OH Ms HEt H OMe COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms HEt H OMe COOY7 Ms HEt H OMe COOCH.sub.2 COCH.sub.3 Ms HEt H OMe COOCH.sub.2 CO.sub.2 CH.sub.3 Ms HEt H OMe COOCH(CH.sub.3)COOEt Ms HEt H OMe COOCH.sub.2 CH.sub.2 OPh Ms HEt H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms HEt H OMe COOPh4-CH.sub.3 Ms HEt H OMe COOPh4-Cl Ms HEt H OMe COOPh4-NO.sub.2 Ms HEt H OMe COOCH.sub.2 SiMe.sub.3 Ms HEt H OMe COOY8 Ms HEt H OMe COOCH.sub.2 Y8 Ms HEt H OMe COOY9 Ms HEt H OMe COOY10 Ms HEt H OMe CONHSO.sub.2 CH.sub.3 Ms HEt H OMe CONHSO.sub.2 CF.sub.3 Ms Hi-Pr H Me COOY4 Ms Hi-Pr H Me COOY5 Ms Hi-Pr H Me COOY6 Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 Cl Ms Hi-Pr H Me COOCH.sub.2 CF.sub.3 Ms Hi-Pr H Me COOCH.sub.2 CClCH.sub.2 Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms Hi-Pr H Me COOCH.sub.2 SCH.sub.3 Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 OMs Ms Hi-Pr H Me COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 Ms Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 CN Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 OH Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms Hi-Pr H Me COOY7 Ms Hi-Pr H Me COOCH.sub.2 COCH.sub.3 Ms Hi-Pr H Me COOCH.sub.2 CO.sub.2 CH.sub.3 Ms Hi-Pr H Me COOCH(CH.sub.3)COOEt Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 OPh Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms Hi-Pr H Me COOPh4-CH.sub.3 Ms Hi-Pr H Me COOPh4-Cl Ms Hi-Pr H Me COOPh4-NO.sub.2 Ms Hi-Pr H Me COOCH.sub.2 SiMe.sub.3 Ms Hi-Pr H Me COOY8 Ms Hi-Pr H Me COOCH.sub.2 Y8 Ms Hi-Pr H Me COOY9 Ms Hi-Pr H Me COOY10 Ms Hi-Pr H Me CONHSO.sub.2 CH.sub.3 Ms Hi-Pr H Me CONHSO.sub.2 CF.sub.3 Ms Hi-Pr H Cl COOY4 Ms Hi-Pr H Cl COOY5 Ms Hi-Pr H Cl COOY6 Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 Cl Ms Hi-Pr H Cl COOCH.sub.2 CF.sub.3 Ms Hi-Pr H Cl COOCH.sub.2 CClCH.sub.2 Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms Hi-Pr H Cl COOCH.sub.2 SCH.sub.3 Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 OMs Ms Hi-Pr H Cl COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 Ms Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 CN Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 OH Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms Hi-Pr H Cl COOY7 Ms Hi-Pr H Cl COOCH.sub.2 COCH.sub.3 Ms Hi-Pr H Cl COOCH.sub.2 CO.sub.2 CH.sub.3 Ms Hi-Pr H Cl COOCH(CH.sub.3)COOEt Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 OPh Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms Hi-Pr H Cl COOPh4-CH.sub.3 Ms Hi-Pr H Cl COOPh4-Cl Ms Hi-Pr H Cl COOPh4-NO.sub.2 Ms Hi-Pr H Cl COOCH.sub.2 SiMe.sub.3 Ms Hi-Pr H Cl COOY8 Ms Hi-Pr H Cl COOCH.sub.2 Y8 Ms Hi-Pr H Cl COOY9 Ms Hi-Pr H Cl COOY10 Ms Hi-Pr H Cl CONHSO.sub.2 CH.sub.3 Ms Hi-Pr H Cl CONHSO.sub.2 CF.sub.3 Ms Hi-Pr H OMe COOY4 Ms Hi-Pr H OMe COOY5 Ms Hi-Pr H OMe COOY6 Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 Cl Ms Hi-Pr H OMe COOCH.sub.2 CF.sub.3 Ms Hi-Pr H OMe COOCH.sub.2 CClCH.sub.2 Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 OCH.sub.3 Ms Hi-Pr H OMe COOCH.sub.2 SCH.sub.3 Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 OMs Ms Hi-Pr H OMe COOCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 Ms Hi-Pr H OMe COOCH.sub.2 CH.sub. 2 Ms Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 CN Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 NHCH.sub.3 Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 OH Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 Ms Hi-Pr H OMe COOY7 Ms Hi-Pr H OMe COOCH.sub.2 COCH.sub.3 Ms Hi-Pr H OMe COOCH.sub.2 CO.sub.2 CH.sub.3 Ms Hi-Pr H OMe COOCH(CH.sub.3)COOEt Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 OPh Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms Hi-Pr H OMe COOPh4-CH.sub.3 Ms Hi-Pr H OMe COOPh4-Cl Ms Hi-Pr H OMe COOPh4-NO.sub.2 Ms Hi-Pr H OMe COOCH.sub.2 SiMe.sub.3 Ms Hi-Pr H OMe COOY8 Ms Hi-Pr H OMe COOCH.sub.2 Y8 Ms Hi-Pr H OMe COOY9 Ms Hi-Pr H OMe COOY10 Ms Hi-Pr H OMe CONHSO.sub.2 CH.sub.3 Ms Hi-Pr H OMe CONHSO.sub.2 CF.sub.3 Ms HMe H Me CON(CH.sub.3)OCH.sub.3 Ms HMe H Me CONHPh Ms HMe H Me COOCH.sub.2 COC(CH.sub.3).sub.3 Ms HMe H Me COOCH.sub.2 COPh Ms HMe H Me COOSi(CH.sub.3).sub.3 Ms HMe H Me COONC(CH.sub.3).sub.2 Ms HMe H Me COOY11 Ms HMe H Me COOY12 Ms HMe H Me COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms HMe H Me COOCH.sub.2 OCOCH.sub.3 Ms HMe H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms HMe H OMe CON(CH.sub.3)OCH.sub.3 Ms HMe H OMe CONHPh Ms HMe H OMe COOCH.sub.2 COC(CH.sub.3).sub.3 Ms HMe H OMe COOCH.sub.2 COPh Ms HMe H OMe COOSi(CH.sub.3).sub.3 Ms HMe H OMe COONC(CH.sub.3).sub.2 Ms HMe H OMe COOY11 Ms HMe H OMe COOY12 Ms HMe H OMe COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms HMe H OMe COOCH.sub.2 OCOCH.sub.3 Ms HMe H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms HMe H Cl CON(CH.sub.3)OCH.sub.3 Ms HMe H Cl CONHPh Ms HMe H Cl COOCH.sub.2 COC(CH.sub.3).sub.3 Ms HMe H Cl COOCH.sub.2 COPh Ms HMe H Cl COOSi(CH.sub.3).sub.3 Ms HMe H Cl COONC(CH.sub.3).sub.2 Ms HMe H Cl COOY11 Ms HMe H Cl COOY12 Ms HMe H Cl COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms HMe H Cl COOCH.sub.2 OCOCH.sub.3 Ms HMe H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms HEt H Me CON(CH.sub.3)OCH.sub.3 Ms HEt H Me CONHPh Ms HEt H Me COOCH.sub.2 COC(CH.sub.3).sub.3 Ms HEt H Me COOCH.sub.2 COPh Ms HEt H Me COOSi(CH.sub.3).sub.3 Ms HEt H Me COONC(CH.sub.3).sub.2 Ms HEt H Me COOY11 Ms HEt H Me COOY12 Ms HEt H Me COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms HEt H Me COOCH.sub.2 OCOCH.sub.3 Ms HEt H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms HEt H OMe CON(CH.sub.3)OCH.sub.3 Ms HEt H OMe CONHPh Ms HEt H OMe COOCH.sub.2 COC(CH.sub.3).sub.3 Ms HEt H OMe COOCH.sub.2 COPh Ms HEt H OMe COOSi(CH.sub.3).sub.3 Ms HEt H OMe COONC(CH.sub.3).sub.2 Ms HEt H OMe COOY11 Ms HEt H OMe COOY12 Ms HEt H OMe COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms HEt H OMe COOCH.sub.2 OCOCH.sub.3 Ms HEt H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms HEt H Cl CON(CH.sub.3)OCH.sub.3 Ms HEt H Cl CONHPh Ms HEt H Cl COOCH.sub.2 COC(CH.sub.3).sub.3 Ms HEt H Cl COOCH.sub.2 COPh Ms HEt H Cl COOSi(CH.sub.3).sub.3 Ms HEt H Cl COONC(CH.sub.3).sub.2 Ms HEt H Cl COOY11 Ms HEt H Cl COOY12 Ms HEt H Cl COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms HEt H Cl COOCH.sub.2 OCOCH.sub.3 Ms HEt H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms Hi-Pr H Me CON(CH.sub.3)OCH.sub.3 Ms Hi-Pr H Me CONHPh Ms Hi-Pr H Me COOCH.sub.2 COC(CH.sub.3).sub.3 Ms Hi-Pr H Me COOCH.sub.2 COPh Ms Hi-Pr H Me COOSi(CH.sub.3).sub.3 Ms Hi-Pr H Me COONC(CH.sub.3).sub.2 Ms Hi-Pr H Me COOY11 Ms Hi-Pr H Me COOY12 Ms H
TABLE 5__________________________________________________________________________ ##STR38##A B X Y Z Q__________________________________________________________________________i-Pr H Me COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms Hi-Pr H Me COOCH.sub.2 OCOCH.sub.3 Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms Hi-Pr H Me COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms Hi-Pr H OMe CON(CH.sub.3)OCH.sub.3 Ms Hi-Pr H OMe CONHPh Ms Hi-Pr H OMe COOCH.sub.2 COC(CH.sub.3).sub.3 Ms Hi-Pr H OMe COOCH.sub.2 COPh Ms Hi-Pr H OMe COOSi(CH.sub.3).sub.3 Ms Hi-Pr H OMe COONC(CH.sub.3).sub.2 Ms Hi-Pr H OMe COOY11 Ms Hi-Pr H OMe COOY12 Ms Hi-Pr H OMe COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms Hi-Pr H OMe COOCH.sub.2 OCOCH.sub.3 Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms Hi-Pr H OMe COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms Hi-Pr H Cl CON(CH.sub.3)OCH.sub.3 Ms Hi-Pr H Cl CONHPh Ms Hi-Pr H Cl COOCH.sub.2 COC(CH.sub.3).sub.3 Ms Hi-Pr H Cl COOCH.sub.2 COPh Ms Hi-Pr H Cl COOSi(CH.sub.3).sub.3 Ms Hi-Pr H Cl COONC(CH.sub.3).sub.2 Ms Hi-Pr H Cl COOY11 Ms Hi-Pr H Cl COOY12 Ms Hi-Pr H Cl COOCH.sub.2 OCOC(CH.sub.3).sub.3 Ms Hi-Pr H Cl COOCH.sub.2 OCOCH.sub.3 Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms Hi-Pr H Cl COOCH.sub.2 CH.sub.2 OCH.sub.2 CCH Ms HMe H Me CH.sub.2 OH Ms HMe H Me CH.sub.2 OMe Ms HMe H Me CH.sub.2 OMe Cl HMe H Me CH.sub.2 OMe MeS HMe H Me CH.sub.2 OMe MeSO HMe H Me CH.sub.2 OMe Ms Q1Me H Me CH.sub.2 OMe MeS Q1Me H Me CH.sub.2 OMe MeSO Q1Me H Me CH.sub.2 OMe Ms Q2Me H Me CH.sub.2 OMe MeS Q2Me H Me CH.sub.2 OMe MeSO Q2Me H Me CH.sub.2 OMe Ms Q3Me H Me CH.sub.2 OMe MeS Q3Me H Me CH.sub.2 OMe MeSO Q3Me H Me CH.sub.2 OMe Ms Q4Me H Me CH.sub.2 OMe Ms Q5Me H Me CH.sub.2 OMe Ms Q6Me H Me CH.sub.2 OMe Ms Q7Me H Me CH.sub.2 OMe Ms Q8Me H Me CH.sub.2 OMe Ms Q9Me H Me CH.sub.2 OEt Ms HMe H Me CH.sub.2 OEt Cl HMe H Me CH.sub.2 OEt MeS HMe H Me CH.sub.2 OEt MeSO HMe H Me CH.sub.2 OEt Ms Q1Me H Me CH.sub.2 OEt MeS Q1Me H Me CH.sub.2 OEt MeSO Q1Me H Me CH.sub.2 OEt Ms Q2Me H Me CH.sub.2 OEt MeS Q2Me H Me CH.sub.2 OEt MeSO Q2Me H Me CH.sub.2 OEt Ms Q3Me H Me CH.sub.2 OEt MeS Q3Me H Me CH.sub.2 OEt MeSO Q3Me H Me CH.sub.2 OEt Ms Q4Me H Me CH.sub.2 OEt Ms Q5Me H Me CH.sub.2 OEt Ms Q6Me H Me CH.sub.2 OEt Ms Q7Me H Me CH.sub.2 OEt Ms Q8Me H Me CH.sub.2 OEt Ms Q9Me H Me CH.sub.2 OPri Ms HMe H Me CH.sub.2 OPri Cl HMe H Me CH.sub.2 OPri MeS HMe H Me CH.sub.2 OPri MeSO HMe H Me CH.sub.2 OPri Ms Q1Me H Me CH.sub.2 OPri Ms Q2Me H Me CH.sub.2 OPri Ms Q3Me H Me CH.sub.2 OPrn Ms HMe H Me CH.sub.2 OPrn Cl HMe H Me CH.sub.2 OPrn MeS HMe H Me CH.sub.2 OPrn MeSO HMe H Me CH.sub.2 OCHCH.sub.2 Ms HMe H Me CH.sub.2 OCHCH.sub.2 Cl HMe H Me CH.sub.2 OCHCH.sub.2 MeS HMe H Me CH.sub.2 OCHCH.sub.2 MeSO HMe H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HMe H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HMe H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HMe H Me CH.sub.2 OCH.sub.2 CCH Ms HMe H Me CH.sub.2 OCH.sub.2 CCH Cl HMe H Me CH.sub.2 OCH.sub.2 CCH MeS HMe H Me CH.sub.2 OCH.sub.2 CCH MeSO HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeSO HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 Br Ms HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 CN Ms HMe H Me CH.sub.2 OAmn Ms HMe H Me CH.sub.2 OY5 Ms HMe H Me CHMeOH Ms HMe H Me CHMeOMe Ms HMe H Me CHMeOMe Cl HMe H Me CHMeOMe MeS HMe H Me CHMeOMe MeSO HMe H Me CHMeOMe Ms Q1Me H Me CHMeOMe Ms Q2Me H Me CHMeOMe Ms Q3Me H Me CHMeOEt Ms HMe H Me CHMeOEt Cl HMe H Me CHMeOEt MeS HMe H Me CHMeOEt MeSO HMe H Me CHMeOEt Ms Q1Me H Me CHMeOEt Ms Q2Me H Me CHMeOEt Ms Q3Me H Me CHMeOPri Ms HMe H Me CHMeOPri Cl HMe H Me CHMeOPri MeS HMe H Me CHMeOPri MeSO HMe H Me CHMeOPrn Ms HMe H Me CHMeOCHCH.sub.2 Ms HMe H Me CHMeOCHCH.sub.2 Ms HMe H Me CHMeOCH.sub.2 CHCH.sub.2 Ms HMe H Me CHMeOCH.sub.2 C CH Ms HMe H Me CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe H Me CHMeOY5 Ms HMe H Me CMe.sub.2 OH Ms HMe H Me CMe.sub.2 OMe Ms HMe H Me CMe.sub.2 OMe Cl HMe H Me CMe.sub.2 OMe MeS HMe H Me CMe.sub.2 OMe MeSO HMe H Me CMe.sub.2 OEt Ms HMe H Me CMe.sub.2 OEt Cl HMe H Me CMe.sub.2 OEt MeS HMe H Me CMe.sub.2 OEt MeSO HMe H Me CMe.sub.2 OPri Ms HMe H Me CH.sub.2 CH.sub.2 OMe Ms HMe H Me CH.sub.2 CH.sub.2 OMe Cl HMe H Me CH.sub.2 CH.sub.2 OMe MeS HMe H Me CH.sub.2 CH.sub.2 OMe MeSO HMe H Me CH.sub.2 CH.sub.2 OEt Ms HMe H Me CH.sub.2 CH.sub.2 OEt Cl HMe H Me CH.sub.2 CH.sub.2 OEt MeS HMe H Me CH.sub.2 CH.sub.2 OEt MeSO HMe H Me CH.sub.2 CH.sub.2 OPri Ms HMe H Me CH.sub.2 CH.sub.2 OPri Cl HMe H Me CH.sub.2 CH.sub.2 OPri MeS HMe H Me CH.sub.2 CH.sub.2 OPri MeSO HMe H Me CHEtOH Ms HMe H Me CHEtOMe Ms HMe H Me CHEtOMe Cl HMe H Me CHEtOMe MeS HMe H Me CHEtOMe MeSO HMe H Me CHEtOEt Ms HMe H Me CHEtOPri Ms HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HMe H Me CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HMe H Me CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe H Me CH.sub.2 OY8 Ms HMe H Me CH.sub.2 OY9 Ms HMe H Me CH.sub.2 OY10 Ms HMe H Me CHMeOY8 Ms HMe H Me CHMeOY9 Ms HMe H Me CHMeOY10 Ms HMe H Me CH.sub.2 OY13 Ms HMe H Me CHMeOY13 Ms HMe H Me CH.sub.2 NHMe Ms HMe H Me CH.sub.2 NMe.sub.2 Ms HMe H Me CH.sub.2 NEtMe Ms HMe H Me CH.sub.2 NEt.sub.2 Ms HMe H Me CH.sub.2Y14 Ms HMe H Me CHMeNMe.sub.2 Ms HMe H Me CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe H Me CH.sub.2 OCH.sub.2 Ph Ms HMe H Me CHMeOCH.sub.2 Ph Ms HMe H Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe H Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe H Me CH.sub.2 OCHMeCO.sub.2 Me Ms HMe H Me CH.sub.2 CN Ms HMe H Me CHMeCN Ms HMe H Me CH.sub.2 SMe Ms HMe H Me CH.sub.2 SMe Cl HMe H Me CH.sub.2 SMe MeS HMe H Me CH.sub.2 SMe MeSO HMe H Me CH.sub.2 SEt Ms HMe H Me CH.sub.2 SEt Cl HMe H Me CH.sub.2 SEt MeS HMe H Me CH.sub.2 SEt MeSO HMe H Me CH.sub.2 SOMe Ms HMe H Me CH.sub.2 SOEt Ms HMe H Me CH.sub.2 SO.sub.2 Me Ms HMe H Me CH.sub.2 SO.sub.2 Me Cl HMe H Me CH.sub.2 SO.sub.2 Me MeS HMe H Me CH.sub.2 SO.sub.2 Me MeSO HMe H Me CH.sub.2 SO.sub.2 Et Ms HMe H Me CH.sub.2 SO.sub.2 Et Cl HMe H Me CH.sub.2 SO.sub.2 Et MeS HMe H Me CH.sub.2 SO.sub.2 Et MeSO HMe H Me CHMeSMe Ms HMe H Me CHMeSEt Ms HMe H Me CHMeSO.sub.2 Me Ms HMe H Me CHMeSO.sub.2 Et Ms HMe H Me CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe H Me CH.sub.2 OCOMe Ms HMe H Me CH.sub.2 OCOEt Ms HMe H Me CHMeOCOMe Ms HMe H Me CH.sub.2 OSO.sub.2 Me Ms HMe H Me CH.sub.2 OSO.sub.2 Et Ms HMe H Me CHMeOSO.sub.2 Me Ms HEt H Me CH.sub.2 OH Ms HEt H Me CH.sub.2 OMe Ms HEt H Me CH.sub.2 OMe Cl HEt H Me CH.sub.2 OMe MeS HEt H Me CH.sub.2 OMe MeSO HEt H Me CH.sub.2 OMe Ms Q1Et H Me CH.sub.2 OMe MeS Q1Et H Me CH.sub.2 OMe MeSO Q1Et H Me CH.sub.2 OMe Ms Q2Et H Me CH.sub.2 OMe MeS Q2Et H Me CH.sub.2 OMe MeSO Q2Et H Me CH.sub.2 OMe Ms Q3Et H Me CH.sub.2 OMe MeS Q3Et H Me CH.sub.2 OMe MeSO Q3Et H Me CH.sub.2 OMe Ms Q4Et H Me CH.sub.2 OMe Ms Q5Et H Me CH.sub.2 OMe Ms Q6Et H Me CH.sub.2 OMe Ms Q7Et H Me CH.sub.2 OMe Ms Q8Et H Me CH.sub.2 OMe Ms Q9Et H Me CH.sub.2 OEt Ms HEt H Me CH.sub.2 OEt Cl HEt H Me CH.sub.2 OEt MeS HEt H Me CH.sub.2 OEt MeSO HEt H Me CH.sub.2 OEt Ms Q1Et H Me CH.sub.2 OEt MeS Q1Et H Me CH.sub.2 OEt MeSO Q1Et H Me CH.sub.2 OEt Ms Q2Et H Me CH.sub.2 OEt MeS Q2Et H Me CH.sub.2 OEt MeSO Q2Et H Me CH.sub.2 OEt Ms Q3Et H Me CH.sub.2 OEt MeS Q3Et H Me CH.sub.2 OEt MeSO Q3Et H Me CH.sub.2 OEt Ms Q4Et H Me CH.sub.2 OEt Ms Q5Et H Me CH.sub.2 OEt Ms Q6Et H Me CH.sub.2 OEt Ms Q7Et H Me CH.sub.2 OEt Ms Q8Et H Me CH.sub.2 OEt Ms Q9Et H Me CH.sub.2 OPri Ms HEt H Me CH.sub.2 OPri Cl HEt H Me CH.sub.2 OPri MeS HEt H Me CH.sub.2 OPri MeSO HEt H Me CH.sub.2 OPri Ms Q1Et H Me CH.sub.2 OPri Ms Q2Et H Me CH.sub.2 OPri Ms Q3Et H Me CH.sub.2 OPrn Ms HEt H Me CH.sub.2 OPrn Cl HEt H Me CH.sub.2 OPrn MeS HEt H Me CH.sub.2 OPrn MeSO HEt H Me CH.sub.2 OCHCH.sub.2 Ms HEt H Me CH.sub.2 OCHCH.sub.2 Cl HEt H Me CH.sub.2 OCHCH.sub.2 MeS HEt H Me CH.sub.2 OCHCH.sub.2 MeSO HEt H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HEt H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HEt H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HEt H Me CH.sub.2 OCH.sub.2 CCH Ms HEt H Me CH.sub.2 OCH.sub.2 CCH Cl HEt H Me CH.sub.2 OCH.sub.2 CCH MeS HEt H Me CH.sub.2 OCH.sub.2 CCH MeSO HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeSO HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 Br Ms HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 CN Ms HEt H Me CH.sub.2 OAmn Ms HEt H Me CH.sub.2 OY5 Ms HEt H Me CHMeOH Ms HEt H Me CHMeOMe Ms HEt H Me CHMeOMe Cl HEt H Me CHMeOMe MeS HEt H Me CHMeOMe MeSO HEt H Me CHMeOMe Ms Q1Et H Me CHMeOMe Ms Q2Et H Me CHMeOMe Ms Q3Et H Me CHMeOEt Ms HEt H Me CHMeOEt Cl HEt H Me CHMeOEt MeS HEt H Me CHMeOEt MeSO HEt H Me CHMeOEt Ms Q1Et H Me CHMeOEt Ms Q2Et H Me CHMeOEt Ms Q3Et H Me CHMeOPri Ms HEt H Me CHMeOPri Cl HEt H Me CHMeOPri MeS HEt H Me CHMeOPri MeSO HEt H Me CHMeOPrn Ms HEt H Me CHMeOCHCH.sub.2 Ms HEt H Me CHMeOCHCH.sub.2 Ms HEt H Me CHMeOCH.sub.2 CHCH.sub.2 Ms HEt H Me CHMeOCH.sub.2 CCH Ms HEt H Me CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt H Me CHMeOY5 Ms HEt H Me CMe.sub.2 OH Ms HEt H Me CMe.sub.2 OMe Ms HEt H Me CMe.sub.2 OMe Cl HEt H Me CMe.sub.2 OMe MeS HEt H Me CMe.sub.2 OMe MeSO HEt H Me CMe.sub.2 OEt Ms HEt H Me CMe.sub.2 OEt Cl HEt H Me CMe.sub.2 OEt MeS HEt H Me CMe.sub.2 OEt MeSO HEt H Me CMe.sub.2 OPri Ms HEt H Me CH.sub.2 CH.sub.2 OMe Ms HEt H Me CH.sub.2 CH.sub.2 OMe Cl HEt H Me CH.sub.2 CH.sub.2 OMe MeS HEt H Me CH.sub.2 CH.sub.2 OMe MeSO HEt H Me CH.sub.2 CH.sub.2 OEt Ms HEt H Me CH.sub.2 CH.sub.2 OEt Cl HEt H Me CH.sub.2 CH.sub.2 OEt MeS HEt H Me CH.sub.2 CH.sub.2 OEt MeSO HEt H Me CH.sub.2 CH.sub.2 OPri Ms HEt H Me CH.sub.2 CH.sub.2 OPri Cl HEt H Me CH.sub.2 CH.sub.2 OPri MeS HEt H Me CH.sub.2 CH.sub.2 OPri MeSO HEt H Me CHEtOH Ms HEt H Me CHEtOMe Ms HEt H Me CHEtOMe Cl HEt H Me CHEtOMe MeS HEt H Me CHEtOMe MeSO HEt H Me CHEtOEt Ms HEt H Me CHEtOPri Ms HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HEt H Me CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HEt H Me CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt H Me CH.sub.2 OY8 Ms HEt H Me CH.sub.2 OY9 Ms HEt H Me CH.sub.2 OY10 Ms HEt H Me CHMeOY8 Ms HEt H Me CHMeOY9 Ms HEt H Me CHMeOY10 Ms HEt H Me CH.sub.2 OY13 Ms HEt H Me CHMeOY13 Ms HEt H Me CH.sub.2 NHMe Ms HEt H Me CH.sub.2 NMe.sub.2 Ms HEt H Me CH.sub.2 NEtMe Ms HEt H Me CH.sub.2 NEt.sub.2 Ms HEt H Me CH.sub.2Y14 Ms HEt H Me CHMeNMe.sub.2 Ms HEt H Me CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt H Me CH.sub.2 OCH.sub.2 Ph Ms HEt H Me CHMeOCH.sub.2 Ph Ms HEt H Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt H Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt H Me CH.sub.2 OCHMeCO.sub.2 Me Ms HEt H Me CH.sub.2 CN Ms HEt H Me CHMeCN Ms HEt H Me CH.sub.2 SMe Ms HEt H Me CH.sub.2 SMe Cl HEt H Me CH.sub.2 SMe MeS HEt H Me CH.sub.2 SMe MeSO HEt H Me CH.sub.2 SEt Ms HEt H Me CH.sub.2 SEt Cl HEt H Me CH.sub.2 SEt MeS HEt H Me CH.sub.2 SEt MeSO HEt H Me CH.sub.2 SOMe Ms HEt H Me CH.sub.2 SOEt Ms HEt H Me CH.sub.2 SO.sub.2 Me Ms HEt H Me CH.sub.2 SO.sub.2 Me Cl HEt H Me CH.sub.2 SO.sub.2 Me MeS HEt H Me CH.sub.2 SO.sub.2 Me MeSO HEt H Me CH.sub.2 SO.sub.2 Et Ms HEt H Me CH.sub.2 SO.sub.2 Et Cl HEt H Me CH.sub.2 SO.sub.2 Et MeS HEt H Me CH.sub.2 SO.sub.2 Et MeSO HEt H Me CHMeSMe Ms HEt H Me CHMeSEt Ms HEt H Me CHMeSO.sub.2 Me Ms HEt H Me CHMeSO.sub.2 Et Ms HEt H Me CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt H Me CH.sub.2 OCOMe Ms HEt H Me CH.sub.2 OCOEt Ms HEt H Me CHMeOCOMe Ms HEt H Me CH.sub.2 OSO.sub.2 Me Ms HEt H Me CH.sub.2 OSO.sub.2 Et Ms HEt H Me CHMeOSO.sub.2 Me Ms HPri H Me CH.sub.2 OH Ms HPri H Me CH.sub.2 OMe Ms HPri H Me CH.sub.2 OMe Cl HPri H Me CH.sub.2 OMe MeS HPri H Me CH.sub.2 OMe MeSO HPri H Me CH.sub.2 OMe Ms Q1Pri H Me CH.sub.2 OMe MeS Q1Pri H Me CH.sub.2 OMe MeSO Q1Pri H Me CH.sub.2 OMe Ms Q2Pri H Me CH.sub.2 OMe MeS Q2Pri H Me CH.sub.2 OMe MeSO Q2Pri H Me CH.sub.2 OMe Ms Q3Pri H Me CH.sub.2 OMe MeS Q3Pri H Me CH.sub.2 OMe MeSO Q3Pri H Me CH.sub.2 OMe Ms Q4Pri H Me CH.sub.2 OMe Ms Q5Pri H Me CH.sub.2 OMe Ms Q6Pri H Me CH.sub.2 OMe Ms Q7Pri H Me CH.sub.2 OMe Ms Q8Pri H Me CH.sub.2 OMe Ms Q9Pri H Me CH.sub.2 OEt Ms HPri H Me CH.sub.2 OEt Cl HPri H Me CH.sub.2 OEt MeS HPri H Me CH.sub.2 OEt MeSO HPri H Me CH.sub.2 OEt Ms Q1Pri H Me CH.sub.2 OEt MeS Q1Pri H Me CH.sub.2 OEt MeSO Q1Pri H Me CH.sub.2 OEt Ms Q2Pri H Me CH.sub.2 OEt MeS Q2Pri H Me CH.sub.2 OEt MeSO Q2Pri H Me CH.sub.2 OEt Ms Q3Pri H Me CH.sub.2 OEt MeS Q3Pri H Me CH.sub.2 OEt MeSO Q3Pri H Me CH.sub.2 OEt Ms Q4Pri H Me CH.sub.2 OEt Ms Q5Pri H Me CH.sub.2 OEt Ms Q6Pri H Me CH.sub.2 OEt Ms Q7Pri H Me CH.sub.2 OEt Ms Q8Pri H Me CH.sub.2 OEt Ms Q9Pri H Me CH.sub.2 OPri Ms HPri H Me CH.sub.2 OPri Cl HPri H Me CH.sub.2 OPri MeS HPri H Me CH.sub.2 OPri MeSO HPri H Me CH.sub.2 OPri Ms Q1Pri H Me CH.sub.2 OPri Ms Q2Pri H Me CH.sub.2 OPri Ms Q3Pri H Me CH.sub.2 OPrn Ms HPri H Me CH.sub.2 OPrn Cl HPri H Me CH.sub.2 OPrn MeS HPri H Me CH.sub.2 OPrn MeSO HPri H Me CH.sub.2 OCHCH.sub.2 Ms HPri H Me CH.sub.2 OCHCH.sub.2 Cl HPri H Me CH.sub.2 OCHCH.sub.2 MeS HPri H Me CH.sub.2 OCHCH.sub.2 MeSO HPri H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HPri H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HPri H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HPri H Me CH.sub.2 OCH.sub.2 CCH Ms HPri H Me CH.sub.2 OCH.sub.2 CCH Cl HPr i H Me CH.sub.2 OCH.sub.2 CCH MeS HPri H Me CH.sub.2 OCH.sub.2 CCH MeSO HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeSO HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 Br Ms HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 CN Ms HPri H Me CH.sub.2 OAmn Ms HPri H Me CH.sub.2 OY5 Ms HPri H Me CHMeOH Ms HPri H Me CHMeOMe Ms HPri H Me CHMeOMe Cl HPri H Me CHMeOMe MeS HPri H Me CHMeOMe MeSO HPri H Me CHMeOMe Ms Q1Pri H Me CHMeOMe Ms Q2Pri H Me CHMeOMe Ms Q3Pri H Me CHMeOEt Ms HPri H Me CHMeOEt Cl HPri H Me CHMeOEt MeS HPri H Me CHMeOEt MeSO HPri H Me CHMeOEt Ms Q1Pri H Me CHMeOEt Ms Q2Pri H Me CHMeOEt Ms Q3Pri H Me CHMeOPri Ms HPri H Me CHMeOPri Cl HPri H Me CHMeOPri MeS HPri H Me CHMeOPri MeSO HPri H Me CHMeOPrn Ms HPri H Me CHMeOCHCH.sub.2 Ms HPri H Me CHMeOCHCH.sub.2 Ms HPri H Me CHMeOCH.sub.2 CHCH.sub.2 Ms HPri H Me CHMeOCH.sub.2 CCH Ms HPri H Me CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri H Me CHMeOY5 Ms HPri H Me CMe.sub.2 OH Ms HPri H Me CMe.sub.2 OMe Ms HPri H Me CMe.sub.2 OMe Cl HPri H Me CMe.sub.2 OMe MeS HPri H Me CMe.sub.2 OMe MeSO HPri H Me CMe.sub.2 OEt Ms HPri H Me CMe.sub.2 OEt Cl HPri H Me CMe.sub.2 OEt MeS HPri H Me CMe.sub.2 OEt MeSO HPri H Me CMe.sub.2 OPri Ms HPri H Me CH.sub.2 CH.sub.2 OMe Ms HPri H Me CH.sub.2 CH.sub.2 OMe Cl HPri H Me CH.sub.2 CH.sub.2 OMe MeS HPri H Me CH.sub.2 CH.sub.2 OMe MeSO HPri H Me CH.sub.2 CH.sub.2 OEt Ms HPri H Me CH.sub.2 CH.sub.2 OEt Cl HPri H Me CH.sub.2 CH.sub.2 OEt MeS HPri H Me CH.sub.2 CH.sub.2 OEt MeSO HPri H Me CH.sub.2 CH.sub.2 OPri Ms HPri H Me CH.sub.2 CH.sub.2 OPri Cl HPri H Me CH.sub.2 CH.sub.2 OPri MeS HPri H Me CH.sub.2 CH.sub.2 OPri MeSO HPri H Me CHEtOH Ms HPri H Me CHEtOMe Ms HPri H Me CHEtOMe Cl HPr i H Me CHEtOMe MeS HPri H Me CHEtOMe MeSO HPri H Me CHEtOEt Ms HPri H Me CHEtOPri Ms HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HPri H Me CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HPri H Me CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri H Me CH.sub.2 OY8 Ms HPri H Me CH.sub.2 OY9 Ms HPri H Me CH.sub.2 OY10 Ms HPri H Me CHMeOY8 Ms HPri H Me CHMeOY9 Ms HPri H Me CHMeOY10 Ms HPri H Me CH.sub.2 OY13 Ms HPri H Me CHMeOY13 Ms HPri H Me CH.sub.2 NHMe Ms HPri H Me CH.sub.2 NMe.sub.2 Ms HPri H Me CH.sub. 2 NEtMe Ms HPri H Me CH.sub.2 NEt.sub.2 Ms HPri H Me CH.sub.2Y14 Ms HPri H Me CHMeNMe.sub.2 Ms HPri H Me CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri H Me CH.sub.2 OCH.sub.2 Ph Ms HPri H Me CHMeOCH.sub.2 Ph Ms HPri H Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri H Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri H Me CH.sub.2 OCHMeCO.sub.2 Me Ms HPri H Me CH.sub.2 CN Ms HPri H Me CHMeCN Ms HPri H Me CH.sub.2 SMe Ms HPri H Me CH.sub.2 SMe Cl HPri H Me CH.sub.2 SMe MeS HPri H Me CH.sub.2 SMe MeSO HPri H Me CH.sub.2 SEt Ms HPri H Me CH.sub.2 SEt Cl HPri H Me CH.sub.2 SEt MeS HPri H Me CH.sub.2 SEt MeSO HPri H Me CH.sub.2 SOMe Ms HPri H Me CH.sub.2 SOEt Ms HPri H Me CH.sub.2 SO.sub.2 Me Ms HPri H Me CH.sub.2 SO.sub.2 Me Cl HPri H Me CH.sub.2 SO.sub.2 Me MeS HPri H Me CH.sub.2 SO.sub.2 Me MeSO HPri H Me CH.sub.2 SO.sub.2 Et Ms HPri H Me CH.sub.2 SO.sub.2 Et Cl HPri H Me CH.sub.2 SO.sub.2 Et MeS HPri H Me CH.sub.2 SO.sub.2 Et MeSO HPri H Me CHMeSMe Ms HPri H Me CHMeSEt Ms HPri H Me CHMeSO.sub.2 Me Ms HPri H Me CHMeSO.sub.2 Et Ms HPri H Me CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri H Me CH.sub.2 OCOMe Ms HPri H Me CH.sub.2 OCOEt Ms HPri H Me CHMeOCOMe Ms HPri H Me CH.sub.2 OSO.sub.2 Me Ms HPri H Me CH.sub.2 OSO.sub.2 Et Ms HPri H Me CHMeOSO.sub.2 Me Ms H__________________________________________________________________________
TABLE 5__________________________________________________________________________ ##STR39##A B X Y Z Q__________________________________________________________________________Me H Cl CH.sub.2 OH Ms HMe H Cl CH.sub.2 OMe Ms HMe H Cl CH.sub.2 OMe Cl HMe H Cl CH.sub.2 OMe MeS HMe H Cl CH.sub.2 OMe MeSO HMe H Cl CH.sub.2 OMe Ms Q1Me H Cl CH.sub.2 OMe MeS Q1Me H Cl CH.sub.2 OMe MeSO Q1Me H Cl CH.sub.2 OMe Ms Q2Me H Cl CH.sub.2 OMe MeS Q2Me H Cl CH.sub.2 OMe MeSO Q2Me H Cl CH.sub.2 OMe Ms Q3Me H Cl CH.sub.2 OMe MeS Q3Me H Cl CH.sub.2 OMe MeSO Q3Me H Cl CH.sub.2 OMe Ms Q4Me H Cl CH.sub. 2 OMe Ms Q5Me H Cl CH.sub.2 OMe Ms Q6Me H Cl CH.sub.2 OMe Ms Q7Me H Cl CH.sub.2 OMe Ms Q8Me H Cl CH.sub.2 OMe Ms Q9Me H Cl CH.sub.2 OEt Ms HMe H Cl CH.sub.2 OEt Cl HMe H Cl CH.sub.2 OEt MeS HMe H Cl CH.sub.2 OEt MeSO HMe H Cl CH.sub.2 OEt Ms Q1Me H Cl CH.sub.2 OEt MeS Q1Me H Cl CH.sub.2 OEt MeSO Q1Me H Cl CH.sub.2 OEt Ms Q2Me H Cl CH.sub.2 OEt MeS Q2Me H Cl CH.sub.2 OEt MeSO Q2Me H Cl CH.sub.2 OEt Ms Q3Me H Cl CH.sub.2 OEt MeS Q3Me H Cl CH.sub.2 OEt MeSO Q3Me H Cl CH.sub.2 OEt Ms Q4Me H Cl CH.sub.2 OEt Ms Q5Me H Cl CH.sub.2 OEt Ms Q6Me H Cl CH.sub.2 OEt Ms Q7Me H Cl CH.sub.2 OEt Ms Q8Me H Cl CH.sub.2 OEt Ms Q9Me H Cl CH.sub.2 OPri Ms HMe H Cl CH.sub.2 OPri Cl HMe H Cl CH.sub.2 OPri MeS HMe H Cl CH.sub.2 OPri MeSO HMe H Cl CH.sub.2 OPri Ms Q1Me H Cl CH.sub.2 OPri Ms Q2Me H Cl CH.sub.2 OPri Ms Q3Me H Cl CH.sub.2 OPrn Ms HMe H Cl CH.sub.2 OPrn Cl HMe H Cl CH.sub.2 OPrn MeS HMe H Cl CH.sub.2 OPrn MeSO HMe H Cl CH.sub.2 OCHCH.sub.2 Ms HMe H Cl CH.sub.2 OCHCH.sub.2 Cl HMe H Cl CH.sub.2 OCHCH.sub.2 MeS HMe H Cl CH.sub.2 OCHCH.sub.2 MeSO HMe H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HMe H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HMe H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HMe H Cl CH.sub.2 OCH.sub.2 CCH Ms HMe H Cl CH.sub.2 OCH.sub.2 CCH Cl HMe H Cl CH.sub.2 OCH.sub.2 CCH MeS HMe H Cl CH.sub.2 OCH.sub.2 CCH MeSO HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeSO HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Br Ms HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 CN Ms HMe H Cl CH.sub.2 OAmn Ms HMe H Cl CH.sub.2 OY5 Ms HMe H Cl CHMeOH Ms HMe H Cl CHMeOMe Ms HMe H Cl CHMeOMe Cl HMe H Cl CHMeOMe MeS HMe H Cl CHMeOMe MeSO HMe H Cl CHMeOMe Ms Q1Me H Cl CHMeOMe Ms Q2Me H Cl CHMeOMe Ms Q3Me H Cl CHMeOEt Ms HMe H Cl CHMeOEt Cl HMe H Cl CHMeOEt MeS HMe H Cl CHMeOEt MeSO HMe H Cl CHMeOEt Ms Q1Me H Cl CHMeOEt Ms Q2Me H Cl CHMeOEt Ms Q3Me H Cl CHMeOPri Ms HMe H Cl CHMeOPri Cl HMe H Cl CHMeOPri MeS HMe H Cl CHMeOPri MeSO HMe H Cl CHMeOPrn Ms HMe H Cl CHMeOCHCH.sub.2 Ms HMe H Cl CHMeOCHCH.sub.2 Ms HMe H Cl CHMeOCH.sub.2 CHCH.sub.2 Ms HMe H Cl CHMeOCH.sub.2 CCH Ms HMe H Cl CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe H Cl CHMeOY5 Ms HMe H Cl CHMe.sub.2 OH Ms HMe H Cl CHMe.sub.2 OMe Ms HMe H Cl CHMe.sub.2 OMe Cl HMe H Cl CHMe.sub.2 OMe MeS HMe H Cl CHMe.sub.2 OMe MeSO HMe H Cl CHMe.sub.2 OEt Ms HMe H Cl CHMe.sub.2 OEt Cl HMe H Cl CHMe.sub.2 OEt MeS HMe H Cl CHMe.sub.2 OEt MeSO HMe H Cl CHMe.sub.2 OPri Ms HMe H Cl CH.sub.2 CH.sub.2 OMe Ms HMe H Cl CH.sub.2 CH.sub.2 OMe Cl HMe H Cl CH.sub.2 CH.sub.2 OMe MeS HMe H Cl CH.sub.2 CH.sub.2 OMe MeSO HMe H Cl CH.sub.2 CH.sub.2 OEt Ms HMe H Cl CH.sub.2 CH.sub.2 OEt Cl HMe H Cl CH.sub.2 CH.sub.2 OEt MeS HMe H Cl CH.sub.2 CH.sub.2 OEt MeSO HMe H Cl CH.sub.2 CH.sub.2 OPri Ms HMe H Cl CH.sub.2 CH.sub.2 OPri Cl HMe H Cl CH.sub.2 CH.sub.2 OPri MeS HMe H Cl CH.sub.2 CH.sub.2 OPri MeSO HMe H Cl CHEtOH Ms HMe H Cl CHEtOMe Ms HMe H Cl CHEtOMe Cl HMe H Cl CHEtOMe MeS HMe H Cl CHEtOMe MeSO HMe H Cl CHEtOEt Ms HMe H Cl CHEtOPri Ms HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HMe H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HMe H Cl CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe H Cl CH.sub.2 OY8 Ms HMe H Cl CH.sub.2 OY9 Ms HMe H Cl CH.sub.2 OY10 Ms HMe H Cl CHMeOY8 Ms HMe H Cl CHMeOY9 Ms HMe H Cl CHMeOY10 Ms HMe H Cl CH.sub.2 OY13 Ms HMe H Cl CHMeOY13 Ms HMe H Cl CH.sub.2 NHMe Ms HMe H Cl CH.sub.2 NMe.sub.2 Ms HMe H Cl CH.sub.2 NEtMe Ms HMe H Cl CH.sub.2 NEt.sub.2 Ms HMe H Cl CH.sub.2Y14 Ms HMe H Cl CHMeNMe.sub.2 Ms HMe H Cl CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe H Cl CH.sub.2 OCH.sub.2 Ph Ms HMe H Cl CHMeOCH.sub.2 Ph Ms HMe H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe H Cl CH.sub.2 OCHMeCO.sub.2 Me Ms HMe H Cl CH.sub.2 CN Ms HMe H Cl CHMeCN Ms HMe H Cl CH.sub.2 SMe Ms HMe H Cl CH.sub.2 SMe Cl HMe H Cl CH.sub.2 SMe MeS HMe H Cl CH.sub.2 SMe MeSO HMe H Cl CH.sub.2 SEt Ms HMe H Cl CH.sub.2 SEt Cl HMe H Cl CH.sub.2 SEt MeS HMe H Cl CH.sub.2 SEt MeSO HMe H Cl CH.sub.2 SOMe Ms HMe H Cl CH.sub.2 SOEt Ms HMe H Cl CH.sub.2 SO.sub.2 Me Ms HMe H Cl CH.sub.2 SO.sub.2 Me Cl HMe H Cl CH.sub.2 SO.sub.2 Me MeS HMe H Cl CH.sub.2 SO.sub.2 Me MeSO HMe H Cl CH.sub.2 SO.sub.2 Et Ms HMe H Cl CH.sub.2 SO.sub.2 Et Cl HMe H Cl CH.sub.2 SO.sub.2 Et MeS HMe H Cl CH.sub.2 SO.sub.2 Et MeSO HMe H Cl CHMeSMe Ms HMe H Cl CHMeSEt Ms HMe H Cl CHMeSO.sub.2 Me Ms HMe H Cl CHMeSO.sub.2 Et Ms HMe H Cl CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe H Cl CH.sub.2 OCOMe Ms HMe H Cl CH.sub.2 OCOEt Ms HMe H Cl CHMeOCOMe Ms HMe H Cl CH.sub.2 OSO.sub.2 Me Ms HMe H Cl CH.sub.2 OSO.sub.2 Et Ms HMe H Cl CHMeOSO.sub.2 Me Ms HEt H Cl CH.sub.2 OH Ms HEt H Cl CH.sub.2 OMe Ms HEt H Cl CH.sub.2 OMe Cl HEt H Cl CH.sub.2 OMe MeS HEt H Cl CH.sub.2 OMe MeSO HEt H Cl CH.sub.2 OMe Ms Q1Et H Cl CH.sub.2 OMe MeS Q1Et H Cl CH.sub.2 OMe MeSO Q1Et H Cl CH.sub.2 OMe Ms Q2Et H Cl CH.sub.2 OMe MeS Q2Et H Cl CH.sub.2 OMe MeSO Q2Et H Cl CH.sub.2 OMe Ms Q3Et H Cl CH.sub.2 OMe MeS Q3Et H Cl CH.sub.2 OMe MeSO Q3Et H Cl CH.sub.2 OMe Ms Q4Et H Cl CH.sub.2 OMe Ms Q5Et H Cl CH.sub.2 OMe Ms Q6Et H Cl CH.sub.2 OMe Ms Q7Et H Cl CH.sub.2 OMe Ms Q8Et H Cl CH.sub.2 OMe Ms Q9Et H Cl CH.sub.2 OEt Ms HEt H Cl CH.sub.2 OEt Cl HEt H Cl CH.sub.2 OEt MeS HEt H Cl CH.sub.2 OEt MeSO HEt H Cl CH.sub.2 OEt Ms Q1Et H Cl CH.sub.2 OEt MeS Q1Et H Cl CH.sub.2 OEt MeSO Q1Et H Cl CH.sub.2 OEt Ms Q2Et H Cl CH.sub.2 OEt MeS Q2Et H Cl CH.sub.2 OEt MeSO Q2Et H Cl CH.sub.2 OEt Ms Q3Et H Cl CH.sub.2 OEt MeS Q3Et H Cl CH.sub.2 OEt MeSO Q3Et H Cl CH.sub.2 OEt Ms Q4Et H Cl CH.sub.2 OEt Ms Q5Et H Cl CH.sub.2 OEt Ms Q6Et H Cl CH.sub.2 OEt Ms Q7Et H Cl CH.sub.2 OEt Ms Q8Et H Cl CH.sub.2 OEt Ms Q9Et H Cl CH.sub.2 OPri Ms HEt H Cl CH.sub.2 OPri Cl HEt H Cl CH.sub.2 OPri MeS HEt H Cl CH.sub.2 OPri MeSO HEt H Cl CH.sub.2 OPri Ms Q1Et H Cl CH.sub.2 OPri Ms Q2Et H Cl CH.sub.2 OPri Ms Q3Et H Cl CH.sub.2 OPrn Ms HEt H Cl CH.sub.2 OPrn Cl HEt H Cl CH.sub.2 OPrn MeS HEt H Cl CH.sub.2 OPrn MeSO HEt H Cl CH.sub.2 OCHCH.sub.2 Ms HEt H Cl CH.sub.2 OCHCH.sub.2 Cl HEt H Cl CH.sub.2 OCHCH.sub.2 MeS HEt H Cl CH.sub.2 OCHCH.sub.2 MeSO HEt H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HEt H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HEt H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HEt H Cl CH.sub.2 OCH.sub.2 C CH Ms HEt H Cl CH.sub.2 OCH.sub.2 CCH Cl HEt H Cl CH.sub.2 OCH.sub.2 CCH MeS HEt H Cl CH.sub.2 OCH.sub.2 CCH MeSO HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeSO HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Br Ms HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 CN Ms HEt H Cl CH.sub.2 OAmn Ms HEt H Cl CH.sub.2 OY5 Ms HEt H Cl CHMeOH Ms HEt H Cl CHMeOMe Ms HEt H Cl CHMeOMe Cl HEt H Cl CHMeOMe MeS HEt H Cl CHMeOMe MeSO HEt H Cl CHMeOMe Ms Q1Et H Cl CHMeOMe Ms Q2Et H Cl CHMeOMe Ms Q3Et H Cl CHMeOEt Ms HEt H Cl CHMeOEt Cl HEt H Cl CHMeOEt MeS HEt H Cl CHMeOEt MeSO HEt H Cl CHMeOEt Ms Q1Et H Cl CHMeOEt Ms Q2Et H Cl CHMeOEt Ms Q3Et H Cl CHMeOPri Ms HEt H Cl CHMeOPri Cl HEt H Cl CHMeOPri MeS HEt H Cl CHMeOPri MeSO HEt H Cl CHMeOPrn Ms HEt H Cl CHMeOCHCH.sub.2 Ms HEt H Cl CHMeOCHCH.sub.2 Ms HEt H Cl CHMeOCH.sub.2 CHCH.sub.2 Ms HEt H Cl CHMeOCH.sub.2 CCH Ms HEt H Cl CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt H Cl CHMeOY5 Ms HEt H Cl CMe.sub.2 OH Ms HEt H Cl CMe.sub.2 OMe Ms HEt H Cl CMe.sub.2 OMe Cl HEt H Cl CMe.sub.2 OMe MeS HEt H Cl CMe.sub.2 OMe MeSO HEt H Cl CMe.sub.2 OEt Ms HEt H Cl CMe.sub.2 OEt Cl HEt H Cl CMe.sub.2 OEt MeS HEt H Cl CMe.sub.2 OEt MeSO HEt H Cl CMe.sub.2 OPri Ms HEt H Cl CH.sub.2 CH.sub.2 OMe Ms HEt H Cl CH.sub.2 CH.sub.2 OMe Cl HEt H Cl CH.sub.2 CH.sub.2 OMe MeS HEt H Cl CH.sub.2 CH.sub.2 OMe MeSO HEt H Cl CH.sub.2 CH.sub.2 OEt Ms HEt H Cl CH.sub.2 CH.sub.2 OEt Cl HEt H Cl CH.sub.2 CH.sub.2 OEt MeS HEt H Cl CH.sub.2 CH.sub.2 OEt MeSO HEt H Cl CH.sub.2 CH.sub.2 OPri Ms HEt H Cl CH.sub.2 CH.sub.2 OPri Cl HEt H Cl CH.sub.2 CH.sub.2 OPri MeS HEt H Cl CH.sub.2 CH.sub.2 OPri MeSO HEt H Cl CHEtOH Ms HEt H Cl CHEtOMe Ms HEt H Cl CHEtOMe Cl HEt H Cl CHEtOMe MeS HEt H Cl CHEtOMe MeSO HEt H Cl CHEtOEt Ms HEt H Cl CHEtOPri Ms HEt H Cl CH.sub.2 OCH.sub.2 CH.sub. 2 OMe Ms HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HEt H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HEt H Cl CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt H Cl CH.sub.2 OY8 Ms HEt H Cl CH.sub.2 OY9 Ms HEt H Cl CH.sub.2 OY10 Ms HEt H Cl CHMeOY8 Ms HEt H Cl CHMeOY9 Ms HEt H Cl CHMeOY10 Ms HEt H Cl CH.sub.2 OY13 Ms HEt H Cl CHMeOY13 Ms HEt H Cl CH.sub.2 NHMe Ms HEt H Cl CH.sub.2 NMe.sub.2 Ms HEt H Cl CH.sub.2 NEtMe Ms HEt H Cl CH.sub.2 NEt.sub.2 Ms HEt H Cl CH.sub.2Y14 Ms HEt H Cl CHMeNMe.sub.2 Ms HEt H Cl CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt H Cl CH.sub.2 OCH.sub.2 Ph Ms HEt H Cl CHMeOCH.sub. 2 Ph Ms HEt H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt H Cl CH.sub.2 OCHMeCO.sub.2 Me Ms HEt H Cl CH.sub.2 CN Ms HEt H Cl CHMeCN Ms HEt H Cl CH.sub.2 SMe Ms HEt H Cl CH.sub.2 SMe Cl HEt H Cl CH.sub.2 SMe MeS HEt H Cl CH.sub.2 SMe MeSO HEt H Cl CH.sub.2 SEt Ms HEt H Cl CH.sub.2 SEt Cl HEt H Cl CH.sub.2 SEt MeS HEt H Cl CH.sub.2 SEt MeSO HEt H Cl CH.sub.2 SOMe Ms HEt H Cl CH.sub.2 SOEt Ms HEt H Cl CH.sub.2 SO.sub.2 Me Ms HEt H Cl CH.sub.2 SO.sub.2 Me Cl HEt H Cl CH.sub.2 SO.sub.2 Me MeS HEt H Cl CH.sub.2 SO.sub.2 Me MeSO HEt H Cl CH.sub.2 SO.sub.2 Et Ms HEt H Cl CH.sub.2 SO.sub.2 Et Cl HEt H Cl CH.sub.2 SO.sub.2 Et MeS HEt H Cl CH.sub.2 SO.sub.2 Et MeSO HEt H Cl CHMeSMe Ms HEt H Cl CHMeSEt Ms HEt H Cl CHMeSO.sub.2 Me Ms HEt H Cl CHMeSO.sub.2 Et Ms HEt H Cl CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt H Cl CH.sub.2 OCOMe Ms HEt H Cl CH.sub.2 OCOEt Ms HEt H Cl CHMeOCOMe Ms HEt H Cl CH.sub.2 OSO.sub.2 Me Ms HEt H Cl CH.sub.2 OSO.sub.2 Et Ms HEt H Cl CHMeOSO.sub.2 Me Ms HPri H Cl CH.sub.2 OH Ms HPri H Cl CH.sub.2 OMe Ms HPri H Cl CH.sub.2 OMe Cl HPri H Cl CH.sub.2 OMe MeS HPri H Cl CH.sub.2 OMe MeSO HPri H Cl CH.sub.2 OMe Ms Q1Pri H Cl CH.sub.2 OMe MeS Q1Pri H Cl CH.sub.2 OMe MeSO Q1Pri H Cl CH.sub.2 OMe Ms Q2Pri H Cl CH.sub.2 OMe MeS Q2Pri H Cl CH.sub.2 OMe MeSO Q2Pri H Cl CH.sub.2 OMe Ms Q3Pri H Cl CH.sub.2 OMe MeS Q3Pri H Cl CH.sub.2 OMe MeSO Q3Pri H Cl CH.sub.2 OMe Ms Q4Pri H Cl CH.sub.2 OMe Ms Q5Pri H Cl CH.sub.2 OMe Ms Q6Pri H Cl CH.sub.2 OMe Ms Q7Pri H Cl CH.sub.2 OMe Ms Q8Pri H Cl CH.sub.2 OMe Ms Q9Pri H Cl CH.sub.2 OEt Ms HPri H Cl CH.sub.2 OEt Cl HPri H Cl CH.sub.2 OEt MeS HPri H Cl CH.sub.2 OEt MeSO HPri H Cl CH.sub.2 OEt Ms Q1Pri H Cl CH.sub.2 OEt MeS Q1Pri H Cl CH.sub.2 OEt MeSO Q1Pri H Cl CH.sub.2 OEt Ms Q2Pri H Cl CH.sub.2 OEt MeS Q2Pri H Cl CH.sub.2 OEt MeSO Q2Pri H Cl CH.sub.2 OEt Ms Q3Pri H Cl CH.sub.2 OEt MeS Q3Pri H Cl CH.sub.2 OEt MeSO Q3Pr i H Cl CH.sub.2 OEt Ms Q4Pri H Cl CH.sub.2 OEt Ms Q5Pri H Cl CH.sub.2 OEt Ms Q6Pri H Cl CH.sub.2 OEt Ms Q7Pri H Cl CH.sub.2 OEt Ms Q8Pri H Cl CH.sub.2 OEt Ms Q9Pri H Cl CH.sub.2 OPri Ms HPri H Cl CH.sub.2 OPri Cl HPri H Cl CH.sub.2 OPri MeS HPri H Cl CH.sub.2 OPri MeSO HPri H Cl CH.sub.2 OPri Ms Q1Pri H Cl CH.sub.2 OPri Ms Q2Pri H Cl CH.sub.2 OPri Ms Q3Pri H Cl CH.sub.2 OPrn Ms HPri H Cl CH.sub.2 OPrn Cl HPri H Cl CH.sub.2 OPrn MeS HPri H Cl CH.sub.2 OPrn MeSO HPri H Cl CH.sub.2 OCHCH.sub.2 Ms HPri H Cl CH.sub.2 OCHCH.sub.2 Cl HPri H Cl CH.sub.2 OCHCH.sub.2 MeS HPri H Cl CH.sub.2 OCHCH.sub.2 MeSO HPri H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HPri H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HPri H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HPri H Cl CH.sub.2 OCH.sub.2 CCH Ms HPri H Cl CH.sub.2 OCH.sub.2 CCH Cl HPri H Cl CH.sub.2 OCH.sub.2 CCH MeS HPri H Cl CH.sub.2 OCH.sub.2 CCH MeSO HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeSO HPri H Cl CH.sub. 2 OCH.sub.2 CH.sub.2 Br Ms HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 CN Ms HPri H Cl CH.sub.2 OAmn Ms HPri H Cl CH.sub.2 OY5 Ms HPri H Cl CHMeOH Ms HPri H Cl CHMeOMe Ms HPri H Cl CHMeOMe Cl HPri H Cl CHMeOMe MeS HPri H Cl CHMeOMe MeSO HPri H Cl CHMeOMe Ms Q1Pri H Cl CHMeOMe Ms Q2Pri H Cl CHMeOMe Ms Q3Pri H Cl CHMeOEt Ms HPri H Cl CHMeOEt Cl HPri H Cl CHMeOEt MeS HPri H Cl CHMeOEt MeSO HPri H Cl CHMeOEt Ms Q1Pri H Cl CHMeOEt Ms Q2Pri H Cl CHMeOEt Ms Q3Pri H Cl CHMeOPri Ms HPri H Cl CHMeOPri Cl HPri H Cl CHMeOPri MeS HPri H Cl CHMeOPri MeSO HPri H Cl CHMeOPrn Ms HPri H Cl CHMeOCHCH.sub.2 Ms HPri H Cl CHMeOCH CH.sub.2 Ms HPri H Cl CHMeOCH.sub.2 CHCH.sub.2 Ms HPri H Cl CHMeOCH.sub.2 CCH Ms HPri H Cl CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri H Cl CHMeOY5 Ms HPri H Cl CMe.sub.2 OH Ms HPri H Cl CMe.sub.2 OMe Ms HPri H Cl CMe.sub.2 OMe Cl HPri H Cl CMe.sub.2 OMe MeS HPri H Cl CMe.sub.2 OMe MeSO HPri H Cl CMe.sub.2 OEt Ms HPri H Cl CMe.sub.2 OEt Cl HPri H Cl CMe.sub.2 OEt MeS HPri H Cl CMe.sub.2 OEt MeSO HPri H Cl CMe.sub.2 OPri Ms HPri H Cl CH.sub.2 CH.sub.2 OMe Ms HPri H Cl CH.sub.2 CH.sub.2 OMe Cl HPri H Cl CH.sub.2 CH.sub.2 OMe MeS HPri H Cl CH.sub.2 CH.sub.2 OMe MeSO HPri H Cl CH.sub.2 CH.sub.2 OEt Ms HPr i H Cl CH.sub.2 CH.sub.2 OEt Cl HPri H Cl CH.sub.2 CH.sub.2 OEt MeS HPri H Cl CH.sub.2 CH.sub.2 OEt MeSO HPri H Cl CH.sub.2 CH.sub.2 OPri Ms HPri H Cl CH.sub.2 CH.sub.2 OPri Cl HPri H Cl CH.sub.2 CH.sub.2 OPri MeS HPri H Cl CH.sub.2 CH.sub.2 OPri MeSO HPri H Cl CHEtOH Ms HPri H Cl CHEtOMe Ms HPri H Cl CHEtOMe Cl HPri H Cl CHEtOMe MeS HPri H Cl CHEtOMe MeSO HPri H Cl CHEtOEt Ms HPri H Cl CHEtOPri Ms HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HPri H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HPri H Cl CHMeOCH.sub. 2 CH.sub.2 OMe Ms HPri H Cl CH.sub.2 OY8 Ms HPri H Cl CH.sub.2 OY9 Ms HPri H Cl CH.sub.2 OY10 Ms HPri H Cl CHMeOY8 Ms HPri H Cl CHMeOY9 Ms HPri H Cl CHMeOY10 Ms HPri H Cl CH.sub.2 OY13 Ms HPri H Cl CHMeOY13 Ms HPri H Cl CH.sub.2 NHMe Ms HPri H Cl CH.sub.2 NMe.sub.2 Ms HPri H Cl CH.sub.2 NEtMe Ms HPri H Cl CH.sub.2 NEt.sub.2 Ms HPri H Cl CH.sub.2Y14 Ms HPri H Cl CHMeNMe.sub.2 Ms HPri H Cl CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri H Cl CH.sub.2 OCH.sub.2 Ph Ms HPri H Cl CHMeOCH.sub.2 Ph Ms HPri H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri H Cl CH.sub.2 OCHMeCO.sub.2 Me Ms HPri H Cl CH.sub.2 CN Ms HPri H Cl CHMeCN Ms HPri H Cl CH.sub.2 SMe Ms HPri H Cl CH.sub.2 SMe Cl HPri H Cl CH.sub.2 SMe MeS HPri H Cl CH.sub.2 SMe MeSO HPri H Cl CH.sub.2 SEt Ms HPri H Cl CH.sub.2 SEt Cl HPri H Cl CH.sub.2 SEt MeS HPri H Cl CH.sub.2 SEt MeSO HPri H Cl CH.sub.2 SOMe Ms HPri H Cl CH.sub.2 SOEt Ms HPri H Cl CH.sub.2 SO.sub.2 Me Ms HPri H Cl CH.sub.2 SO.sub.2 Me Cl HPri H Cl CH.sub.2 SO.sub.2 Me MeS HPri H Cl CH.sub.2 SO.sub.2 Me MeSO HPri H Cl CH.sub.2 SO.sub.2 Et Ms HPri H Cl CH.sub.2 SO.sub.2 Et Cl HPri H Cl CH.sub.2 SO.sub.2 Et MeS HPri H Cl CH.sub.2 SO.sub.2 Et MeSO HPri H Cl CHMeSMe Ms HPri H Cl CHMeSEt Ms HPri H Cl CHMeSO.sub.2 Me Ms HPri H Cl CHMeSO.sub.2 Et Ms HPri H Cl CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri H Cl CH.sub.2 OCOMe Ms HPri H Cl CH.sub.2 OCOEt Ms HPri H Cl CHMeOCOMe Ms HPri H Cl CH.sub.2 OSO.sub.2 Me Ms HPri H Cl CH.sub.2 OSO.sub.2 Et Ms HPri H Cl CHMeOSO.sub.2 Me Ms HMe H MeO CH.sub.2 OH Ms HMe H MeO CH.sub.2 OMe Ms HMe H MeO CH.sub.2 OMe Cl HMe H MeO CH.sub.2 OMe MeS HMe H MeO CH.sub.2 OMe MeSO HMe H MeO CH.sub.2 OMe Ms Q1Me H MeO CH.sub.2 OMe MeS Q1Me H MeO CH.sub.2 OMe MeSO Q1Me H MeO CH.sub.2 OMe Ms Q2Me H MeO CH.sub.2 OMe MeS Q2Me H MeO CH.sub.2 OMe MeSO Q2Me H MeO CH.sub.2 OMe Ms Q3Me H MeO CH.sub.2 OMe MeS Q3Me H MeO CH.sub.2 OMe MeSO Q3Me H MeO CH.sub.2 OMe Ms Q4Me H MeO CH.sub.2 OMe Ms Q5Me H MeO CH.sub.2 OMe Ms Q6Me H MeO CH.sub.2 OMe Ms Q7Me H MeO CH.sub.2 OMe Ms Q8Me H MeO CH.sub.2 OMe Ms Q9Me H MeO CH.sub.2 OEt Ms HMe H MeO CH.sub.2 OEt Cl HMe H MeO CH.sub.2 OEt MeS HMe H MeO CH.sub.2 OEt MeSO HMe H MeO CH.sub.2 OEt Ms Q1Me H MeO CH.sub.2 OEt MeS Q1Me H MeO CH.sub.2 OEt MeSO Q1Me H MeO CH.sub.2 OEt Ms Q2Me H MeO CH.sub.2 OEt MeS Q2Me H MeO CH.sub.2 OEt MeSO Q2Me H MeO CH.sub.2 OEt Ms Q3Me H MeO CH.sub.2 OEt MeS Q3Me H MeO CH.sub.2 OEt MeSO Q3Me H MeO CH.sub.2 OEt Ms Q4Me H MeO CH.sub.2 OEt Ms Q5Me H MeO CH.sub.2 OEt Ms Q6Me H MeO CH.sub.2 OEt Ms Q7Me H MeO CH.sub.2 OEt Ms Q8Me H MeO CH.sub.2 OEt Ms Q9Me H MeO CH.sub.2 OPri Ms H__________________________________________________________________________
TABLE 5__________________________________________________________________________ ##STR40##A B X Y Z Q__________________________________________________________________________Me H MeO CH.sub.2 OPri Cl HMe H MeO CH.sub.2 OPri MeS HMe H MeO CH.sub.2 OPri MeSO HMe H MeO CH.sub.2 OPri Ms Q1Me H MeO CH.sub.2 OPri Ms Q2Me H MeO CH.sub.2 OPri Ms Q3Me H MeO CH.sub.2 OPrn Ms HMe H MeO CH.sub.2 OPrn Cl HMe H MeO CH.sub.2 OPrn MeS HMe H MeO CH.sub.2 OPrn MeSO HMe H MeO CH.sub.2 OCHCH.sub.2 Ms HMe H MeO CH.sub.2 OCHCH.sub.2 Cl HMe H MeO CH.sub.2 OCHCH.sub.2 MeS HMe H MeO CH.sub. 2 OCHCH.sub.2 MeSO HMe H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HMe H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HMe H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HMe H MeO CH.sub.2 OCH.sub.2 CCH Ms HMe H MeO CH.sub.2 OCH.sub.2 CCH Cl HMe H MeO CH.sub.2 OCH.sub.2 CCH MeS HMe H MeO CH.sub.2 OCH.sub.2 CCH MeSO HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeSO HMe H MeO CH.sub.2 OY5 Ms HMe H MeO CHMeOH Ms HMe H MeO CHMeOMe Ms HMe H MeO CHMeOMe Cl HMe H MeO CHMeOMe MeS HMe H MeO CHMeOMe MeSO HMe H MeO CHMeOMe Ms Q1Me H MeO CHMeOMe Ms Q2Me H MeO CHMeOMe Ms Q3Me H MeO CHMeOEt Ms HMe H MeO CHMeOEt Cl HMe H MeO CHMeOEt MeS HMe H MeO CHMeOEt MeSO HMe H MeO CHMeOEt Ms Q1Me H MeO CHMeOEt Ms Q2Me H MeO CHMeOEt Ms Q3Me H MeO CHMeOPri Ms HMe H MeO CHMeOPri Cl HMe H MeO CHMeOPri MeS HMe H MeO CHMeOPri MeSO HMe H MeO CHMeOPrn Ms HMe H MeO CHMeOCHCH.sub.2 Ms HMe H MeO CHMeOCHCH.sub.2 Ms HMe H MeO CHMeOCH.sub.2 CHCH.sub.2 Ms HMe H MeO CHMeOCH.sub.2 CCH Ms HMe H MeO CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe H MeO CHMeOY5 Ms HMe H MeO CMe.sub.2 OH Ms HMe H MeO CMe.sub.2 OMe Ms HMe H MeO CMe.sub.2 OMe Cl HMe H MeO CMe.sub.2 OMe MeS HMe H MeO CMe.sub.2 OMe MeSO HMe H MeO CMe.sub.2 OEt Ms HMe H MeO CMe.sub.2 OEt Cl HMe H MeO CMe.sub.2 OEt MeS HMe H MeO CMe.sub.2 OEt MeSO HMe H MeO CMe.sub.2 OPri Ms HMe H MeO CH.sub.2 CH.sub.2 OMe Ms HMe H MeO CH.sub.2 CH.sub.2 OMe Cl HMe H MeO CH.sub.2 CH.sub.2 OMe MeS HMe H MeO CH.sub.2 CH.sub.2 OMe MeSO HMe H MeO CH.sub.2 CH.sub.2 OEt Ms HMe H MeO CH.sub.2 CH.sub.2 OEt Cl HMe H MeO CH.sub.2 CH.sub.2 OEt MeS HMe H MeO CH.sub.2 CH.sub.2 OEt MeSO HMe H MeO CH.sub.2 CH.sub.2 OPri Ms HMe H MeO CH.sub.2 CH.sub.2 OPri Cl HMe H MeO CH.sub.2 CH.sub.2 OPri MeS HMe H MeO CH.sub.2 CH.sub.2 OPri MeSO HMe H MeO CHEtOH Ms HMe H MeO CHEtOMe Ms HMe H MeO CHEtOMe Cl HMe H MeO CHEtOMe MeS HMe H MeO CHEtOMe MeSO HMe H MeO CHEtOEt Ms HMe H MeO CHEtOPri Ms HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HMe H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HMe H MeO CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe H MeO CH.sub.2 OY8 Ms HMe H MeO CH.sub.2 OY9 Ms HMe H MeO CH.sub.2 OY10 Ms HMe H MeO CHMeOY8 Ms HMe H MeO CHMeOY9 Ms HMe H MeO CHMeOY10 Ms HMe H MeO CH.sub.2 OY13 Ms HMe H MeO CHMeOY13 Ms HMe H MeO CH.sub.2 NHMe Ms HMe H MeO CH.sub.2 NMe.sub.2 Ms HMe H MeO CH.sub.2 NEtMe Ms HMe H MeO CH.sub.2 NEt.sub.2 Ms HMe H MeO CH.sub.2Y14 Ms HMe H MeO CHMeNMe.sub.2 Ms HMe H MeO CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe H MeO CH.sub.2 OCH.sub.2 Ph Ms HMe H MeO CHMeOCH.sub.2 Ph Ms HMe H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe H MeO CH.sub.2 OCHMeCO.sub.2 Me Ms HMe H MeO CH.sub.2 CN Ms HMe H MeO CHMeCN Ms HMe H MeO CH.sub.2 SMe Ms HMe H MeO CH.sub.2 SMe Cl HMe H MeO CH.sub.2 SMe MeS HMe H MeO CH.sub.2 SMe MeSO HMe H MeO CH.sub.2 SEt Ms HMe H MeO CH.sub.2 SEt Cl HMe H MeO CH.sub.2 SEt MeS HMe H MeO CH.sub.2 SEt MeSO HMe H MeO CH.sub.2 SOMe Ms HMe H MeO CH.sub.2 SOEt Ms HMe H MeO CH.sub.2 SO.sub.2 Me Ms HMe H MeO CH.sub.2 SO.sub.2 Me Cl HMe H MeO CH.sub.2 SO.sub.2 Me MeS HMe H MeO CH.sub.2 SO.sub.2 Me MeSO HMe H MeO CH.sub.2 SO.sub.2 Et Ms HMe H MeO CH.sub.2 SO.sub.2 Et Cl HMe H MeO CH.sub.2 SO.sub.2 Et MeS HMe H MeO CH.sub.2 SO.sub.2 Et MeSO HMe H MeO CHMeSMe Ms HMe H MeO CHMeSEt Ms HMe H MeO CHMeSO.sub.2 Me Ms HMe H MeO CHMeSO.sub.2 Et Ms HMe H MeO CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe H MeO CH.sub.2 OCOMe Ms HMe H MeO CH.sub.2 OCOEt Ms HMe H MeO CHMeOCOMe Ms HMe H MeO CH.sub.2 OSO.sub.2 Me Ms HMe H MeO CH.sub.2 OSO.sub.2 Et Ms HMe H MeO CHMeOSO.sub.2 Me Ms HEt H MeO CH.sub.2 OH Ms HEt H MeO CH.sub.2 OMe Ms HEt H MeO CH.sub.2 OMe Cl HEt H MeO CH.sub.2 OMe MeS HEt H MeO CH.sub.2 OMe MeSO HEt H MeO CH.sub.2 OMe Ms Q1Et H MeO CH.sub.2 OMe MeS Q1Et H MeO CH.sub.2 OMe MeSO Q1Et H MeO CH.sub.2 OMe Ms Q2Et H MeO CH.sub.2 OMe MeS Q2Et H MeO CH.sub.2 OMe MeSO Q2Et H MeO CH.sub.2 OMe Ms Q3Et H MeO CH.sub.2 OMe MeS Q3Et H MeO CH.sub.2 OMe MeSO Q3Et H MeO CH.sub.2 OMe Ms Q4Et H MeO CH.sub.2 OMe Ms Q5Et H MeO CH.sub.2 OMe Ms Q6Et H MeO CH.sub.2 OMe Ms Q7Et H MeO CH.sub.2 OMe Ms Q8Et H MeO CH.sub.2 OMe Ms Q9Et H MeO CH.sub.2 OEt Ms HEt H MeO CH.sub.2 OEt Cl HEt H MeO CH.sub.2 OEt MeS HEt H MeO CH.sub.2 OEt MeSO HEt H MeO CH.sub.2 OEt Ms Q1Et H MeO CH.sub.2 OEt MeS Q1Et H MeO CH.sub.2 OEt MeSO Q1Et H MeO CH.sub.2 OEt Ms Q2Et H MeO CH.sub.2 OEt MeS Q2Et H MeO CH.sub.2 OEt MeSO Q2Et H MeO CH.sub.2 OEt Ms Q3Et H MeO CH.sub.2 OEt MeS Q3Et H MeO CH.sub.2 OEt MeSO Q3Et H MeO CH.sub.2 OEt Ms Q4Et H MeO CH.sub.2 OEt Ms Q5Et H MeO CH.sub.2 OEt Ms Q6Et H MeO CH.sub.2 OEt MS Q7Et H MeO CH.sub.2 OEt Ms Q8Et H MeO CH.sub.2 OEt Ms Q9Et H MeO CH.sub.2 OPri Ms HEt H MeO CH.sub.2 OPri Cl HEt H MeO CH.sub.2 OPri MeS HEt H MeO CH.sub.2 OPri MeSO HEt H MeO CH.sub.2 OPri Ms Q1Et H MeO CH.sub.2 OPri Ms Q2Et H MeO CH.sub.2 OPri Ms Q3Et H MeO CH.sub.2 OPrn Ms HEt H MeO CH.sub.2 OPrn Cl HEt H MeO CH.sub.2 OPrn MeS HEt H MeO CH.sub.2 OPrn MeSO HEt H MeO CH.sub.2 OCHCH.sub.2 Ms HEt H MeO CH.sub.2 OCHCH.sub.2 Cl HEt H MeO CH.sub.2 OCHCH.sub.2 MeS HEt H MeO CH.sub.2 OCHCH.sub.2 MeSO HEt H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HEt H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HEt H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HEt H MeO CH.sub.2 OCH.sub.2 CCH Ms HEt H MeO CH.sub.2 OCH.sub.2 CCH Cl HEt H MeO CH.sub.2 OCH.sub.2 CCH MeS HEt H MeO CH.sub.2 OCH.sub.2 CCH MeSO HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeSO HEt H MeO CH.sub.2 OY5 Ms HEt H MeO CHMeOH Ms HEt H MeO CHMeOMe Ms HEt H MeO CHMeOMe Cl HEt H MeO CHMeOMe MeS HEt H MeO CHMeOMe MeSO HEt H MeO CHMeOMe Ms Q1Et H MeO CHMeOMe Ms Q2Et H MeO CHMeOMe Ms Q3Et H MeO CHMeOEt Ms HEt H MeO CHMeOEt Cl HEt H MeO CHMeOEt MeS HEt H MeO CHMeOEt MeSO HEt H MeO CHMeOEt Ms Q1Et H MeO CHMeOEt Ms Q2Et H MeO CHMeOEt Ms Q3Et H MeO CHMeOPri Ms HEt H MeO CHMeOPri Cl HEt H MeO CHMeOPri MeS HEt H MeO CHMeOPri MeSO HEt H MeO CHMeOPrn Ms HEt H MeO CHMeOCHCH.sub.2 Ms HEt H MeO CHMeOCHCH.sub.2 Ms HEt H MeO CHMeOCH.sub.2 CHCH.sub.2 Ms HEt H MeO CHMeOCH.sub.2 CCH Ms HEt H MeO CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt H MeO CHMeOY5 Ms HEt H MeO CMe.sub.2 OH Ms HEt H MeO CMe.sub.2 OMe Ms HEt H MeO CMe.sub.2 OMe Cl HEt H MeO CMe.sub.2 OMe MeS HEt H MeO CMe.sub.2 OMe MeSO HEt H MeO CMe.sub.2 OEt Ms HEt H MeO CMe.sub.2 OEt Cl HEt H MeO CMe.sub.2 OEt MeS HEt H MeO CMe.sub.2 OEt MeSO HEt H MeO CMe.sub.2 OPri Ms HEt H MeO CH.sub.2 CH.sub.2 OMe Ms HEt H MeO CH.sub.2 CH.sub.2 OMe Cl HEt H MeO CH.sub.2 CH.sub.2 OMe MeS HEt H MeO CH.sub.2 CH.sub.2 OMe MeSO HEt H MeO CH.sub.2 CH.sub.2 OEt Ms HEt H MeO CH.sub.2 CH.sub.2 OEt Cl HEt H MeO CH.sub.2 CH.sub.2 OEt MeS HEt H MeO CH.sub.2 CH.sub.2 OEt MeSO HEt H MeO CH.sub.2 CH.sub.2 OPri Ms HEt H MeO CH.sub.2 CH.sub.2 OPri Cl HEt H MeO CH.sub.2 CH.sub.2 OPri MeS HEt H MeO CH.sub.2 CH.sub.2 OPri MeSO HEt H MeO CHEtOH Ms HEt H MeO CHEtOMe Ms HEt H MeO CHEtOMe Cl HEt H MeO CHEtOMe MeS HEt H MeO CHEtOMe MeSO HEt H MeO CHEtOEt Ms HEt H MeO CHEtOPri Ms HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HEt H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HEt H MeO CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt H MeO CH.sub.2 OY8 Ms HEt H MeO CH.sub.2 OY9 Ms HEt H MeO CH.sub.2 OY10 Ms HEt H MeO CHMeOY8 Ms HEt H MeO CHMeOY9 Ms HEt H MeO CHMeOY10 Ms HEt H MeO CH.sub.2 OY13 Ms HEt H MeO CHMeOY13 Ms HEt H MeO CH.sub.2 NHMe Ms HEt H MeO CH.sub.2 NMe.sub.2 Ms HEt H MeO CH.sub.2 NEtMe Ms HEt H MeO CH.sub.2 NEt.sub.2 Ms HEt H MeO CH.sub.2Y14 Ms HEt H MeO CHMeNMe.sub.2 Ms HEt H MeO CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt H MeO CH.sub.2 OCH.sub.2 Ph Ms HEt H MeO CHMeOCH.sub.2 Ph Ms HEt H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt H MeO CH.sub.2 OCHMeCO.sub.2 Me Ms HEt H MeO CH.sub.2 CN Ms HEt H MeO CHMeCN Ms HEt H MeO CH.sub.2 SMe Ms HEt H MeO CH.sub.2 SMe Cl HEt H MeO CH.sub.2 SMe MeS HEt H MeO CH.sub.2 SMe MeSO HEt H MeO CH.sub.2 SEt Ms HEt H MeO CH.sub.2 SEt Cl HEt H MeO CH.sub.2 SEt MeS HEt H MeO CH.sub.2 SEt MeSO HEt H MeO CH.sub.2 SOMe Ms HEt H MeO CH.sub.2 SOEt Ms HEt H MeO CH.sub.2 SO.sub.2 Me Ms HEt H MeO CH.sub.2 SO.sub.2 Me Cl HEt H MeO CH.sub.2 SO.sub.2 Me MeS HEt H MeO CH.sub.2 SO.sub.2 Me MeSO HEt H MeO CH.sub.2 SO.sub.2 Et Ms HEt H MeO CH.sub.2 SO.sub.2 Et Cl HEt H MeO CH.sub.2 SO.sub.2 Et MeS HEt H MeO CH.sub.2 SO.sub.2 Et MeSO HEt H MeO CHMeSMe Ms HEt H MeO CHMeSEt Ms HEt H MeO CHMeSO.sub.2 Me Ms HEt H MeO CHMeSO.sub.2 Et Ms HEt H MeO CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt H MeO CH.sub.2 OCOMe Ms HEt H MeO CH.sub.2 OCOEt Ms HEt H MeO CHMeOCOMe Ms HEt H MeO CH.sub.2 OSO.sub.2 Me Ms HEt H MeO CH.sub.2 OSO.sub.2 Et Ms HEt H MeO CHMeOSO.sub.2 Me Ms HPri H MeO CH.sub.2 OH Ms HPri H MeO CH.sub.2 OMe Ms HPri H MeO CH.sub.2 OMe Cl HPri H MeO CH.sub.2 OMe MeS HPri H MeO CH.sub.2 OMe MeSO HPri H MeO CH.sub.2 OMe Ms Q1Pri H MeO CH.sub.2 OMe MeS Q1Pri H MeO CH.sub.2 OMe MeSO Q1Pri H MeO CH.sub.2 OMe Ms Q2Pri H MeO CH.sub.2 OMe MeS Q2Pri H MeO CH.sub.2 OMe MeSO Q2Pri H MeO CH.sub.2 OMe Ms Q3Pri H MeO CH.sub.2 OMe MeS Q3Pri H MeO CH.sub.2 OMe MeSO Q3Pri H MeO CH.sub.2 OMe Ms Q4Pri H MeO CH.sub.2 OMe Ms Q5Pri H MeO CH.sub.2 OMe Ms Q6Pri H MeO CH.sub.2 OMe Ms Q7Pri H MeO CH.sub.2 OMe Ms Q8Pri H MeO CH.sub.2 OMe Ms Q9Pri H MeO CH.sub.2 OEt Ms HPri H MeO CH.sub.2 OEt Cl HPri H MeO CH.sub.2 OEt MeS HPri H MeO CH.sub.2 OEt MeSO HPri H MeO CH.sub.2 OEt Ms Q1Pri H MeO CH.sub.2 OEt MeS Q1Pri H MeO CH.sub.2 OEt MeSO Q1Pri H MeO CH.sub.2 OEt Ms Q2Pri H MeO CH.sub.2 OEt MeS Q2Pri H MeO CH.sub.2 OEt MeSO Q2Pri H MeO CH.sub.2 OEt Ms Q3Pri H MeO CH.sub.2 OEt MeS Q3Pri H MeO CH.sub.2 OEt MeSO Q3Pri H MeO CH.sub.2 OEt Ms Q4Pri H MeO CH.sub.2 OEt Ms Q5Pri H MeO CH.sub.2 OEt Ms Q6Pri H MeO CH.sub.2 OEt Ms Q7Pri H MeO CH.sub.2 OEt Ms Q8Pri H MeO CH.sub.2 OEt Ms Q9Pri H MeO CH.sub.2 OPri Ms HPri H MeO CH.sub.2 OPri Cl HPri H MeO CH.sub.2 OPri MeS HPri H MeO CH.sub.2 OPri MeSO HPri H MeO CH.sub.2 OPri Ms Q1Pri H MeO CH.sub.2 OPri Ms Q2Pri H MeO CH.sub.2 OPri Ms Q3Pri H MeO CH.sub.2 OPrn Ms HPri H MeO CH.sub.2 OPrn Cl HPri H MeO CH.sub.2 OPrn MeS HPri H MeO CH.sub.2 OPrn MeSO HPri H MeO CH.sub.2 OCHCH.sub.2 Ms HPri H MeO CH.sub.2 OCHCH.sub.2 Cl HPri H MeO CH.sub.2 OCHCH.sub.2 MeS HPri H MeO CH.sub.2 OCHCH.sub.2 MeSO HPri H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Cl HPri H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 MeS HPri H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 MeSO HPri H MeO CH.sub.2 OCH.sub.2 CCH Ms HPri H MeO CH.sub.2 OCH.sub.2 CCH Cl HPri H MeO CH.sub.2 OCH.sub.2 CCH MeS HPri H MeO CH.sub.2 OCH.sub.2 CCH MeSO HPri H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Cl HPri H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl MeS HPri H MeO CH.sub. 2 OCH.sub.2 CH.sub.2 Cl MeSO HPri H MeO CH.sub.2 OY5 Ms HPri H MeO CHMeOH Ms HPri H MeO CHMeOMe Ms HPri H MeO CHMeOMe Cl HPri H MeO CHMeOMe MeS HPri H MeO CHMeOMe MeSO HPri H MeO CHMeOMe Ms Q1Pri H MeO CHMeOMe Ms Q2Pri H MeO CHMeOMe Ms Q3Pri H MeO CHMeOEt Ms HPri H MeO CHMeOEt Cl HPri H MeO CHMeOEt MeS HPri H MeO CHMeOEt MeSO HPri H MeO CHMeOEt Ms Q1Pri H MeO CHMeOEt Ms Q2Pri H MeO CHMeOEt Ms Q3Pri H MeO CHMeOPri Ms HPri H MeO CHMeOPri Cl HPri H MeO CHMeOPri MeS HPri H MeO CHMeOPri MeSO HPri H MeO CHMeOPrn Ms HPri H MeO CHMeOCHCH.sub.2 Ms HPri H MeO CHMeOCHCH.sub.2 Ms HPri H MeO CHMeOCH.sub.2 CHCH.sub.2 Ms HPri H MeO CHMeOCH.sub.2 C CH Ms HPri H MeO CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri H MeO CHMeOY5 Ms HPri H MeO CMe.sub.2 OH Ms HPri H MeO CMe.sub.2 OMe Ms HPri H MeO CMe.sub.2 OMe Cl HPri H MeO CMe.sub.2 OMe MeS HPri H MeO CMe.sub.2 OMe MeSO HPri H MeO CMe.sub.2 OEt Ms HPri H MeO CMe.sub.2 OEt Cl HPri H MeO CMe.sub.2 OEt MeS HPri H MeO CMe.sub.2 OEt MeSO HPri H MeO CMe.sub.2 OPri Ms HPri H MeO CH.sub.2 CH.sub.2 OMe Ms HPri H MeO CH.sub.2 CH.sub.2 OMe Cl HPri H MeO CH.sub.2 CH.sub.2 OMe MeS HPri H MeO CH.sub.2 CH.sub.2 OMe MeSO HPri H MeO CH.sub.2 CH.sub.2 OEt Ms HPri H MeO CH.sub.2 CH.sub.2 OEt Cl HPri H MeO CH.sub.2 CH.sub.2 OEt MeS HPri H MeO CH.sub.2 CH.sub.2 OEt MeSO HPri H MeO CH.sub.2 CH.sub.2 OPri Ms HPri H MeO CH.sub.2 CH.sub.2 OPri Cl HPri H MeO CH.sub.2 CH.sub.2 OPri MeS HPri H MeO CH.sub.2 CH.sub.2 OPri MeSO HPri H MeO CHEtOH Ms HPri H MeO CHEtOMe Ms HPri H MeO CHEtOMe Cl HPri H MeO CHEtOMe MeS HPri H MeO CHEtOMe MeSO HPri H MeO CHEtOEt Ms HPri H MeO CHEtOPri Ms HPri H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HPri H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HPri H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HPri H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HPri H MeO CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri H MeO CH.sub.2 OY8 Ms HPri H MeO CH.sub.2 O Y9 Ms HPri H MeO CH.sub.2 OY10 Ms HPri H MeO CHMeOY8 Ms HPri H MeO CHMeOY9 Ms HPri H MeO CHMeOY10 Ms HPri H MeO CH.sub.2 OY13 Ms HPri H MeO CHMeOY13 Ms HPri H MeO CH.sub.2 NHMe Ms HPri H MeO CH.sub.2 NMe.sub.2 Ms HPri H MeO CH.sub.2 NEtMe Ms HPri H MeO CH.sub.2 NEt.sub.2 Ms HPri H MeO CH.sub.2Y14 Ms HPri H MeO CHMeNMe.sub.2 Ms HPri H MeO CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri H MeO CH.sub.2 OCH.sub.2 Ph Ms HPri H MeO CHMeOCH.sub.2 Ph Ms HPri H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri H MeO CH.sub.2 OCHMeCO.sub.2 Me Ms HPri H MeO CH.sub.2 CN Ms HPri H MeO CHMeCN Ms HPri H MeO CH.sub. 2 SMe Ms HPri H MeO CH.sub.2 SMe Cl HPri H MeO CH.sub.2 SMe MeS HPri H MeO CH.sub.2 SMe MeSO HPri H MeO CH.sub.2 SEt Ms HPri H MeO CH.sub.2 SEt Cl HPri H MeO CH.sub.2 SEt MeS HPri H MeO CH.sub.2 SEt MeSO HPri H MeO CH.sub.2 SOMe Ms HPri H MeO CH.sub.2 SOEt Ms HPri H MeO CH.sub.2 SO.sub.2 Me Ms HPri H MeO CH.sub.2 SO.sub.2 Me Cl HPri H MeO CH.sub.2 SO.sub.2 Me MeS HPri H MeO CH.sub.2 SO.sub.2 Me MeSO HPri H MeO CH.sub.2 SO.sub.2 Et Ms HPri H MeO CH.sub.2 SO.sub.2 Et Cl HPri H MeO CH.sub.2 SO.sub.2 Et MeS HPri H MeO CH.sub.2 SO.sub.2 Et MeSO HPri H MeO CHMeSMe Ms HPri H MeO CHMeSEt Ms HPri H MeO CHMeSO.sub.2 Me Ms HPri H MeO CHMeSO.sub.2 Et Ms HPri H MeO CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri H MeO CH.sub.2 OCOMe Ms HPri H MeO CH.sub.2 OCOEt Ms HPri H MeO CHMeOCOMe Ms HPri H MeO CH.sub.2 OSO.sub.2 Me Ms HPri H MeO CH.sub.2 OSO.sub.2 Et Ms HPri H MeO CHMeOSO.sub.2 Me Ms HMe Me Me CH.sub.2 OH Ms HMe Me Me CH.sub.2 OMe Ms HMe Me Me CH.sub.2 OMe Cl HMe Me Me CH.sub.2 OMe MeS HMe Me Me CH.sub.2 OMe MeSO HMe Me Me CH.sub.2 OMe Ms Q1Me Me Me CH.sub.2 OMe Cl Q1Me Me Me CH.sub.2 OMe MeS Q1Me Me Me CH.sub.2 OMe MeSO Q2Me Me Me CH.sub.2 OMe MeS Q2Me Me Me CH.sub.2 OMe MeSO Q2Me Me Me CH.sub.2 OMe Ms Q3Me Me Me CH.sub.2 OMe MeS Q3Me Me Me CH.sub.2 OMe MeSO Q3Me Me Me CH.sub.2 OEt Ms HMe Me Me CH.sub.2 OEt Cl HMe Me Me CH.sub.2 OEt MeS HMe Me Me CH.sub.2 OEt MeSO HMe Me Me CH.sub.2 OEt Ms Q1Me Me Me CH.sub.2 OEt MeS Q1Me Me Me CH.sub.2 OEt MeSO Q1Me Me Me CH.sub.2 OEt Ms Q2Me Me Me CH.sub.2 OEt MeS Q2Me Me Me CH.sub.2 OEt MeSO Q2Me Me Me CH.sub.2 OEt Ms Q3Me Me Me CH.sub.2 OEt MeS Q3Me Me Me CH.sub.2 OEt MeSO Q3Me Me Me CH.sub.2 OPri Ms HMe Me Me CH.sub.2 OPri Cl HMe Me Me CH.sub.2 OPri MeS HMe Me Me CH.sub.2 OPri MeSO HMe Me Me CH.sub.2 OPri Ms Q1Me Me Me CH.sub.2 OPri Ms Q2Me Me Me CH.sub.2 OPri Ms Q3Me Me Me CH.sub.2 OPrn Ms HMe Me Me CH.sub.2 OCHCH.sub.2 Ms HMe Me Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe Me Me CH.sub.2 OCH.sub.2 C CH Ms HMe Me Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe Me Me CH.sub.2 OY5 Ms HMe Me Me CHMeOH Ms HMe Me Me CHMeOMe Ms HMe Me Me CHMeOMe Cl HMe Me Me CHMeOMe MeS HMe Me Me CHMeOMe MeSO HMe Me Me CHMeOMe Ms Q1Me Me Me CHMeOMe Ms Q2Me Me Me CHMeOMe Ms Q3Me Me Me CHMeOEt Ms HMe Me Me CHMeOEt Cl HMe Me Me CHMeOEt MeS HMe Me Me CHMeOEt MeSO HMe Me Me CHMeOEt Ms Q1Me Me Me CHMeOEt Ms Q2Me Me Me CHMeOEt Ms Q3Me Me Me CHMeOPri Ms HMe Me Me CHMeOPri Cl HMe Me Me CHMeOPri MeS HMe Me Me CHMeOPri MeSO HMe Me Me CHMeOPrn Ms HMe Me Me CHMeOCHCH.sub.2 Ms HMe Me Me CHMeOCHCH.sub.2 Ms HMe Me Me CHMeOCH.sub.2 CHCH.sub.2 Ms HMe Me Me CHMeOCH.sub.2 CCH Ms HMe Me Me CHMeOCH.sub.2 CH.sub. 2 Cl Ms HMe Me Me CHMeOY5 Ms HMe Me Me CMe.sub.2 OH Ms HMe Me Me CMe.sub.2 OMe Ms HMe Me Me CMe.sub.2 OEt Ms HMe Me Me CMe.sub.2 OPri Ms HMe Me Me CH.sub.2 CH.sub.2 OMe Ms HMe Me Me CH.sub.2 CH.sub.2 OEt Ms HMe Me Me CH.sub.2 CH.sub.2 OPri Ms HMe Me Me CHEtOH Ms HMe Me Me CHEtOMe Ms HMe Me Me CHEtOMe Cl HMe Me Me CHEtOMe MeS HMe Me Me CHEtOMe MeSO HMe Me Me CHEtOEt Ms HMe Me Me CHEtOPri Ms H
TABLE 5__________________________________________________________________________ ##STR41##A B X Y Z Q__________________________________________________________________________Me Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HMe Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HMe Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HMe Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HMe Me Me CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe Me Me CH.sub.2 OY8 Ms HMe Me Me CH.sub.2 OY9 Ms HMe Me Me CH.sub.2 OY10 Ms HMe Me Me CHMeOY8 Ms HMe Me Me CHMeOY9 Ms HMe Me Me CHMeOY10 Ms HMe Me Me CH.sub.2 O Y13 Ms HMe Me Me CHMeOY13 Ms HMe Me Me CH.sub.2 NMe.sub.2 Ms HMe Me Me CH.sub.2Y14 Ms HMe Me Me CHMeNMe.sub.2 Ms HMe Me Me CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe Me Me CH.sub.2 OCH.sub.2 Ph Ms HMe Me Me CHMeOCH.sub.2 Ph Ms HMe Me Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe Me Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe Me Me CH.sub.2 OCHMeCO.sub.2 Me Ms HMe Me Me CH.sub.2 CN Ms HMe Me Me CHMeCN Ms HMe Me Me CH.sub.2 SMe Ms HMe Me Me CH.sub.2 SMe Cl HMe Me Me CH.sub.2 SMe MeS HMe Me Me CH.sub.2 SMe MeSO HMe Me Me CH.sub.2 SEt Ms HMe Me Me CH.sub.2 SEt Cl HMe Me Me CH.sub.2 SEt MeS HMe Me Me CH.sub.2 SEt MeSO HMe Me Me CH.sub.2 SOMe Ms HMe Me Me CH.sub.2 SOEt Ms HMe Me Me CH.sub.2 SO.sub.2 Me Ms HMe Me Me CH.sub.2 SO.sub.2 Me Cl HMe Me Me CH.sub.2 SO.sub.2 Me MeS HMe Me Me CH.sub.2 SO.sub.2 Me MeSO HMe Me Me CH.sub.2 SO.sub.2 Et Ms HMe Me Me CH.sub.2 SO.sub.2 Et CL HMe Me Me CH.sub.2 SO.sub.2 Et MeS HMe Me Me CH.sub.2 SO.sub.2 Et MeSO HMe Me Me CHMeSMe Ms HMe Me Me CHMeSEt Ms HMe Me Me CHMeSO.sub.2 Me Ms HMe Me Me CHMeSO.sub.2 Et Ms HMe Me Me CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe Me Me CH.sub.2 OCOMe Ms HMe Me Me CH.sub.2 OCOEt Ms HMe Me Me CHMeOCOMe Ms HMe Me Me CH.sub.2 OSO.sub.2 Me Ms HMe Me Me CH.sub.2 OSO.sub.2 Et Ms HMe Me Me CHMeOSO.sub.2 Me Ms HEt Me Me CH.sub.2 OH Ms HEt Me Me CH.sub.2 OMe Ms HEt Me Me CH.sub.2 OMe Cl HEt Me Me CH.sub.2 OMe MeS HEt Me Me CH.sub.2 OMe MeSO HEt Me Me CH.sub.2 OMe Ms Q1Et Me Me CH.sub.2 OMe Cl Q1Et Me Me CH.sub.2 OMe MeS Q1Et Me Me CH.sub.2 OMe MeSO Q2Et Me Me CH.sub.2 OMe MeS Q2Et Me Me CH.sub.2 OMe MeSO Q2Et Me Me CH.sub.2 OMe Ms Q3Et Me Me CH.sub.2 OMe MeS Q3Et Me Me CH.sub.2 OMe MeSO Q3Et Me Me CH.sub.2 OEt Ms HEt Me Me CH.sub.2 OEt Cl HEt Me Me CH.sub.2 OEt MeS HEt Me Me CH.sub.2 OEt MeSO HEt Me Me CH.sub.2 OEt Ms Q1Et Me Me CH.sub.2 OEt MeS Q1Et Me Me CH.sub.2 OEt MeSO Q1Et Me Me CH.sub.2 OEt Ms Q2Et Me Me CH.sub.2 OEt MeS Q2Et Me Me CH.sub.2 OEt MeSO Q2Et Me Me CH.sub.2 OEt Ms Q3Et Me Me CH.sub.2 OEt MeS Q3Et Me Me CH.sub.2 OEt MeSO Q3Et Me Me CH.sub.2 OEt MeSO Q3Et Me Me CH.sub.2 OPri Ms HEt Me Me CH.sub.2 OPr i Cl HEt Me Me CH.sub.2 OPri MeS HEt Me Me CH.sub.2 OPri MeSO HEt Me Me CH.sub.2 OPri Ms Q1Et Me Me CH.sub.2 OPri Ms Q2Et Me Me CH.sub.2 OPri Ms Q3Et Me Me CH.sub.2 OPrn Ms HEt Me Me CH.sub.2 OCHCH.sub.2 Ms HEt Me Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt Me Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt Me Me CH.sub.2 OY5 Ms HEt Me Me CHMeOH Ms HEt Me Me CHMeOMe Ms HEt Me Me CHMeOMe Cl HEt Me Me CHMeOMe MeS HEt Me Me CHMeOMe MeSO HEt Me Me CHMeOMe Ms Q1Et Me Me CHMeOMe Ms Q2Et Me Me CHMeOMe Ms Q3Et Me Me CHMeOEt Ms HEt Me Me CHMeOEt Cl HEt Me Me CHMeOEt MeS HEt Me Me CHMeOEt MeSO HEt Me Me CHMeOEt Ms Q1Et Me Me CHMeOEt Ms Q2Et Me Me CHMeOEt Ms Q3Et Me Me CHMeOPri Ms HEt Me Me CHMeOPri Cl HEt Me Me CHMeOPri MeS HEt Me Me CHMeOPri MeSO HEt Me Me CHMeOPrn Ms HEt Me Me CHMeOCHCH.sub.2 Ms HEt Me Me CHMeOCHCH.sub.2 Ms HEt Me Me CHMeOCH.sub.2 CHCH.sub.2 Ms HEt Me Me CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt Me Me CHMeOY5 Ms HEt Me Me CMe.sub.2 OH Ms HEt Me Me CMe.sub.2 OMe Ms HEt Me Me CMe.sub.2 OEt Ms HEt Me Me CMe.sub.2 OPri Ms HEt Me Me CH.sub.2 CH.sub.2 OMe Ms HEt Me Me CH.sub.2 CH.sub.2 OEt Ms HEt Me Me CH.sub.2 CH.sub.2 OPri Ms HEt Me Me CHEtOH Ms HEt Me Me CHEtOMe Ms HEt Me Me CHEtOMe Cl HEt Me Me CHEtOMe MeS HEt Me Me CHEtOMe MeSO HEt Me Me CHEtOEt Ms HEt Me Me CHEtOPri Ms HEt Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HEt Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HEt Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HEt Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HEt Me Me CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt Me Me CH.sub.2 OY8 Ms HEt Me Me CH.sub.2 OY9 Ms HEt Me Me CH.sub.2 OY10 Ms HEt Me Me CHMeOY8 Ms HEt Me Me CHMeOY9 Ms HEt Me Me CHMeOYJ10 Ms HEt Me Me CH.sub.2 OY13 Ms HEt Me Me CHMeOY13 Ms HEt Me Me CH.sub.2 NMe.sub.2 Ms HEt Me Me CH.sub.2Y14 Ms HEt Me Me CHMeNMe.sub.2 Ms HEt Me Me CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt Me Me CH.sub.2 OCH.sub.2 Ph Ms HEt Me Me CHMeOCH.sub.2 Ph Ms HEt Me Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Me Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt Me Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt Me Me CH.sub.2 OCHMeCO.sub.2 Me Ms HEt Me Me CH.sub.2 CN Ms HEt Me Me CHMeCN Ms HEt Me Me CH.sub.2 SMe Ms HEt Me Me CH.sub.2 SMe Cl HEt Me Me CH.sub.2 SMe MeS HEt Me Me CH.sub.2 SMe MeSO HEt Me Me CH.sub.2 SEt Ms HEt Me Me CH.sub.2 SEt Cl HEt Me Me CH.sub.2 SEt MeS HEt Me Me CH.sub.2 SEt MeSO HEt Me Me CH.sub.2 SOMe Ms HEt Me Me CH.sub.2 SOEt Ms HEt Me Me CH.sub.2 SO.sub.2 Me Ms HEt Me Me CH.sub.2 SO.sub.2 Me Cl HEt Me Me CH.sub.2 SO.sub.2 Me MeS HEt Me Me CH.sub.2 SO.sub.2 Me MeSO HEt Me Me CH.sub.2 SO.sub.2 Et Ms HEt Me Me CH.sub.2 SO.sub.2 Et Cl HEt Me Me CH.sub.2 SO.sub.2 Et MeS HEt Me Me CH.sub.2 SO.sub.2 Et MeSO HEt Me Me CHMeSMe Ms HEt Me Me CHMeSEt Ms HEt Me Me CHMeSO.sub.2 Me Ms HEt Me Me CHMeSO.sub.2 Et Ms HEt Me Me CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt Me Me CH.sub.2 OCOMe Ms HEt Me Me CH.sub.2 OCOEt Ms HEt Me Me CHMeOCOMe Ms HEt Me Me CH.sub.2 OSO.sub.2 Me Ms HEt Me Me CH.sub.2 OSO.sub.2 Et Ms HEt Me Me CHMeOSO.sub.2 Me Ms HPri Me Me CH.sub.2 OH Ms HPri Me Me CH.sub.2 OMe Ms HPri Me Me CH.sub.2 OMe Cl HPri Me Me CH.sub.2 OMe MeS HPri Me Me CH.sub.2 OMe MeSO HPri Me Me CH.sub.2 OMe Ms Q1Pri Me Me CH.sub.2 OMe Cl Q1Pri Me Me CH.sub.2 OMe MeS Q1Pri Me Me CH.sub.2 OMe MeSO Q2Pri Me Me CH.sub.2 OMe MeS Q2Pri Me Me CH.sub.2 OMe MeSO Q2Pri Me Me CH.sub.2 OMe Ms Q3Pri Me Me CH.sub.2 OMe MeS Q3Pri Me Me CH.sub.2 OMe MeSO Q3Pri Me Me CH.sub.2 OEt Ms HPri Me Me CH.sub.2 OEt Cl HPri Me Me CH.sub.2 OEt MeS HPri Me Me CH.sub.2 OEt MeSO HPri Me Me CH.sub.2 OEt Ms Q1Pri Me Me CH.sub.2 OEt MeS Q1Pri Me Me CH.sub.2 OEt MeSO Q1Pri Me Me CH.sub.2 OEt Ms Q2Pri Me Me CH.sub.2 OEt MeS Q2Pri Me Me CH.sub.2 OEt MeSO Q2Pri Me Me CH.sub.2 OEt Ms Q3Pri Me Me CH.sub.2 OEt MeS Q3Pri Me Me CH.sub.2 OEt MeSO Q3Pri Me Me CH.sub.2 OPri Ms HPri Me Me CH.sub.2 OPri Cl HPri Me Me CH.sub.2 OPri MeS HPri Me Me CH.sub.2 OPri MeSO HPri Me Me CH.sub.2 OPri Ms Q1Pri Me Me CH.sub.2 OPri Ms Q2Pri Me Me CH.sub.2 OPri Ms Q3Pri Me Me CH.sub.2 OPrn Ms HPri Me Me CH.sub. 2 OCHCH.sub.2 Ms HPri Me Me CH.sub.2 OCH.sub.2 CH2 Ms HPri Me Me CH.sub.2 OCH.sub.2 CCH Ms HPri Me Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri Me Me CH.sub.2 OY5 Ms HPri Me Me CHMeOH Ms HPri Me Me CHMeOMe Ms HPri Me Me CHMeOMe Cl HPri Me Me CHMeOMe MeS HPri Me Me CHMeOMe MeSO HPri Me Me CHMeOMe Ms Q1Pri Me Me CHMeOMe Ms Q2Pri Me Me CHMeOMe Ms Q3Pri Me Me CHMeOEt Ms HPri Me Me CHMeOEt Cl HPri Me Me CHMeOEt MeS HPri Me Me CHMeOEt MeSO HPri Me Me CHMeOEt Ms Q1Pri Me Me CHMeOEt Ms Q2Pri Me Me CHMeOEt Ms Q3Pri Me Me CHMeOPri Ms HPri Me Me CHMeOPri Cl HPri Me Me CHMeOPri MeS HPri Me Me CHMeOPri MeSO HPr i Me Me CHMeOPrn Ms HPri Me Me CHMeOCHCH.sub.2 Ms HPri Me Me CHMeOCHCH.sub.2 Ms HPri Me Me CHMeOCH.sub.2 CHCH.sub.2 Ms HPri Me Me CHMeOCH.sub.2 CCH Ms HPri Me Me CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri Me Me CMe.sub.2 OH Ms HPri Me Me CMe.sub.2 OMe Ms HPri Me Me CMe.sub.2 OEt Ms HPri Me Me CMe.sub.2 OPri Ms HPri Me Me CH.sub.2 CH.sub.2 OMe Ms HPri Me Me CH.sub.2 CH.sub.2 OEt Ms HPri Me Me CH.sub.2 CH.sub.2 OPri Ms HPri Me Me CHEtOH Ms HPri Me Me CHEtOMe Ms HPri Me Me CHEtOMe Cl HPri Me Me CHEtOMe MeS HPri Me Me CHEtOMe MeSO HPri Me Me CHEtOEt Ms HPri Me Me CHEtOPri Ms HPri Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HPri Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HPri Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HPri Me Me CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HPri Me Me CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri Me Me CH.sub.2 OY8 Ms HPri Me Me CH.sub.2 OY9 Ms HPri Me Me CH.sub.2 OY10 Ms HPri Me Me CHMeOY8 Ms HPri Me Me CHMeOY9 Ms HPri Me Me CHMeOY10 Ms HPri Me Me CH.sub.2 OY13 Ms HPri Me Me CHMeOY13 Ms HPri Me Me CH.sub.2 NMe.sub.2 Ms HPri Me Me CH.sub.2Y14 Ms HPri Me Me CHMeNMe.sub.2 Ms HPri Me Me CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri Me Me CH.sub.2 OCH.sub.2 Ph Ms HPri Me Me CHMeOCH.sub.2 Ph Ms HPri Me Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Me Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri Me Me CH.sub.2 OCHMeCO.sub.2 Me Ms HPri Me Me CH.sub.2 CN Ms HPri Me Me CHMeCN Ms HPri Me Me CH.sub.2 SMe Ms HPri Me Me CH.sub.2 SMe Cl HPri Me Me CH.sub.2 SMe MeS HPri Me Me CH.sub.2 SMe MeSO HPri Me Me CH.sub.2 SEt Ms HPri Me Me CH.sub.2 SEt Cl HPri Me Me CH.sub.2 SEt MeS HPri Me Me CH.sub.2 SEt MeSO HPri Me Me CH.sub.2 SOMe Ms HPri Me Me CH.sub.2 SOEt Ms HPri Me Me CH.sub.2 SO.sub.2 Me Ms HPri Me Me CH.sub.2 SO.sub.2 Me Cl HPri Me Me CH.sub.2 SO.sub.2 Me MeS HPri Me Me CH.sub.2 SO.sub.2 Me MeSO HPri Me Me CH.sub.2 SO.sub.2 Et Ms HPri Me Me CH.sub.2 SO.sub.2 Et Cl HPri Me Me CH.sub.2 SO.sub.2 Et MeS HPri Me Me CH.sub.2 SO.sub.2 Et MeSO HPri Me Me CHMeSMe Ms HPri Me Me CHMeSEt Ms HPri Me Me CHMeSO.sub.2 Me Ms HPri Me Me CHMeSO.sub.2 Et Ms HPri Me Me CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri Me Me CH.sub.2 OCOMe Ms HPri Me Me CH.sub.2 OCOEt Ms HPri Me Me CHMeOCOMe Ms HPri Me Me CH.sub.2 OSO.sub.2 Me Ms HPri Me Me CH.sub.2 OSO.sub.2 Et Ms HPri Me Me CHMeOSO.sub.2 Me Ms HMe Me Cl CH.sub.2 OH Ms HMe Me Cl CH.sub.2 OMe Ms HMe Me Cl CH.sub.2 OMe Cl HMe Me Cl CH.sub.2 OMe MeS HMe Me Cl CH.sub.2 OMe MeSO HMe Me Cl CH.sub.2 OMe Ms Q1Me Me Cl CH.sub.2 OMe Cl Q1Me Me Cl CH.sub.2 OMe MeS Q1Me Me Cl CH.sub.2 OMe MeSO Q2Me Me Cl CH.sub.2 OMe MeS Q2Me Me Cl CH.sub.2 OMe MeSO Q2Me Me Cl CH.sub.2 OMe Ms Q3Me Me Cl CH.sub.2 OMe MeS Q3Me Me Cl CH.sub.2 OMe MeSO Q3Me Me Cl CH.sub.2 OEt Ms HMe Me Cl CH.sub.2 OEt Cl HMe Me Cl CH.sub.2 OEt MeS HMe Me Cl CH.sub.2 OEt MeSO HMe Me Cl CH.sub.2 OEt Ms Q1Me Me Cl CH.sub.2 OEt MeS Q1Me Me Cl CH.sub.2 OEt MeSO Q1Me Me Cl CH.sub.2 OEt Ms Q2Me Me Cl CH.sub.2 OEt MeS Q2Me Me Cl CH.sub.2 OEt MeSO Q2Me Me Cl CH.sub.2 OEt Ms Q3Me Me Cl CH.sub.2 OEt MeS Q3Me Me Cl CH.sub.2 OEt MeSO Q3Me Me Cl CH.sub.2 OPri Ms HMe Me Cl CH.sub.2 OPri Cl HMe Me Cl CH.sub.2 OPri MeS HMe Me Cl CH.sub.2 OPri MeSO HMe Me Cl CH.sub.2 OPri Ms Q1Me Me Cl CH.sub.2 OPri Ms Q2Me Me Cl CH.sub. 2 OPri Ms Q3Me Me Cl CH.sub.2 OPrn Ms HMe Me Cl CH.sub.2 OCHCH.sub.2 Ms HMe Me Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe Me Cl CH.sub.2 OCH.sub.2 CCH Ms HMe Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe Me Cl CH.sub.2 OY5 Ms HMe Me Cl CHMeOH Ms HMe Me Cl CHMeOMe Ms HMe Me Cl CHMeOMe Cl HMe Me Cl CHMeOMe MeS HMe Me Cl CHMeOMe MeSO HMe Me Cl CHMeOMe Ms Q1Me Me Cl CHMeOMe Ms Q2Me Me Cl CHMeOMe Ms Q3Me Me Cl CHMeOEt Ms HMe Me Cl CHMeOEt Ms HMe Me Cl CHMeOEt Cl HMe Me Cl CHMeOEt MeS HMe Me Cl CHMeOEt MeSO HMe Me Cl CHMeOEt Ms Q1Me Me Cl CHMeOEt Ms Q2Me Me Cl CHMeOEt Ms Q3Me Me Cl CHMeOPri Ms HMe Me Cl CHMeOPri Cl HMe Me Cl CHMeOPri MeS HMe Me Cl CHMeOPri MeSO HMe Me Cl CHMeOPrn Ms HMe Me Cl CHMeOCHCH.sub.2 Ms HMe Me Cl CHMeOCHCH.sub.2 Ms HMe Me Cl CHMeOCH.sub.2 CHCH.sub.2 Ms HMe Me Cl CHMeOCH.sub.2 CCH Ms HMe Me Cl CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe Me Cl CHMeOY5 Ms HMe Me Cl CME.sub.2 OH Ms HMe Me Cl CMe.sub.2 OMe Ms HMe Me Cl CMe.sub.2 OEt Ms HMe Me Cl CMe.sub.2 OPri Ms HMe Me Cl CH.sub.2 CH.sub.2 OMe Ms HMe Me Cl CH.sub.2 CH.sub.2 OEt Ms HMe Me Cl CH.sub.2 CH.sub.2 OPri Ms HMe Me Cl CHEtOH Ms HMe Me Cl CHEtOMe Ms HMe Me Cl CHEtOMe Cl HMe Me Cl CHEtOMe MeS HMe Me Cl CHEtOMe MeSO HMe Me Cl CHEtOEt Ms HMe Me Cl CHEtOPri Ms HMe Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HMe Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HMe Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HMe Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HMe Me Cl CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe Me Cl CH.sub.2 OY8 Ms HMe Me Cl CH.sub.2 OY9 Ms HMe Me Cl CH.sub.2 OY10 Ms HMe Me Cl CHMeOY8 Ms HMe Me Cl CHMeOY9 Ms HMe Me Cl CHMeOY10 Ms HMe Me Cl CH.sub.2 OY13 Ms HMe Me Cl CHMeOY13 Ms HMe Me Cl CH.sub.2 NMe.sub.2 Ms HMe Me Cl CH.sub.2Y14 Ms HMe Me Cl CHMeNMe.sub.2 Ms HMe Me Cl CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe Me Cl CH.sub.2 OCH.sub.2 Ph Ms HMe Me Cl CHMeOCH.sub.2 Ph Ms HMe Me Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe Me Cl CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe Me Cl CH.sub.2 OCHMeCO.sub.2 Me Ms HMe Me Cl CH.sub.2 CN Ms HMe Me Cl CHMeCN Ms HMe Me Cl CH.sub.2 SMe Ms HMe Me Cl CH.sub.2 SMe Cl HMe Me Cl CH.sub.2 SMe MeS HMe Me Cl CH.sub.2 SMe MeSO HMe Me Cl CH.sub.2 SEt Ms HMe Me Cl CH.sub.2 SEt Cl HMe Me Cl CH.sub.2 SEt MeS HMe Me Cl CH.sub.2 SEt MeSO HMe Me Cl CH.sub.2 SOMe Ms HMe Me Cl CH.sub.2 SOEt Ms HMe Me Cl CH.sub.2 SO.sub.2 Me Ms HMe Me Cl CH.sub.2 SO.sub.2 Me Cl HMe Me Cl CH.sub.2 SO.sub.2 Me MeS HMe Me Cl CH.sub.2 SO.sub.2 Me MeSO HMe Me Cl CH.sub.2 SO.sub.2 Et Ms HMe Me Cl CH.sub.2 SO.sub.2 Et Cl HMe Me Cl CH.sub.2 SO.sub.2 Et MeS HMe Me Cl CH.sub.2 SO.sub.2 Et MeSO HMe Me Cl CHMeSMe Ms HMe Me Cl CHMeSEt Ms HMe Me Cl CHMeSO.sub.2 Me Ms HMe Me Cl CHMeSO.sub.2 Et Ms HMe Me Cl CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe Me Cl CH.sub.2 OCOMe Ms HMe Me Cl CH.sub.2 OCOEt Ms HMe Me Cl CHMeOCOMe Ms HMe Me Cl CH.sub.2 OSO.sub.2 Me Ms HMe Me Cl CH.sub.2 OSO.sub.2 Et Ms HMe Me Cl CHMeOSO.sub.2 Me Ms HEt Me Cl CH.sub.2 OH Ms HEt Me Cl CH.sub.2 OMe Ms HEt Me Cl CH.sub.2 OMe Cl HEt Me Cl CH.sub.2 OMe MeS HEt Me Cl CH.sub.2 OMe MeSO HEt Me Cl CH.sub.2 OMe Ms Q1Et Me Cl CH.sub.2 OMe Cl Q1Et Me Cl CH.sub.2 OMe MeS Q1Et Me Cl CH.sub.2 OMe MeSO Q2Et Me Cl CH.sub.2 OMe MeS Q2Et Me Cl CH.sub.2 OMe MeSO Q2Et Me Cl CH.sub.2 OMe Ms Q3Et Me Cl CH.sub.2 OMe MeS Q3Et Me Cl CH.sub.2 OMe MeSO Q3Et Me Cl CH.sub.2 OEt Ms HEt Me Cl CH.sub.2 OEt Cl HEt Me Cl CH.sub.2 OEt MeS HEt Me Cl CH.sub.2 OEt MeSO HEt Me Cl CH.sub.2 OEt Ms Q1Et Me Cl CH.sub.2 OEt MeS Q1Et Me Cl CH.sub.2 OEt MeSO Q1Et Me Cl CH.sub.2 OEt Ms Q2Et Me Cl CH.sub.2 OEt MeS Q2Et Me Cl CH.sub.2 OEt MeSO Q2Et Me Cl CH.sub.2 OEt Ms Q3Et Me Cl CH.sub.2 OEt MeS Q3Et Me Cl CH.sub.2 OEt MeSO Q3Et Me Cl CH.sub.2 OPri Ms HEt Me Cl CH.sub.2 OPri Cl HEt Me Cl CH.sub.2 OPri MeS HEt Me Cl CH.sub.2 OPri MeSO HEt Me Cl CH.sub.2 OPri Ms Q1Et Me Cl CH.sub.2 OPri Ms Q2Et Me Cl CH.sub.2 OPri Ms Q3Et Me Cl CH.sub.2 OPrn Ms HEt Me Cl CH.sub.2 OCHCH.sub.2 Ms HEt Me Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt Me Cl CH.sub.2 OCH.sub.2 CCH Ms HEt Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt Me Cl CH.sub.2 OY5 Ms HEt Me Cl CHMeOH Ms HEt Me Cl CHMeOMe Ms HEt Me Cl CHMeOMe Cl HEt Me Cl CHMeOMe MeS HEt Me Cl CHMeOMe MeSO HEt Me Cl CHMeOMe Ms Q1Et Me Cl CHMeOMe Ms Q2Et Me Cl CHMeOMe Ms Q3Et Me Cl CHMeOEt Ms HEt Me Cl CHMeOEt Cl HEt Me Cl CHMeOEt MeS HEt Me Cl CHMeOEt MeSO HEt Me Cl CHMeOEt Ms Q1Et Me Cl CHMeOEt Ms Q2Et Me Cl CHMeOEt Ms Q3Et Me Cl CHMeOPri Ms HEt Me Cl CHMeOPri Cl HEt Me Cl CHMeOPri MeS HEt Me Cl CHMeOPri MeSO HEt Me Cl CHMeOPrn Ms HEt Me Cl CHMeOCHCH.sub.2 Ms HEt Me Cl CHMeOCHCH.sub.2 Ms HEt Me Cl CHMeOCH.sub.2 CHCH.sub.2 Ms HEt Me Cl CHMeOCH.sub.2 CCH Ms HEt Me Cl CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt Me Cl CHMeOY5 Ms HEt Me Cl CMe.sub.2 OH Ms HEt Me Cl CMe.sub.2 OMe Ms HEt Me Cl CMe.sub.2 OEt Ms HEt Me Cl CMe.sub.2 OPri Ms HEt Me Cl CH.sub.2 CH.sub.2 OMe Ms HEt Me Cl CH.sub.2 CH.sub.2 OEt Ms HEt Me Cl CH.sub.2 CH.sub.2 OPri Ms HEt Me Cl CHEtOH Ms HEt Me Cl CHEtOMe Ms HEt Me Cl CHEtOMe Cl HEt Me Cl CHEtOMe MeS HEt Me Cl CHEtOEt Ms HEt Me Cl CHEtOPri Ms HEt Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HEt Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HEt Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HEt Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HEt Me Cl CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt Me Cl CH.sub.2 OY8 Ms HEt Me Cl CH.sub.2 OY9 Ms HEt Me Cl CH.sub.2 OY10 Ms HEt Me Cl CHMeO Y8 Ms HEt Me Cl CHMeOY9 Ms HEt Me Cl CHMeOY10 Ms HEt Me Cl CH.sub.2 OY13 Ms HEt Me Cl CHMeOY13 Ms HEt Me Cl CH.sub.2 NMe.sub.2 Ms HEt Me Cl CH.sub.2Y14 Ms HEt Me Cl CHMeNMe.sub.2 Ms HEt Me Cl CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt Me Cl CH.sub.2 OCH.sub.2 Ph Ms HEt Me Cl CHMeOCH.sub.2 Ph Ms HEt Me Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Me Cl CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt Me Cl CH.sub.2 OCHMeCO.sub.2 Me Ms HEt Me Cl CH.sub.2 CN Ms HEt Me Cl CHMeCN Ms HEt Me Cl CH.sub.2 SMe Ms HEt Me Cl CH.sub.2 SMe Cl HEt Me Cl CH.sub.2 SMe MeS HEt Me Cl CH.sub.2 SMe MeSO HEt Me Cl CH.sub.2 SEt Ms HEt Me Cl CH.sub.2 SEt Cl HEt Me Cl CH.sub.2 SEt MeS HEt Me Cl CH.sub.2 SEt MeSO HEt Me Cl CH.sub.2 SOMe Ms HEt Me Cl CH.sub.2 SOEt Ms HEt Me Cl CH.sub.2 SO.sub.2 Me Ms HEt Me Cl CH.sub.2 SO.sub.2 Me Cl HEt Me Cl CH.sub.2 SO.sub.2 Me MeS HEt Me Cl CH.sub.2 SO.sub.2 Me MeSO HEt Me Cl CH.sub.2 SO.sub.2 Et Ms HEt Me Cl CH.sub.2 SO.sub.2 Et Cl HEt Me Cl CH.sub.2 SO.sub.2 Et MeS HEt Me Cl CH.sub.2 SO.sub.2 Et MeSO HEt Me Cl CHMeSMe Ms HEt Me Cl CHMeSEt Ms HEt Me Cl CHMeSO.sub.2 Me Ms HEt Me Cl CHMeSO.sub.2 Et Ms HEt Me Cl CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt Me Cl CH.sub.2 OCOMe Ms HEt Me Cl CH.sub.2 OCOEt Ms HEt Me Cl CHMeOCOMe Ms HEt Me Cl CH.sub.2 OSO.sub.2 Me Ms HEt Me Cl CH.sub.2 OSO.sub.2 Et Ms HEt Me Cl CHMeOSO.sub.2 Me Ms HPri Me Cl CH.sub.2 OH Ms HPri Me Cl CH.sub.2 OMe Ms HPri Me Cl CH.sub.2 OMe Cl HPri Me Cl CH.sub.2 OMe MeS HPri Me Cl CH.sub.2 OMe MeSO HPri Me Cl CH.sub.2 OMe Ms Q1Pri Me Cl CH.sub.2 OMe Cl Q1Pri Me Cl CH.sub.2 OMe MeS Q1Pri Me Cl CH.sub.2 OMe MeSO Q2Pri Me Cl CH.sub.2 OMe MeS Q2Pri Me Cl CH.sub.2 OMe MeSO Q2Pri Me Cl CH.sub.2 OMe Ms Q3
TABLE 5__________________________________________________________________________ ##STR42##A B X Y Z Q__________________________________________________________________________Pri Me Cl CH.sub.2 OMe MeS Q3Pri Me Cl CH.sub.2 OMe MeSO Q3Pri Me Cl CH.sub.2 OEt Ms HPri Me Cl CH.sub.2 OEt Cl HPri Me Cl CH.sub.2 OEt MeS HPri Me Cl CH.sub.2 OEt MeSO HPri Me Cl CH.sub.2 OEt Ms Q1Pri Me Cl CH.sub.2 OEt MeS Q1Pri Me Cl CH.sub.2 OEt MeSO Q1Pri Me Cl CH.sub.2 OEt Ms Q2Pri Me Cl CH.sub.2 OEt MeS Q2Pri Me Cl CH.sub.2 OEt MeSO Q2Pri Me Cl CH.sub.2 OEt Ms Q3Pri Me Cl CH.sub.2 OEt MeS Q3Pri Me Cl CH.sub.2 OEt MeSO Q3Pri Me Cl CH.sub.2 OPri Ms HPri Me Cl CH.sub.2 OPri Cl HPri Me Cl CH.sub.2 OPri MeS HPri Me Cl CH.sub.2 OPri MeSO HPri Me Cl CH.sub.2 OPri Ms Q1Pri Me Cl CH.sub.2 OPri Ms Q2Pri Me Cl CH.sub.2 OPri Ms Q3Pri Me Cl CH.sub.2 OPrn Ms HPri Me Cl CH.sub.2 OCHCH.sub.2 Ms HPri Me Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri Me Cl CH.sub.2 OCH.sub.2 CCH Ms HPri Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri Me Cl CH.sub.2 OY5 Ms HPri Me Cl CHMeOH Ms HPri Me Cl CHMeOMe Ms HPri Me Cl CHMeOMe Cl HPri Me Cl CHMeOMe MeS HPri Me Cl CHMeOMe MeSO HPri Me Cl CHMeOMe Ms Q1Pri Me Cl CHMeOMe Ms Q2Pri Me Cl CHMeOMe Ms Q3Pri Me Cl CHMeOEt Ms HPri Me Cl CHMeOEt Ms HPri Me Cl CHMeOEt Cl HPri Me Cl CHMeOEt MeS HPri Me Cl CHMeOEt MeSO HPri Me Cl CHMeOEt Ms Q1Pri Me Cl CHMeOEt Ms Q2Pri Me Cl CHMeOEt Ms Q3Pri Me Cl CHMeOPri Ms HPri Me Cl CHMeOPri Cl HPri Me Cl CHMeOPri MeS HPri Me Cl CHMeOPri MeSO HPri Me Cl CHMeOPrn Ms HPri Me Cl CHMeOCHCH.sub.2 Ms HPri Me Cl CHMeOCHCH.sub.2 Ms HPri Me Cl CHMeOCH.sub.2 CHCH.sub.2 Ms HPri Me Cl CHMeOCH.sub.2 CCH Ms HPri Me Cl CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri Me Cl CHMeOY5 Ms HPri Me Cl CMe.sub.2 OH Ms HPri Me Cl CMe.sub.2 OMe Ms HPri Me Cl CMe.sub.2 OEt Ms HPri Me Cl CMe.sub.2 OPri Ms HPri Me Cl CH.sub.2 CH.sub.2 OMe Ms HPri Me Cl CH.sub.2 CH.sub.2 OEt Ms HPri Me Cl CH.sub.2 CH.sub.2 OPri Ms HPri Me Cl CHEtOH Ms HPri Me Cl CHEtOMe Ms HPri Me Cl CHEtOMe Cl HPri Me Cl CHEtOMe MeS HPri Me Cl CHEtOMe MeSO HPri Me Cl CHEtOEt Ms HPri Me Cl CHEtOPri Ms HPri Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HPri Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HPri Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HPri Me Cl CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HPri Me Cl CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri Me Cl CH.sub.2 OY8 Ms HPri Me Cl CH.sub.2 OY9 Ms HPri Me Cl CH.sub. 2 OY10 Ms HPri Me Cl CHMeOY8 Ms HPri Me Cl CHMeOY9 Ms HPri Me Cl CHMeOY10 Ms HPri Me Cl CH.sub.2 OY13 Ms HPri Me Cl CHMeOY13 Ms HPri Me Cl CH.sub.2 NMe.sub.2 Ms HPri Me Cl CH.sub.2Y14 Ms HPri Me Cl CHMeNMe.sub.2 Ms HPri Me Cl CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri Me Cl CH.sub.2 OCH.sub.2 Ph Ms HPri Me Cl CHMeOCH.sub.2 Ph Ms HPri Me Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Me Cl CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri Me Cl CH.sub.2 OCHMeCO.sub.2 Me Ms HPri Me Cl CH.sub.2 CN Ms HPri Me Cl CHMeCN Ms HPri Me Cl CH.sub.2 SMe Ms HPri Me Cl CH.sub.2 SMe Cl HPri Me Cl CH.sub.2 SMe MeS HPri Me Cl CH.sub.2 SMe MeSO HPri Me Cl CH.sub. 2 SEt Ms HPri Me Cl CH.sub.2 SEt Cl HPri Me Cl CH.sub.2 SEt MeS HPri Me Cl CH.sub.2 SEt MeSO HPri Me Cl CH.sub.2 SOMe Ms HPri Me Cl CH.sub.2 SOEt Ms HPri Me Cl CH.sub.2 SO.sub.2 Me Ms HPri Me Cl CH.sub.2 SO.sub.2 Me Cl HPri Me Cl CH.sub.2 SO.sub.2 Me MeS HPri Me Cl CH.sub.2 SO.sub.2 Me MeSO HPri Me Cl CH.sub.2 SO.sub.2 Et Ms HPri Me Cl CH.sub.2 SO.sub.2 Et Cl HPri Me Cl CH.sub.2 SO.sub.2 Et MeS HPri Me Cl CH.sub.2 SO.sub.2 Et MeSO HPri Me Cl CHMeSMe Ms HPri Me Cl CHMeSEt Ms HPri Me Cl CHMeSO.sub.2 Me Ms HPri Me Cl CHMeSO.sub.2 Et Ms HPri Me Cl CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri Me Cl CH.sub.2 OCOMe Ms HPri Me Cl CH.sub.2 OCOEt Ms HPri Me Cl CHMeOCOMe Ms HPri Me Cl CH.sub.2 OSO.sub.2 Me Ms HPri Me Cl CH.sub.2 OSO.sub.2 Et Ms HPri Me Cl CHMeOSO.sub.2 Me Ms HMe Me MeO CH.sub.2 OH Ms HMe Me MeO CH.sub.2 OMe Ms HMe Me MeO CH.sub.2 OMe Cl HMe Me MeO CH.sub.2 OMe MeS HMe Me MeO CH.sub.2 OMe MeSO HMe Me MeO CH.sub.2 OMe Ms Q1Me Me MeO CH.sub.2 OMe Cl Q1Me Me MeO CH.sub.2 OMe MeS Q1Me Me MeO CH.sub.2 OMe MeSO Q2Me Me MeO CH.sub.2 OMe MeS Q2Me Me MeO CH.sub.2 OMe MeSO Q2Me Me MeO CH.sub.2 OMe Ms Q3Me Me MeO CH.sub.2 OMe MeS Q3Me Me MeO CH.sub.2 OMe MeSO Q3Me Me MeO CH.sub.2 OEt Ms HMe Me MeO CH.sub.2 OEt Cl HMe Me MeO CH.sub.2 OEt MeS HMe Me MeO CH.sub.2 OEt MeSO HMe Me MeO CH.sub.2 OEt Ms Q1Me Me MeO CH.sub.2 OEt MeS Q1Me Me MeO CH.sub.2 OEt MeSO Q1Me Me MeO CH.sub.2 OEt Ms Q2Me Me MeO CH.sub.2 OEt MeS Q2Me Me MeO CH.sub.2 OEt MeSO Q2Me Me MeO CH.sub.2 OEt Ms Q3Me Me MeO CH.sub.2 OEt MeS Q3Me Me MeO CH.sub.2 OEt MeSO Q3Me Me MeO CH.sub.2 OPri Ms HMe Me MeO CH.sub.2 OPri Cl HMe Me MeO CH.sub.2 OPri MeS HMe Me MeO CH.sub.2 OPri MeSO HMe Me MeO CH.sub.2 OPri Ms Q1Me Me MeO CH.sub.2 OPri Ms Q2Me Me MeO CH.sub.2 OPri Ms Q3Me Me MeO CH.sub.2 OPrn Ms HMe Me MeO CH.sub.2 OCHCH.sub.2 Ms HMe Me MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe Me MeO CH.sub.2 OCH.sub.2 CCH Ms HMe Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe Me MeO CH.sub.2 OY5 Ms HMe Me MeO CHMeOH Ms HMe Me MeO CHMeOMe Ms HMe Me MeO CHMeOMe Cl HMe Me MeO CHMeOMe MeS HMe Me MeO CHMeOMe MeSO HMe Me MeO CHMeOMe Ms Q1Me Me MeO CHMeOMe Ms Q2Me Me MeO CHMeOMe Ms Q3Me Me MeO CHMeOEt Ms HMe Me MeO CHMeOEt Cl HMe Me MeO CHMeOEt MeS HMe Me MeO CHMeOEt MeSO HMe Me MeO CHMeOEt Ms Q1Me Me MeO CHMeOEt Ms Q2Me Me MeO CHMeOEt Ms Q3Me Me MeO CHMeOPri Ms HMe Me MeO CHMeOPri Cl HMe Me MeO CHMeOPri MeS HMe Me MeO CHMeOPri MeSO HMe Me MeO CHMeOPrn Ms HMe Me MeO CHMeOCHCH.sub.2 Ms HMe Me MeO CHMeOCHCH.sub.2 Ms HMe Me MeO CHMeOCH.sub.2 CHCH.sub.2 Ms HMe Me MeO CHMeOCH.sub.2 CCH Ms HMe Me MeO CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe Me MeO CHMeOY5 Ms HMe Me MeO CMe.sub.2 OH Ms HMe Me MeO CMe.sub.2 OMe Ms HMe Me MeO CMe.sub.2 OEt Ms HMe Me MeO CMe.sub.2 OPri Ms HMe Me MeO CH.sub.2 CH.sub.2 OMe Ms HMe Me MeO CH.sub.2 CH.sub.2 OEt Ms HMe Me MeO CH.sub.2 CH.sub.2 OPri Ms HMe Me MeO CHEtOH Ms HMe Me MeO CHEtOMe Ms HMe Me MeO CHEtOMe Cl HMe Me MeO CHEtOMe MeS HMe Me MeO CHEtOMe MeSO HMe Me MeO CHEtOEt Ms HMe Me MeO CHEtOPri Ms HMe Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HMe Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HMe Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HMe Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HMe Me MeO CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe Me MeO CH.sub.2 OY8 Ms HMe Me MeO CH.sub.2 OY9 Ms HMe Me MeO CH.sub.2 OY10 Ms HMe Me MeO CHMeOY8 Ms HMe Me MeO CHMeOY9 Ms HMe Me MeO CHMeOY10 Ms HMe Me MeO CH.sub.2 OY13 Ms HMe Me MeO CHMeOY13 Ms HMe Me MeO CH.sub.2 NMe.sub.2 Ms HMe Me MeO CH.sub.2Y14 Ms HMe Me MeO CHMeNMe.sub.2 Ms HMe Me MeO CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe Me MeO CH.sub.2 OCH.sub.2 Ph Ms HMe Me MeO CHMeOCH.sub.2 Ph Ms HMe Me MeO CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe Me MeO CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe Me MeO CH.sub.2 OCHMeCO.sub.2 Me Ms HMe Me MeO CH.sub.2 CN Ms HMe Me MeO CHMeCN Ms HMe Me MeO CH.sub.2 SMe Ms HMe Me MeO CH.sub.2 SMe Cl HMe Me MeO CH.sub.2 SMe MeS HMe Me MeO CH.sub.2 SMe MeSO HMe Me MeO CH.sub.2 SEt Ms HMe Me MeO CH.sub.2 SEt Cl HMe Me MeO CH.sub.2 SEt MeS HMe Me MeO CH.sub.2 SEt MeSO HMe Me MeO CH.sub.2 SOMe Ms HMe Me MeO CH.sub.2 SOEt Ms HMe Me MeO CH.sub.2 SO.sub.2 Me Ms HMe Me MeO CH.sub.2 SO.sub.2 Me Cl HMe Me MeO CH.sub.2 SO.sub.2 Me MeS HMe Me MeO CH.sub.2 SO.sub.2 Me MeSO HMe Me MeO CH.sub.2 SO.sub.2 Et Ms HMe Me MeO CH.sub.2 SO.sub.2 Et Cl HMe Me MeO CH.sub.2 SO.sub.2 Et MeS HMe Me MeO CH.sub.2 SO.sub.2 Et MeSO HMe Me MeO CHMeSMe Ms HMe Me MeO CHMeSEt Ms HMe Me MeO CHMeSO.sub.2 Me Ms HMe Me MeO CHMeSO.sub.2 Et Ms HMe Me MeO CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe Me MeO CH.sub.2 OCOMe Ms HMe Me MeO CH.sub.2 OCOEt Ms HMe Me MeO CHMeOCOMe Ms HMe Me MeO CH.sub.2 OSO.sub.2 Me Ms HMe Me MeO CH.sub.2 OSO.sub.2 Et Ms HMe Me MeO CHMeOSO.sub.2 Me Ms HEt Me MeO CH.sub.2 OH Ms HEt Me MeO CH.sub.2 OMe Ms HEt Me MeO CH.sub.2 OMe Cl HEt Me MeO CH.sub.2 OMe MeS HEt Me MeO CH.sub.2 OMe MeSO HEt Me MeO CH.sub.2 OMe Ms Q1Et Me MeO CH.sub.2 OMe Cl Q1Et Me MeO CH.sub.2 OMe MeS Q1Et Me MeO CH.sub.2 OMe MeSO Q2Et Me MeO CH.sub.2 OMe MeS Q2Et Me MeO CH.sub.2 OMe MeSO Q2Et Me MeO CH.sub.2 OMe Ms Q3Et Me MeO CH.sub.2 OMe MeS Q3Et Me MeO CH.sub.2 OMe MeSO Q3Et Me MeO CH.sub.2 OEt Ms HEt Me MeO CH.sub.2 OEt Cl HEt Me MeO CH.sub.2 OEt MeS HEt Me MeO CH.sub.2 OEt MeSO HEt Me MeO CH.sub.2 OEt Ms Q1Et Me MeO CH.sub.2 OEt MeS Q1Et Me MeO CH.sub.2 OEt MeSO Q1Et Me MeO CH.sub.2 OEt Ms Q2Et Me MeO CH.sub.2 OEt MeS Q2Et Me MeO CH.sub.2 OEt MeSO Q2Et Me MeO CH.sub.2 OEt Ms Q3Et Me MeO CH.sub.2 OEt MeS Q3Et Me MeO CH.sub.2 OEt MeSO Q3Et Me MeO CH.sub.2 OPri Ms HEt Me MeO CH.sub.2 OPri Cl HEt Me MeO CH.sub.2 OPri MeS HEt Me MeO CH.sub.2 OPri MeSO HEt Me MeO CH.sub.2 OPri Ms Q1Et Me MeO CH.sub.2 OPri Ms Q2Et Me MeO CH.sub.2 OPri Ms Q3Et Me MeO CH.sub.2 OPrn Ms HEt Me MeO CH.sub.2 OCHCH.sub.2 Ms HEt Me MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt Me MeO CH.sub.2 OCH.sub.2 CCH Ms HEt Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt Me MeO CH.sub.2 OY5 Ms HEt Me MeO CHMeOH Ms HEt Me MeO CHMeOMe Ms HEt Me MeO CHMeOMe Cl HEt Me MeO CHMeOMe MeS HEt Me MeO CHMeOMe MeSO HEt Me MeO CHMeOMe Ms Q1Et Me MeO CHMeOMe Ms Q2Et Me MeO CHMeOMe Ms Q3Et Me MeO CHMeOEt Ms HEt Me MeO CHMeOEt Cl HEt Me MeO CHMeOEt MeS HEt Me MeO CHMeOEt MeSO HEt Me MeO CHMeOEt Ms Q1Et Me MeO CHMeOEt Ms Q2Et Me MeO CHMeOEt Ms Q3Et Me MeO CHMeOPri Ms HEt Me MeO CHMeOPri Cl HEt Me MeO CHMeOPri MeS HEt Me MeO CHMeOPri MeSO HEt Me MeO CHMeOPrn Ms HEt Me MeO CHMeOCHCH.sub.2 Ms HEt Me MeO CHMeOCHCH.sub.2 Ms HEt Me MeO CHMeOCH.sub.2 CHCH.sub.2 Ms HEt Me MeO CHMeOCH.sub.2 CCH Ms HEt Me MeO CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt Me MeO CHMeOY5 Ms HEt Me MeO CMe.sub.2 OH Ms HEt Me MeO CMe.sub.2 OMe Ms HEt Me MeO CMe.sub.2 OEt Ms HEt Me MeO CMe.sub.2 OPri Ms HEt Me MeO CH.sub.2 CH.sub.2 OMe Ms HEt Me MeO CH.sub.2 CH.sub.2 OEt Ms HEt Me MeO CH.sub.2 CH.sub.2 OPri Ms HEt Me MeO CHEtOH Ms HEt Me MeO CHEtOMe Ms HEt Me MeO CHEtOMe Cl HEt Me MeO CHEtOMe MeS HEt Me MeO CHEtOMe MeSO HEt Me MeO CHEtOEt Ms HEt Me MeO CHEtOPri Ms HEt Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HEt Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HEt Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HEt Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HEt Me MeO CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt Me MeO CH.sub.2 OY8 Ms HEt Me MeO CH.sub.2 OY9 Ms HEt Me MeO CH.sub.2 OY10 Ms HEt Me MeO CHMeOY8 Ms HEt Me MeO CHMeOY9 Ms HEt Me MeO CHMeOY10 Ms HEt Me MeO CH.sub.2 OY13 Ms HEt Me MeO CHMeOY13 Ms HEt Me MeO CH.sub.2 NMe.sub.2 Ms HEt Me MeO CH.sub.2 Y14 Ms HEt Me MeO CHMeNMe.sub.2 Ms HEt Me MeO CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt Me MeO CH.sub.2 OCH.sub.2 Ph Ms HEt Me MeO CHMeOCH.sub.2 Ph Ms HEt Me MeO CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Me MeO CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt Me MeO CH.sub.2 OCHMeCO.sub.2 Me Ms HEt Me MeO CH.sub.2 CN Ms HEt Me MeO CHMeCN Ms HEt Me MeO CH.sub.2 SMe Ms HEt Me MeO CH.sub.2 SMe Cl HEt Me MeO CH.sub.2 SMe MeS HEt Me MeO CH.sub.2 SMe MeSO HEt Me MeO CH.sub.2 SEt Ms HEt Me MeO CH.sub.2 SEt Cl HEt Me MeO CH.sub.2 SEt MeS HEt Me MeO CH.sub.2 SEt MeSO HEt Me MeO CH.sub.2 SOMe Ms HEt Me MeO CH.sub.2 SOEt Ms HEt Me MeO CH.sub.2 SO.sub.2 Me Ms HEt Me MeO CH.sub.2 SO.sub.2 Me Cl HEt Me MeO CH.sub.2 SO.sub.2 Me MeS HEt Me MeO CH.sub.2 SO.sub.2 Me MeSO HEt Me MeO CH.sub.2 SO.sub.2 Et Ms HEt Me MeO CH.sub.2 SO.sub.2 Et Cl HEt Me MeO CH.sub.2 SO.sub.2 Et MeS HEt Me MeO CH.sub.2 SO.sub.2 Et MeSO HEt Me MeO CHMeSMe Ms HEt Me MeO CHMeSEt Ms HEt Me MeO CHMeSO.sub.2 Me Ms HEt Me MeO CHMeSO.sub.2 Et Ms HEt Me MeO CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt Me MeO CH.sub.2 OCOMe Ms HEt Me MeO CH.sub.2 OCOEt Ms HEt Me MeO CHMeOCOMe Ms HEt Me MeO CH.sub.2 OSO.sub.2 Me Ms HEt Me MeO CH.sub.2 OSO.sub.2 Et Ms HEt Me MeO CHMeOSO.sub.2 Me Ms HPri Me MeO CH.sub.2 OH Ms HPri Me MeO CH.sub.2 OMe Ms HPri Me MeO CH.sub.2 OMe Cl HPri Me MeO CH.sub.2 OMe MeS HPri Me MeO CH.sub.2 OMe MeSO HPri Me MeO CH.sub.2 OMe Ms Q1Pri Me MeO CH.sub.2 OMe Cl Q1Pri Me MeO CH.sub.2 OMe MeS Q1Pri Me MeO CH.sub.2 OMe MeSO Q2Pri Me MeO CH.sub.2 OMe MeS Q2Pri Me MeO CH.sub.2 OMe MeSO Q2Pri Me MeO CH.sub.2 OMe Ms Q3Pri Me MeO CH.sub.2 OMe MeS Q3Pri Me MeO CH.sub.2 OMe MeSO Q3Pri Me MeO CH.sub.2 OEt Ms HPri Me MeO CH.sub.2 OEt Cl HPri Me MeO CH.sub.2 OEt MeS HPri Me MeO CH.sub.2 OEt MeSO HPri Me MeO CH.sub.2 OEt Ms Q1Pri Me MeO CH.sub.2 OEt MeS Q1Pri Me MeO CH.sub.2 OEt MeSO Q1Pri Me MeO CH.sub.2 OEt Ms Q2Pri Me MeO CH.sub.2 OEt MeS Q2Pri Me MeO CH.sub.2 OEt MeSO Q2Pri Me MeO CH.sub.2 OEt Ms Q3Pri Me MeO CH.sub.2 OEt MeS Q3Pri Me MeO CH.sub.2 OEt MeSO Q3Pri Me MeO CH.sub.2 OPri Ms HPri Me MeO CH.sub.2 OPri Cl HPri Me MeO CH.sub.2 OPri MeS HPri Me MeO CH.sub.2 OPri MeSO HPri Me MeO CH.sub.2 OPri Ms Q1Pri Me MeO CH.sub.2 OPri Ms Q2Pri Me MeO CH.sub.2 OPri Ms Q3Pri Me MeO CH.sub.2 OPrn Ms HPri Me MeO CH.sub.2 OCHCH.sub.2 Ms HPri Me MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri Me MeO CH.sub.2 OCH.sub.2 CCH Ms HPri Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri Me MeO CH.sub.2 OY5 Ms HPri Me MeO CHMeOH Ms HPri Me MeO CHMeOMe Ms HPri Me MeO CHMeOMe Cl HPri Me MeO CHMeOMe MeS HPri Me MeO CHMeOMe MeSO HPri Me MeO CHMeOMe Ms Q1Pri Me MeO CHMeOMe Ms Q2Pri Me MeO CHMeOMe Ms Q3Pri Me MeO CHMeOEt Ms HPri Me MeO CHMeOEt Cl HPri Me MeO CHMeOEt MeS HPri Me MeO CHMeOEt MeSO HPri Me MeO CHMeOEt Ms Q1Pri Me MeO CHMeOEt Ms Q2Pri Me MeO CHMeOEt Ms Q3Pri Me MeO CHMeOPri Ms HPri Me MeO CHMeOPri Cl HPri Me MeO CHMeOPri MeS HPri Me MeO CHMeOPri MeSO HPri Me MeO CHMeOPrn Ms HPri Me MeO CHMeOCHCH.sub.2 Ms HPri Me MeO CHMeOCHCH.sub.2 Ms HPri Me MeO CHMeOCH.sub.2 CHCH.sub.2 Ms HPri Me MeO CHMeOCH.sub.2 CCH Ms HPri Me MeO CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri Me MeO CHMeOY5 Ms HPri Me MeO CMe.sub.2 OH Ms HPri Me MeO CMe.sub.2 OMe Ms HPri Me MeO CMe.sub.2 OEt Ms HPri Me MeO CMe.sub.2 OPri Ms HPri Me MeO CH.sub.2 CH.sub.2 OMe Ms HPri Me MeO CH.sub.2 CH.sub.2 OEt Ms HPri Me MeO CH.sub.2 CH.sub.2 OPri Ms HPri Me MeO CHEtOH Ms HPri Me MeO CHEtOMe Ms HPri Me MeO CHEtOMe Cl HPri Me MeO CHEtOMe MeS HPr i Me MeO CHEtOMe MeSO HPri Me MeO CHEtOEt Ms HPri Me MeO CHEtOPri Ms HPri Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Cl HPri Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeS HPri Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe MeSO HPri Me MeO CH.sub.2 OCH.sub.2 CH.sub.2 OEt Ms HPri Me MeO CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri Me MeO CH.sub.2 OY8 Ms HPri Me MeO CH.sub.2 OY9 Ms HPri Me MeO CH.sub.2 OY10 Ms HPri Me MeO CHMeOY8 Ms HPri Me MeO CHMeOY9 Ms HPri Me MeO CHMeOY10 Ms HPri Me MeO CH.sub.2 OY13 Ms HPri Me MeO CHMeOY13 Ms HPri Me MeO CH.sub.2 NMe.sub.2 Ms HPri Me MeO CH.sub.2Y14 Ms HPri Me MeO CHMeNMe.sub.2 Ms HPri Me MeO CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri Me MeO CH.sub.2 OCH.sub.2 Ph Ms HPri Me MeO CHMeOCH.sub.2 Ph Ms HPri Me MeO CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Me MeO CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri Me MeO CH.sub.2 OCHMeCO.sub.2 Me Ms HPri Me MeO CH.sub.2 CN Ms HPri Me MeO CHMeCN Ms HPri Me MeO CH.sub.2 SMe Ms HPri Me MeO CH.sub.2 SMe Cl HPri Me MeO CH.sub.2 SMe MeS HPri Me MeO CH.sub.2 SMe MeSO HPri Me MeO CH.sub.2 SEt Ms HPri Me MeO CH.sub.2 SEt Cl HPri Me MeO CH.sub.2 SEt MeS HPri Me MeO CH.sub.2 SEt MeSO HPri Me MeO CH.sub.2 SOMe Ms HPri Me MeO CH.sub.2 SOEt Ms HPri Me MeO CH.sub.2 SO.sub.2 Me Ms HPri Me MeO CH.sub.2 SO.sub.2 Me Cl HPri Me MeO CH.sub.2 SO.sub. 2 Me MeS HPri Me MeO CH.sub.2 SO.sub.2 Me MeSO HPri Me MeO CH.sub.2 SO.sub.2 Et Ms HPri Me MeO CH.sub.2 SO.sub.2 Et Cl HPri Me MeO CH.sub.2 SO.sub.2 Et MeS HPri Me MeO CH.sub.2 SO.sub.2 Et MeSO HPri Me MeO CHMeSMe Ms HPri Me MeO CHMeSEt Ms HPri Me MeO CHMeSO.sub.2 Me Ms HPri Me MeO CHMeSO.sub.2 Et Ms HPri Me MeO CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri Me MeO CH.sub.2 OCOMe Ms HPri Me MeO CH.sub.2 OCOEt Ms HPri Me MeO CHMeOCOMe Ms HPri Me MeO CH.sub.2 OSO.sub.2 Me Ms HPri Me MeO CH.sub.2 OSO.sub.2 Et Ms HPri Me MeO CHMeOSO.sub.2 Me Ms HMe H Br CH.sub.2 OH Ms HMe H Br CH.sub.2 OMe Ms HMe H Br CH.sub.2 OMe Cl HMe H Br CH.sub.2 OMe MeS HMe H Br CH.sub.2 OMe MeSO HMe H Br CH.sub.2 OEt Ms HMe H Br CH.sub.2 OEt Cl HMe H Br CH.sub.2 OEt MeS HMe H Br CH.sub.2 OEt MeSO HMe H Br CH.sub.2 OPri Ms HMe H Br CH.sub.2 OPrn Ms HMe H Br CH.sub.2 OCHCH.sub.2 Ms HMe H Br CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H Br CH.sub.2 OCH.sub.2 CCH Ms HMe H Br CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H Br CHMeOH Ms HMe H Br CHMeOMe Ms HMe H Br CHMeOMe Cl HMe H Br CHMeOMe MeS HMe H Br CHMeOMe MeSO HMe H Br CHMeOEt Ms HMe H Br CHMeOCHCH.sub.2 Ms HMe H Br CHMeOCHCH.sub.2 Ms HMe H Br CHMeOCH.sub.2 CHCH.sub.2 Ms HMe H Br CHMeOCH.sub.2 CCH Ms HMe H Br CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe H Br CMe.sub.2 OH Ms HMe H Br CMe.sub.2 OMe Ms HMe H Br CMe.sub.2 OEt Ms HMe H Br CH.sub.2 CH.sub.2 OMe Ms HMe H Br CH.sub.2 CH.sub.2 OEt Ms HMe H Br CHEtOH Ms HMe H Br CHEtOMe Ms HMe H Br CHEtOEt Ms HMe H Br CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe H Br CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe H Br CH.sub.2 NMe.sub.2 Ms HMe H Br CHMeNMe.sub.2 Ms HMe H Br CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe H Br CH.sub.2 OCH.sub.2 Ph Ms HMe H Br CHMeOCH.sub.2 PH Ms HMe H Br CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe H Br CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe H Br CH.sub.2 OCHMeCO.sub.2 Me Ms HMe H Br CH.sub.2 CN Ms HMe H Br CH.sub.2 SMe Ms HMe H Br CH.sub.2 SEt Ms HMe H Br CH.sub.2 SOMe Ms HMe H Br CH.sub.2 SO.sub.2 Me Ms HMe H Br CH.sub.2 SO.sub.2 Et Ms HMe H Br CHMeSMe Ms HMe H Br CHMeSO.sub.2 Me Ms HMe H Br CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe H Br CH.sub.2 OCOMe Ms HMe H Br CHMeOCOMe Ms HMe H Br CH.sub.2 OSO.sub.2 Me Ms HMe H Br CHMeOSO.sub.2 Me Ms HEt H Br CH.sub.2 OH Ms HEt H Br CH.sub.2 OMe Ms HEt H Br CH.sub.2 OMe Cl HEt H Br CH.sub.2 OMe MeS HEt H Br CH.sub.2 OMe MeSO HEt H Br CH.sub.2 OEt Ms HEt H Br CH.sub.2 OEt Cl HEt H Br CH.sub.2 OEt MeS HEt H Br CH.sub.2 OEt MeSO HEt H Br CH.sub.2 OPri Ms HEt H Br CH.sub.2 OPrn Ms HEt H Br CH.sub.2 OCHCH.sub.2 Ms HEt H Br CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H Br CH.sub.2 OCH.sub.2 CCH Ms HEt H Br CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H Br CHMeOH Ms HEt H Br CHMeOMe Ms HEt H Br CHMeOMe Cl HEt H Br CHMeOMe MeS HEt H Br CHMeOMe MeSO HEt H Br CHMeOEt Ms HEt H Br CHMeOCHCH.sub.2 Ms HEt H Br CHMeOCHCH.sub.2 Ms H
TABLE 5__________________________________________________________________________ ##STR43##A B X Y Z Q__________________________________________________________________________Et H Br CHMeOCH.sub.2 CHCH.sub.2 Ms HEt H Br CHMeOCH.sub.2 CCH Ms HEt H Br CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt H Br CMe.sub.2 OH Ms HEt H Br CMe.sub.2 OMe Ms HEt H Br CMe.sub.2 OEt Ms HEt H Br CH.sub.2 CH.sub.2 OMe Ms HEt H Br CH.sub.2 CH.sub.2 OEt Ms HEt H Br CHEtOH Ms HEt H Br CHEtOMe Ms HEt H Br CHEtOEt Ms HEt H Br CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt H Br CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt H Br CH.sub.2 NMe.sub.2 Ms HEt H Br CHMeNMe.sub.2 Ms HEt H Br CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt H Br CH.sub.2 OCH.sub.2 Ph Ms HEt H Br CHMeOCH.sub.2 Ph Ms HEt H Br CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt H Br CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt H Br CH.sub.2 OCHMeCO.sub.2 Me Ms HEt H Br CH.sub.2 CN Ms HEt H Br CH.sub.2 SMe Ms HEt H Br CH.sub.2 SEt Ms HEt H Br CH.sub.2 SOMe Ms HEt H Br CH.sub.2 SO.sub.2 Me Ms HEt H Br CH.sub.2 SO.sub.2 Et Ms HEt H Br CHMeSMe Ms HEt H Br CHMeSO.sub.2 Me Ms HEt H Br CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt H Br CH.sub.2 OCOMe Ms HEt H Br CHMeOCOMe Ms HEt H Br CH.sub.2 OSO.sub.2 Me Ms HEt H Br CHMeOSO.sub.2 Me Ms HPri H Br CH.sub.2 OH Ms HPri H Br CH.sub.2 OMe Ms HPri H Br CH.sub.2 OMe Cl HPri H Br CH.sub.2 OMe MeS HPri H Br CH.sub.2 OMe MeSO HPri H Br CH.sub.2 OEt Ms HPri H Br CH.sub.2 OEt Cl HPri H Br CH.sub.2 OEt MeS HPri H Br CH.sub.2 OEt MeSO HPri H Br CH.sub.2 OPri Ms HPri H Br CH.sub.2 OPrn Ms HPri H Br CH.sub.2 OCHCH.sub.2 Ms HPri H Br CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri H Br CH.sub.2 OCH.sub.2 CCH Ms HPri H Br CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri H Br CH.sub.2 CHMeOH Ms HPri H Br CH.sub.2 CHMeOMe Ms HPri H Br CH.sub.2 CHMeOMe Cl HPri H Br CH.sub.2 CHMeOMe MeS HPri H Br CH.sub.2 CHMeOMe MeSO HPri H Br CH.sub.2 CHMeOEt Ms HPri H Br CH.sub.2 CHMeOCHCH.sub.2 Ms HPri H Br CH.sub.2 CHMeOCHCH.sub.2 Ms HPri H Br CH.sub.2 CHMeOCH.sub.2 CHCH.sub.2 Ms HPri H Br CH.sub.2 CHMeOCH.sub.2 CCH Ms HPri H Br CH.sub.2 CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri H Br CH.sub.2 CMe.sub.2 OH Ms HPri H Br CH.sub.2 CMe.sub.2 OMe Ms HPri H Br CH.sub.2 CMe.sub.2 OEt Ms HPri H Br CH.sub.2 CH.sub.2 CH.sub.2 OMe Ms HPri H Br CH.sub.2 CH.sub.2 CH.sub.2 OEt Ms HPri H Br CH.sub.2 CHEtOH Ms HPri H Br CH.sub.2 CHEtOMe Ms HPri H Br CH.sub.2 CHEtOEt Ms HPri H Br CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri H Br CH.sub.2 CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri H Br CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri H Br CH.sub. 2 CHMeNMe.sub.2 Ms HPri H Br CH.sub.2 CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri H Br CH.sub.2 CH.sub.2 OCH.sub.2 Ph Ms HPri H Br CH.sub.2 CHMeOCH.sub.2 Ph Ms HPri H Br CH.sub.2 CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri H Br CH.sub.2 CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri H Br CH.sub.2 CH.sub.2 OCHMeCO.sub.2 Me Ms HPri H Br CH.sub.2 CH.sub.2 CN Ms HPri H Br CH.sub.2 CH.sub.2 SMe Ms HPri H Br CH.sub.2 CH.sub.2 SEt Ms HPri H Br CH.sub.2 CH.sub.2 SOMe Ms HPri H Br CH.sub.2 CH.sub.2 SO.sub.2 Me Ms HPri H Br CH.sub.2 CH.sub.2 SO.sub.2 Et Ms HPri H Br CH.sub.2 CHMeSMe Ms HPri H Br CH.sub.2 CHMeSO.sub.2 Me Ms HPri H Br CH.sub.2 CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri H Br CH.sub.2 CH.sub.2 OCOMe Ms HPri H Br CH.sub.2 CHMeOCOMe Ms HPri H Br CH.sub.2 CH.sub.2 OSO.sub.2 Me Ms HPri H Br CH.sub.2 CHMeOSO.sub.2 Me Ms HMe H I CH.sub.2 OH Ms HMe H I CH.sub.2 OMe Ms HMe H I CH.sub.2 OMe Cl HMe H I CH.sub.2 OMe MeS HMe H I CH.sub.2 OMe MeSO HMe H I CH.sub.2 OEt Ms HMe H I CH.sub.2 OEt Cl HMe H I CH.sub.2 OEt MeS HMe H I CH.sub.2 OEt MeSO HMe H I CH.sub.2 OPri Ms HMe H I CH.sub.2 OPrn Ms HMe H I CH.sub.2 OCHCH.sub.2 Ms HMe H I CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H I CH.sub.2 OCH.sub.2 CCH Ms HMe H I CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H I CHMeOH Ms HMe H I CHMeOMe Ms HMe H I CHMeOMe Cl HMe H I CHMeOMe MeS HMe H I CHMeOMe MeSO HMe H I CHMeOEt Ms HMe H I CHMeOCHCH.sub.2 Ms HMe H I CHMeOCHCH.sub.2 Ms HMe H I CHMeOCH.sub.2 CHCH.sub.2 Ms HMe H I CHMeOCH.sub.2 CCH Ms HMe H I CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe H I CMe.sub.2 OH Ms HMe H I CH.sub.2 CMe.sub.2 OMe Ms HMe H I CH.sub.2 CMe.sub.2 OEt Ms HMe H I CH.sub.2 CH.sub.2 CH.sub.2 OMe Ms HMe H I CH.sub.2 CH.sub.2 CH.sub.2 OEt Ms HMe H I CH.sub.2 CHEtOH Ms HMe H I CH.sub.2 CHEtOMe Ms HMe H I CH.sub.2 CHEtOEt Ms HMe H I CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe H I CH.sub.2 CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe H I CH.sub.2 NMe.sub.2 Ms HMe H I CH.sub.2 CHMeNMe.sub.2 Ms HMe H I CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe H I CH.sub.2 OCH.sub.2 Ph Ms HMe H I CH.sub.2 CHMeOCH.sub.2 Ph Ms HMe H I CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe H I CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe H I CH.sub.2 OCHMeCO.sub.2 Me Ms HMe H I CH.sub.2 CN Ms HMe H I CH.sub.2 SMe Ms HMe H I CH.sub.2 SEt Ms HMe H I CH.sub.2 SOMe Ms HMe H I CH.sub.2 SO.sub.2 Me Ms HMe H I CH.sub.2 SO.sub.2 Et Ms HMe H I CH.sub.2 CHMeSMe Ms HMe H I CH.sub.2 CHMeSO.sub.2 Me Ms HMe H I CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe H I CH.sub.2 OCOMe Ms HMe H I CH.sub.2 CHMeOCOMe Ms HMe H I CH.sub.2 OSO.sub.2 Me Ms HMe H I CH.sub.2 CHMeOSO.sub.2 Me Ms HEt H I CH.sub.2 OH Ms HEt H I CH.sub.2 OMe Ms HEt H I CH.sub.2 OMe Cl HEt H I CH.sub. 2 OMe MeS HEt H I CH.sub.2 OMe MeSO HEt H I CH.sub.2 OEt Ms HEt H I CH.sub.2 OEt Cl HEt H I CH.sub.2 OEt MeS HEt H I CH.sub.2 OEt MeSO HEt H I CH.sub.2 OPri Ms HEt H I CH.sub.2 OPrn Ms HEt H I CH.sub.2 OCHCH.sub.2 Ms HEt H I CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H I CH.sub.2 OCH.sub.2 CCH Ms HEt H I CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H I CH.sub.2 CHMeOH Ms HEt H I CH.sub.2 CHMeOMe Ms HEt H I CH.sub.2 CHMeOMe Cl HEt H I CH.sub.2 CHMeOMe MeS HEt H I CH.sub.2 CHMeOMe MeSO HEt H I CH.sub.2 CHMeOEt Ms HEt H I CH.sub.2 CHMeOCHCH.sub.2 Ms HEt H I CH.sub.2 CHMeOCHCH.sub.2 Ms HEt H I CH.sub.2 CHMeOCHCH.sub.2 Ms HEt H I CH.sub.2 CHMeOCH.sub. 2 CCH Ms HEt H I CH.sub.2 CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt H I CH.sub.2 CMe.sub.2 OH Ms HEt H I CH.sub.2 CMe.sub.2 OMe Ms HEt H I CH.sub.2 CMe.sub.2 OEt Ms HEt H I CH.sub.2 CH.sub.2 OMe Ms HEt H I CH.sub.2 CH.sub.2 OEt Ms HEt H I CH.sub.2 CHEtOH Ms HEt H I CH.sub.2 CHEtOMe Ms HEt H I CH.sub.2 CHEtOEt Ms HEt H I CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt H I CH.sub.2 CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt H I CH.sub.2 NMe.sub.2 Ms HEt H I CH.sub.2 CHMeNMe.sub.2 Ms HEt H I CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt H I CH.sub.2 OCH.sub.2 Ph Ms HEt H I CH.sub.2 CHMeOCH.sub.2 Ph Ms HEt H I CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt H I CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt H I CH.sub.2 OCHMeCO.sub.2 Me Ms HEt H I CH.sub.2 CN Ms HEt H I CH.sub.2 SMe Ms HEt H I CH.sub.2 SEt Ms HEt H I CH.sub.2 SOMe Ms HEt H I CH.sub.2 SO.sub.2 Me Ms HEt H I CH.sub.2 SO.sub.2 Et Ms HEt H I CH.sub.2 CHMeSMe Ms HEt H I CH.sub.2 CHMeSO.sub.2 Me Ms HEt H I CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt H I CH.sub.2 OCOMe Ms HEt H I CHMeOCOMe Ms HEt H I CH.sub.2 OSO.sub.2 Me Ms HEt H I CHMeOSO.sub.2 Me Ms HPri H I CH.sub.2 OH Ms HPri H I CH.sub.2 OMe Ms HPri H I CH.sub.2 OMe Cl HPri H I CH.sub.2 OMe MeS HPri H I CH.sub.2 OMe MeSO HPri H I CH.sub.2 OEt Ms HPri H I CH.sub.2 OEt Cl HPri H I CH.sub.2 OEt MeS HPri H I CH.sub.2 OEt MeSO HPri H I CH.sub.2 OPri Ms HPri H I CH.sub.2 OPrn Ms HPri H I CH.sub.2 OCHCH.sub.2 Ms HPri H I CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri H I CH.sub.2 OCH.sub.2 CCH Ms HPri H I CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri H I CHMeOH Ms HPri H I CHMeOMe Ms HPri H I CHMeOMe Cl HPri H I CHMeOMe MeS HPri H I CHMeOMe MeSO HPri H I CHMeOEt Ms HPri H I CHMeOCHCH.sub.2 Ms HPri H I CHMeOCHCH.sub.2 Ms HPri H I CHMeOCH.sub.2 CHCH.sub.2 Ms HPri H I CHMeOCH.sub.2 CCH Ms HPri H I CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri H I CMe.sub.2 OH Ms HPri H I CMe.sub.2 OMe Ms HPr i H I CMe.sub.2 OEt Ms HPri H I CH.sub.2 CH.sub.2 OMe Ms HPri H I CH.sub.2 CH.sub.2 OEt Ms HPri H I CHEtOH Ms HPri H I CHEtOMe Ms HPri H I CHEtOEt Ms HPri H I CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri H I CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri H I CH.sub.2 NMe.sub.2 Ms HPri H I CHMeNMe.sub.2 Ms HPri H I CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri H I CH.sub.2 OCH.sub.2 Ph Ms HPri H I CHMeOCH.sub.2 Ph Ms HPri H I CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri H I CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri H I CH.sub.2 OCHMeCO.sub.2 Me Ms HPri H I CH.sub.2 CN Ms HPri H I CH.sub.2 SMe Ms HPri H I CH.sub.2 SEt Ms HPri H I CH.sub.2 SOMe Ms HPri H I CH.sub.2 SO.sub.2 Me Ms HPri H I CH.sub.2 SO.sub.2 Et Ms HPri H I CHMeSMe Ms HPri H I CHMeSO.sub.2 Me Ms HPri H I CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri H I CH.sub.2 OCOMe Ms HPri H I CHMeOCOMe Ms HPri H I CH.sub.2 OSO.sub.2 Me Ms HPri H I CHMeOSO.sub.2 Me Ms HMe H Et CH.sub.2 OH Ms HMe H Et CH.sub.2 OMe Ms HMe H Et CH.sub.2 OMe Cl HMe H Et CH.sub.2 OMe MeS HMe H Et CH.sub.2 OMe MeSO HMe H Et CH.sub.2 OEt Ms HMe H Et CH.sub.2 OEt Cl HMe H Et CH.sub.2 OEt MeS HMe H Et CH.sub.2 OEt MeSO HMe H Et CH.sub.2 OPri Ms HMe H Et CH.sub.2 OPrn Ms HMe H Et CH.sub.2 OCHCH.sub.2 Ms HMe H Et CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H Et CH.sub.2 OCH.sub.2 CCH Ms HMe H Et CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H Et CHMeOH Ms HMe H Et CHMeOMe Ms HMe H Et CHMeOMe Cl HMe H Et CHMeOMe MeS HMe H Et CHMeOMe MeSO HMe H Et CHMeOEt Ms HMe H Et CHMeOCHCH.sub.2 Ms HMe H Et CHMeOCHCH.sub.2 Ms HMe H Et CHMeOCH.sub.2 CHCH.sub.2 Ms HMe H Et CHMeOCH.sub.2 CCH Ms HMe H Et CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe H Et CMe.sub.2 OH Ms HMe H Et CMe.sub.2 OMe Ms HMe H Et CMe.sub.2 OEt Ms HMe H Et CH.sub.2 CH.sub.2 OMe Ms HMe H Et CH.sub.2 CH.sub.2 OEt Ms HMe H Et CHEtOH Ms HMe H Et CHEtOMe Ms HMe H Et CHEtOEt Ms HMe H Et CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe H Et CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe H Et CH.sub.2 NMe.sub.2 Ms HMe H Et CHMeNMe.sub.2 Ms HMe H Et CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe H Et CH.sub.2 OCH.sub.2 Ph Ms HMe H Et CHMeOCH.sub.2 Ph Ms HMe H Et CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe H Et CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe H Et CH.sub.2 OCHMeCO.sub.2 Me Ms HMe H Et CH.sub.2 CN Ms HMe H Et CH.sub.2 SMe Ms HMe H Et CH.sub.2 SEt Ms HMe H Et CH.sub.2 SOMe Ms HMe H Et CH.sub.2 SO.sub.2 Me Ms HMe H Et CH.sub.2 SO.sub.2 Et Ms HMe H Et CHMeSMe Ms HMe H Et CHMeSO.sub.2 Me Ms HMe H Et CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe H Et CH.sub.2 OCOMe Ms HMe H Et CHMeOCOMe Ms HMe H Et CH.sub.2 OSO.sub.2 Me Ms HMe H Et CHMeOSO.sub.2 Me Ms HEt H Et CH.sub.2 OH Ms HEt H Et CH.sub.2 OMe Ms HEt H Et CH.sub.2 OMe Cl HEt H Et CH.sub.2 OMe MeS HEt H Et CH.sub.2 OMe MeSO HEt H Et CH.sub.2 OEt Ms HEt H Et CH.sub.2 OEt Cl HEt H Et CH.sub.2 OEt MeS HEt H Et CH.sub.2 OEt MeSO HEt H Et CH.sub.2 OPri Ms HEt H Et CH.sub.2 OPrn Ms HEt H Et CH.sub.2 OCHCH.sub.2 Ms HEt H Et CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H Et CH.sub.2 OCH.sub.2 CCH Ms HEt H Et CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H Et CHMeOH Ms HEt H Et CHMeOMe Ms HEt H Et CHMeOMe Cl HEt H Et CHMeOMe MeS HEt H Et CHMeOMe MeSO HEt H Et CHMeOEt Ms HEt H Et CHMeOCHCH.sub.2 Ms HEt H Et CHMeOCHCH.sub.2 Ms HEt H Et CHMeOCH.sub.2 CHCH.sub.2 Ms HEt H Et CHMeOCH.sub.2 CCH Ms HEt H Et CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt H Et CMe.sub.2 OH Ms HEt H Et CMe.sub.2 OMe Ms HEt H Et CMe.sub.2 OEt Ms HEt H Et CH.sub.2 CH.sub.2 OMe Ms HEt H Et CH.sub.2 CH.sub.2 OEt Ms HEt H Et CHEtOH Ms HEt H Et CHEtOMe Ms HEt H Et CHEtOEt Ms HEt H Et CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt H Et CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt H Et CH.sub.2 NMe.sub.2 Ms HEt H Et CHMeNMe.sub.2 Ms HEt H Et CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt H Et CH.sub.2 OCH.sub.2 Ph Ms HEt H Et CHMeOCH.sub.2 Ph Ms HEt H Et CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt H Et CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt H Et CH.sub.2 OCHMeCO.sub.2 Me Ms HEt H Et CH.sub.2 CN Ms HEt H Et CH.sub.2 SMe Ms HEt H Et CH.sub.2 SEt Ms HEt H Et CH.sub.2 SOMe Ms HEt H Et CH.sub.2 SO.sub.2 Me Ms HEt H Et CH.sub.2 SO.sub.2 Et Ms HEt H Et CHMeSMe Ms HEt H Et CHMeSO.sub.2 Me Ms HEt H Et CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt H Et CH.sub.2 OCOMe Ms HEt H Et CHMeOCOMe Ms HEt H Et CH.sub.2 OSO.sub.2 Me Ms HEt H Et CHMeOSO.sub.2 Me Ms HPri H Et CH.sub.2 OH Ms HPri H Et CH.sub.2 OMe Ms HPri H Et CH.sub.2 OMe Cl HPri H Et CH.sub.2 OMe MeS HPri H Et CH.sub.2 OMe MeSO HPri H Et CH.sub.2 OEt Ms HPri H Et CH.sub.2 OEt Cl HPri H Et CH.sub.2 OEt MeS HPri H Et CH.sub.2 OEt MeSO HPri H Et CH.sub.2 OPri Ms HPri H Et CH.sub.2 OPrn Ms HPri H Et CH.sub.2 OCHCH.sub.2 Ms HPri H Et CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri H Et CH.sub.2 OCH.sub.2 CCH Ms HPri H Et CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri H Et CHMeOH Ms HPri H Et CHMeOMe Ms HPri H Et CHMeOMe Cl HPri H Et CHMeOMe MeS HPri H Et CHMeOMe MeSO HPri H Et CHMeOEt Ms HPri H Et CHMeOCHCH.sub.2 Ms HPri H Et CHMeOCHCH.sub.2 Ms HPri H Et CHMeOCH.sub.2 CHCH.sub.2 Ms HPri H Et CHMeOCH.sub.2 CCH Ms HPri H Et CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri H Et CMe.sub.2 OH Ms HPri H Et CMe.sub.2 OMe Ms HPri H Et CMe.sub.2 OEt Ms HPri H Et CH.sub.2 CH.sub.2 OMe Ms HPri H Et CH.sub.2 CH.sub.2 OEt Ms HPri H Et CHEtOH Ms HPri H Et CHEtOMe Ms HPri H Et CHEtOEt Ms HPri H Et CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri H Et CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri H Et CH.sub.2 NMe.sub.2 Ms HPri H Et CHMeNMe.sub.2 Ms HPri H Et CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri H Et CH.sub.2 OCH.sub.2 Ph Ms HPri H Et CHMeOCH.sub.2 Ph Ms HPri H Et CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri H Et CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri H Et CH.sub.2 OCHMeCO.sub.2 Me Ms HPri H Et CH.sub.2 CN Ms HPri H Et CH.sub.2 SMe Ms HPri H Et CH.sub.2 SEt Ms HPri H Et CH.sub.2 SOMe Ms HPri H Et CH.sub.2 SO.sub.2 Me Ms HPri H Et CH.sub.2 SO.sub.2 Et Ms HPri H Et CHMeSMe Ms HPri H Et CHMeSO.sub.2 Me Ms HPri H Et CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri H Et CH.sub.2 OCOMe Ms HPri H Et CHMeOCOMe Ms HPri H Et CH.sub.2 OSO.sub.2 Me Ms HPri H Et CHMeOSO.sub.2 Me Ms HMe Me Br CH.sub.2 OH Ms HMe Me Br CH.sub.2 OMe Ms HMe Me Br CH.sub.2 OMe Cl HMe Me Br CH.sub.2 OMe MeS HMe Me Br CH.sub.2 OMe MeSO HMe Me Br CH.sub.2 OEt Ms HMe Me Br CH.sub.2 OEt Cl HMe Me Br CH.sub.2 OEt MeS HMe Me Br CH.sub.2 OEt MeSO HMe Me Br CH.sub.2 OPri Ms HMe Me Br CH.sub.2 OPrn Ms HMe Me Br CH.sub.2 OCHCH.sub.2 Ms HMe Me Br CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe Me Br CH.sub.2 OCH.sub.2 CCH Ms HMe Me Br CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe Me Br CHMeOH Ms HMe Me Br CHMeOMe Ms HMe Me Br CHMeOMe Cl HMe Me Br CHMeOMe MeS HMe Me Br CHMeOMe MeSO HMe Me Br CHMeOEt Ms HMe Me Br CH.sub.2 CH.sub.2 OMe Ms HMe Me Br CH.sub.2 CH.sub.2 OEt Ms HMe Me Br CHEtOH Ms HMe Me Br CHEtOMe Ms HMe Me Br CHEtOEt Ms HMe Me Br CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe Me Br CH.sub.2 NMe.sub.2 Ms HMe Me Br CH.sub.2 OCH.sub.2 Ph Ms HMe Me Br CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe Me Br CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe Me Br CH.sub.2 OCHMeCO.sub.2 Me Ms HMe Me Br CH.sub.2 CN Ms HMe Me Br CH.sub.2 SMe Ms HMe Me Br CH.sub.2 SEt Ms HMe Me Br CH.sub.2 SO.sub.2 Me Ms HMe Me Br CH.sub.2 SO.sub.2 Et Ms HMe Me Br CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe Me Br CH.sub.2 OCOMe Ms HMe Me Br CHMeOCOMe Ms HMe Me Br CH.sub.2 OSO.sub.2 Me Ms HMe Me Br CHMeOSO.sub.2 Me Ms HEt Me Br CH.sub.2 OH Ms HEt Me Br CH.sub.2 OMe Ms HEt Me Br CH.sub.2 OMe Cl HEt Me Br CH.sub.2 OMe MeS HEt Me Br CH.sub.2 OMe MeSO HEt Me Br CH.sub.2 OEt Ms HEt Me Br CH.sub.2 OEt Cl HEt Me Br CH.sub.2 OEt MeS HEt Me Br CH.sub.2 OEt MeSO HEt Me Br CH.sub.2 OPri Ms HEt Me Br CH.sub.2 OPrn Ms HEt Me Br CH.sub.2 OCHCH.sub.2 Ms HEt Me Br CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt Me Br CH.sub.2 OCH.sub.2 CCH Ms HEt Me Br CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt Me Br CHMeOH Ms HEt Me Br CHMeOMe Ms HEt Me Br CHMeOMe Cl HEt Me Br CHMeOMe MeS HEt Me Br CHMeOMe MeSO HEt Me Br CHMeOEt Ms HEt Me Br CH.sub.2 CH.sub.2 OMe Ms HEt Me Br CH.sub.2 CH.sub.2 OEt Ms HEt Me Br CHEtOH Ms HEt Me Br CHEtOMe Ms HEt Me Br CHEtOEt Ms HEt Me Br CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt Me Br CH.sub.2 NMe.sub.2 Ms HEt Me Br CH.sub.2 OCH.sub.2 Ph Ms HEt Me Br CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Me Br CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt Me Br CH.sub.2 OCHMeCO.sub.2 Me Ms HEt Me Br CH.sub.2 CN Ms HEt Me Br CH.sub.2 SMe Ms HEt Me Br CH.sub.2 SEt Ms HEt Me Br CH.sub.2 SO.sub.2 Me Ms HEt Me Br CH.sub.2 SO.sub.2 Et Ms HEt Me Br CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms H
TABLE 5__________________________________________________________________________ ##STR44##A B X Y Z Q__________________________________________________________________________Et Me Br CH.sub.2 OCOMe Ms HEt Me Br CHMeOCOMe Ms HEt Me Br CH.sub.2 OSO.sub.2 Me Ms HEt Me Br CHMeOSO.sub.2 Me Ms HPri Me Br CH.sub.2 OH Ms HPri Me Br CH.sub.2 OMe Ms HPri Me Br CH.sub.2 OMe Cl HPri Me Br CH.sub.2 OMe MeS HPri Me Br CH.sub.2 OMe MeSO HPri Me Br CH.sub.2 OEt Ms HPri Me Br CH.sub.2 OEt Cl HPri Me Br CH.sub.2 OEt MeS HPri Me Br CH.sub.2 OEt MeSO HPri Me Br CH.sub.2 OPri Ms HPr i Me Br CH.sub.2 OPrn Ms HPri Me Br CH.sub.2 OCH CH.sub.2 Ms HPri Me Br CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri Me Br CH.sub.2 OCH.sub.2 CCH Ms HPri Me Br CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri Me Br CHMeOH Ms HPri Me Br CHMeOMe Ms HPri Me Br CHMeOMe Cl HPri Me Br CHMeOMe MeS HPri Me Br CHMeOMe MeSO HPri Me Br CHMeOEt Ms HPri Me Br CH.sub.2 CH.sub.2 OMe Ms HPri Me Br CH.sub.2 CH.sub.2 OEt Ms HPri Me Br CHEtOH Ms HPri Me Br CHEtOMe Ms HPri Me Br CHEtOEt Ms HPri Me Br CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri Me Br CH.sub.2 NMe.sub.2 Ms HPri Me Br CH.sub.2 OCH.sub.2 Ph Ms HPri Me Br CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Me Br CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri Me Br CH.sub.2 OCHMeCO.sub.2 Me Ms HPri Me Br CH.sub.2 CN Ms HPri Me Br CH.sub.2 SMe Ms HPri Me Br CH.sub.2 SEt Ms HPri Me Br CH.sub.2 SO.sub.2 Me Ms HPri Me Br CH.sub.2 SO.sub.2 Et Ms HPri Me Br CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri Me Br CH.sub.2 OCOMe Ms HPri Me Br CHMeOCOMe Ms HPri Me Br CH.sub.2 OSO.sub.2 Me Ms HPri Me Br CHMeOSO.sub.2 Me Ms HMe Me I CH.sub.2 OH Ms HMe Me I CH.sub.2 OMe Ms HMe Me I CH.sub.2 OMe Cl HMe Me I CH.sub.2 OMe MeS HMe Me I CH.sub.2 OMe MeSO HMe Me I CH.sub.2 OEt Ms HMe Me I CH.sub.2 OEt Cl HMe Me I CH.sub.2 OEt MeS HMe Me I CH.sub.2 OEt MeSO HMe Me I CH.sub.2 OPr i Ms HMe Me I CH.sub.2 OPrn Ms HMe Me I CH.sub.2 OCHCH.sub.2 Ms HMe Me I CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe Me I CH.sub.2 OCH.sub.2 CCH Ms HMe Me I CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe Me I CHMeOH Ms HMe Me I CHMeOMe Ms HMe Me I CHMeOMe Cl HMe Me I CHMeOMe MeS HMe Me I CHMeOMe MeSO HMe Me I CHMeOEt Ms HMe Me I CH.sub.2 CH.sub.2 OMe Ms HMe Me I CH.sub.2 CH.sub.2 OEt Ms HMe Me I CHEtOH Ms HMe Me I CHEtOMe Ms HMe Me I CHEtOEt Ms HMe Me I CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe Me I CH.sub.2 NMe.sub.2 Ms HMe Me I CH.sub.2 OCH.sub.2 Ph Ms HMe Me I CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe Me I CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe Me I CH.sub.2 OCHMeCO.sub.2 Me Ms HMe Me I CH.sub.2 CN Ms HMe Me I CH.sub.2 SMe Ms HMe Me I CH.sub.2 SEt Ms HMe Me I CH.sub.2 SO.sub.2 Me Ms HMe Me I CH.sub.2 SO.sub.2 Et Ms HMe Me I CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe Me I CH.sub.2 OCOMe Ms HMe Me I CHMeOCOMe Ms HMe Me I CH.sub.2 OSO.sub.2 Me Ms HMe Me I CH.sub.2 MeOSO.sub.2 Me Ms HEt Me I CH.sub.2 OH Ms HEt Me I CH.sub.2 OMe Ms HEt Me I CH.sub.2 OMe Cl HEt Me I CH.sub.2 OMe MeS HEt Me I CH.sub.2 OMe MeSO HEt Me I CH.sub.2 OEt Ms HEt Me I CH.sub.2 OEt Cl HEt Me I CH.sub.2 OEt MeS HEt Me I CH.sub.2 OEt MeSO HEt Me I CH.sub.2 OPri Ms HEt Me I CH.sub.2 OPrn Ms HEt Me I CH.sub.2 OCHCH.sub.2 Ms HEt Me I CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt Me I CH.sub.2 OCH.sub.2 CCH Ms HEt Me I CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt Me I CHMeOH Ms HEt Me I CHMeOMe Ms HEt Me I CHMeOMe Cl HEt Me I CHMeOMe MeS HEt Me I CHMeOMe MeSO HEt Me I CHMeOEt Ms HEt Me I CH.sub.2 CH.sub.2 OMe Ms HEt Me I CH.sub.2 CH.sub.2 OEt Ms HEt Me I CHEtOH Ms HEt Me I CHEtOMe Ms HEt Me I CHEtOEt Ms HEt Me I CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt Me I CH.sub.2 NMe.sub.2 Ms HEt Me I CH.sub.2 OCH.sub.2 Ph Ms HEt Me I CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Me I CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt Me I CH.sub.2 OCHMeCO.sub.2 Me Ms HEt Me I CH.sub.2 CN Ms HEt Me I CH.sub.2 SMe Ms HEt Me I CH.sub.2 SEt Ms HEt Me I CH.sub.2 SO.sub.2 Me Ms HEt Me I CH.sub.2 SO.sub.2 Et Ms HEt Me I CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt Me I CH.sub.2 OCOMe Ms HEt Me I CHMeOCOMe Ms HEt Me I CH.sub.2 OSO.sub.2 Me Ms HEt Me I CHMeOSO.sub.2 Me Ms HPri Me I CH.sub.2 OH Ms HPri Me I CH.sub.2 OMe Ms HPri Me I CH.sub.2 OMe Cl HPri Me I CH.sub.2 OMe MeS HPri Me I CH.sub.2 OMe MeSO HPri Me I CH.sub.2 OEt Ms HPri Me I CH.sub.2 OEt Cl HPri Me I CH.sub.2 OEt MeS HPri Me I CH.sub.2 OEt MeSO HPri Me I CH.sub.2 OPri Ms HPri Me I CH.sub.2 OPrn Ms HPri Me I CH.sub.2 OCHCH.sub.2 Ms HPri Me I CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri Me I CH.sub.2 OCH.sub.2 C CH Ms HPri Me I CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri Me I CHMeOH Ms HPri Me I CHMeOMe Ms HPri Me I CHMeOMe Cl HPri Me I CHMeOMe MeS HPri Me I CHMeOMe MeSO HPri Me I CHMeOEt Ms HPri Me I CH.sub.2 CH.sub.2 OMe Ms HPri Me I CH.sub.2 CH.sub.2 OEt Ms HPri Me I CHEtOH Ms HPri Me I CHEtOMe Ms HPri Me I CHEtOEt Ms HPri Me I CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri Me I CH.sub.2 NMe.sub.2 Ms HPri Me I CH.sub.2 OCH.sub.2 Ph Ms HPri Me I CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Me I CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri Me I CH.sub.2 OCHMeCO.sub.2 Me Ms HPri Me I CH.sub.2 CN Ms HPri Me I CH.sub.2 SMe Ms HPr i Me I CH.sub.2 SEt Ms HPri Me I CH.sub.2 SO.sub.2 Me Ms HPri Me I CH.sub.2 SO.sub.2 Et Ms HPri Me I CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri Me I CH.sub.2 OCOMe Ms HPri Me I CHMeOCOMe Ms HPri Me I CH.sub.2 OSO.sub.2 Me Ms HPri Me I CHMeOSO.sub.2 Me Ms HMe Me Et CH.sub.2 OH Ms HMe Me Et CH.sub.2 OMe Ms HMe Me Et CH.sub.2 OMe Cl HMe Me Et CH.sub.2 OMe MeS HMe Me Et CH.sub.2 OMe MeSO HMe Me Et CH.sub.2 OEt Ms HMe Me Et CH.sub.2 OEt Cl HMe Me Et CH.sub.2 OEt MeS HMe Me Et CH.sub.2 OEt MeSO HMe Me Et CH.sub.2 OPri Ms HMe Me Et CH.sub.2 OPrn Ms HMe Me Et CH.sub.2 OCHCH.sub.2 Ms HMe Me Et CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe Me Et CH.sub.2 OCH.sub.2 C CH Ms HMe Me Et CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe Me Et CHMeOH Ms HMe Me Et CHMeOMe Ms HMe Me Et CHMeOMe Cl HMe Me Et CHMeOMe MeS HMe Me Et CHMeOMe MeSO HMe Me Et CHMeOEt Ms HMe Me Et CH.sub.2 CH.sub.2 OMe Ms HMe Me Et CH.sub.2 CH.sub.2 OEt Ms HMe Me Et CHEtOH Ms HMe Me Et CHEtOMe Ms HMe Me Et CHEtOEt Ms HMe Me Et CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe Me Et CH.sub.2 NMe.sub.2 Ms HMe Me Et CH.sub.2 OCH.sub.2 Ph Ms HMe Me Et CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe Me Et CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe Me Et CH.sub.2 OCHMeCO.sub.2 Me Ms HMe Me Et CH.sub.2 CN Ms HMe Me Et CH.sub.2 SMe Ms HMe Me Et CH.sub.2 SEt Ms HMe Me Et CH.sub.2 SO.sub.2 Me Ms HMe Me Et CH.sub. 2 SO.sub.2 Et Ms HMe Me Et CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe Me Et CH.sub.2 OCOMe Ms HMe Me Et CHMeOCOMe Ms HMe Me Et CH.sub.2 OSO.sub.2 Me Ms HMe Me Et CHMeOSO.sub.2 Me Ms HEt Me Et CH.sub.2 OH Ms HEt Me Et CH.sub.2 OMe Ms HEt Me Et CH.sub.2 OMe Cl HEt Me Et CH.sub.2 OMe MeS HEt Me Et CH.sub.2 OMe MeSO HEt Me Et CH.sub.2 OEt Ms HEt Me Et CH.sub.2 OEt Cl HEt Me Et CH.sub.2 OEt MeS HEt Me Et CH.sub.2 OEt MeSO HEt Me Et CH.sub.2 OPri Ms HEt Me Et CH.sub.2 OPrn Ms HEt Me Et CH.sub.2 OCHCH.sub.2 Ms HEt Me Et CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt Me Et CH.sub.2 OCH.sub.2 CCH Ms HEt Me Et CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt Me Et CHMeOH Ms HEt Me Et CHMeOMe Ms HEt Me Et CHMeOMe Cl HEt Me Et CHMeOMe MeS HEt Me Et CHMeOMe MeSO HEt Me Et CHMeOEt Ms HEt Me Et CH.sub.2 CH.sub.2 OMe Ms HEt Me Et CH.sub.2 CH.sub.2 OEt Ms HEt Me Et CHEtOH Ms HEt Me Et CHEtOMe Ms HEt Me Et CHEtOEt Ms HEt Me Et CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt Me Et CH.sub.2 NMe.sub.2 Ms HEt Me Et CH.sub.2 OCH.sub.2 Ph Ms HEt Me Et CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Me Et CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt Me Et CH.sub.2 OCHMeCO.sub.2 Me Ms HEt Me Et CH.sub.2 CN Ms HEt Me Et CH.sub.2 SMe Ms HEt Me Et CH.sub.2 SEt Ms HEt Me Et CH.sub.2 SO.sub.2 Me Ms HEt Me Et CH.sub.2 SO.sub.2 Et Ms HEt Me Et CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt Me Et CH.sub.2 OCOMe Ms HEt Me Et CHMeOCOMe Ms HEt Me Et CH.sub.2 OSO.sub.2 Me Ms HEt Me Et CHMeOSO.sub.2 Me Ms HPri Me Et CH.sub.2 OH Ms HPri Me Et CH.sub.2 OMe Ms HPri Me Et CH.sub.2 OMe Cl HPri Me Et CH.sub.2 OMe MeS HPri Me Et CH.sub.2 OMe MeSO HPri Me Et CH.sub.2 OEt Ms HPri Me Et CH.sub.2 OEt Cl HPri Me Et CH.sub.2 OEt MeS HPri Me Et CH.sub.2 OEt MeSO HPri Me Et CH.sub.2 OPri Ms HPri Me Et CH.sub.2 OPrn Ms HPri Me Et CH.sub.2 OCHCH.sub.2 Ms HPri Me Et CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri Me Et CH.sub.2 OCH.sub.2 CCH Ms HPri Me Et CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri Me Et CHMeOH Ms HPri Me Et CHMeOMe Ms HPri Me Et CHMeOMe Cl HPri Me Et CHMeOMe MeS HPri Me Et CHMeOMe MeSO HPri Me Et CHMeOEt Ms HPri Me Et CH.sub.2 CH.sub.2 OMe Ms HPri Me Et CH.sub.2 CH.sub.2 OEt Ms HPri Me Et CHEtOH Ms HPri Me Et CHEtOMe Ms HPri Me Et CHEtOEt Ms HPri Me Et CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri Me Et CH.sub.2 NMe.sub.2 Ms HPri Me Et CH.sub.2 OCH.sub.2 Ph Ms HPri Me Et CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Me Et CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri Me Et CH.sub.2 OCHMeCO.sub.2 Me Ms HPri Me Et CH.sub.2 CN Ms HPri Me Et CH.sub.2 SMe Ms HPri Me Et CH.sub.2 SEt Ms HPri Me Et CH.sub.2 SO.sub.2 Me Ms HPri Me Et CH.sub.2 SO.sub.2 Et Ms HPri Me Et CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri Me Et CH.sub.2 OCOMe Ms HPri Me Et CHMeOCOMe Ms HPri Me Et CH.sub.2 OSO.sub.2 Me Ms HPri Me Et CHMeOSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OH Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OMe Cl HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OMe MeS HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OMe MeSO HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OEt Cl HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OEt MeS HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OEt MeSO HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OPri Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OPrn Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCH.sub.2 CCH Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOH Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOMe Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOMe Cl HCH.sub.2 CHCH.sub.2 H Me CHMeOMe MeS HCH.sub.2 CHCH.sub.2 H Me CHMeOMe MeSO HCH.sub.2 CHCH.sub.2 H Me CHMeOEt Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOCH.sub.2 CCH Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CHCH.sub.2 H Me CMe.sub.2 OH Ms HCH.sub.2 CHCH.sub.2 H Me CMe.sub.2 OMe Ms HCH.sub.2 CHCH.sub. 2 H Me CMe.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 CH.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H Me CHEtOH Ms HCH.sub.2 CHCH.sub.2 H Me CHEtOMe Ms HCH.sub.2 CHCH.sub.2 H Me CHEtOEt Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Me CHMeNMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCH.sub.2 Ph Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOCH.sub.2 Ph Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCHMeCO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 CN Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 SMe Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 SEt Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 SOMe Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 SO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 SO.sub.2 Et Ms HCH.sub.2 CHCH.sub.2 H Me CHMeSMe Ms HCH.sub.2 CHCH.sub.2 H Me CHMeSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OCOMe Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOCOMe Ms HCH.sub.2 CHCH.sub.2 H Me CH.sub.2 OSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Me CHMeOSO.sub.2 Me Ms HCH.sub.2 CCH H Me CH.sub.2 OH Ms HCH.sub.2 C CH H Me CH.sub.2 OMe Ms HCH.sub.2 CCH H Me CH.sub.2 OMe Cl HCH.sub.2 CCH H Me CH.sub.2 OMe MeS HCH.sub.2 CCH H Me CH.sub.2 OMe MeSO HCH.sub.2 CCH H Me CH.sub.2 OEt Ms HCH.sub.2 CCH H Me CH.sub.2 OEt Cl HCH.sub.2 CCH H Me CH.sub.2 OEt MeS HCH.sub.2 CCH H Me CH.sub.2 OEt MeSO HCH.sub.2 CCH H Me CH.sub.2 OPri Ms HCH.sub.2 CCH H Me CH.sub.2 OPrn Ms HCH.sub.2 C CH H Me CH.sub.2 OCHCH.sub.2 Ms HCH.sub.2 CCH H Me CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CCH H Me CH.sub.2 OCH.sub.2 CCH Ms HCH.sub.2 CCH H Me CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CCH H Me CHMeOH Ms HCH.sub.2 CCH H Me CHMeOMe Ms HCH.sub.2 CCH H Me CHMeOMe Cl HCH.sub.2 CCH H Me CHMeOMe MeS HCH.sub.2 CCH H Me CHMeOMe MeSO HCH.sub.2 CCH H Me CHMeOEt Ms HCH.sub.2 CCH H Me CHMeOCHCH.sub.2 Ms HCH.sub.2 CCH H Me CHMeOCHCH.sub.2 Ms HCH.sub.2 CCH H Me CHMeOCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CCH H Me CHMeOCH.sub.2 CCH Ms HCH.sub.2 CCH H Me CHMeOCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CCH H Me CMe.sub.2 OH Ms HCH.sub.2 CCH H Me CMe.sub.2 OMe Ms HCH.sub.2 CCH H Me CMe.sub.2 OEt Ms HCH.sub.2 CCH H Me CH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 C CH H Me CH.sub.2 CH.sub.2 OEt Ms HCH.sub.2 CCH H Me CHEtOH Ms HCH.sub.2 CCH H Me CHEtOMe Ms HCH.sub.2 CCH H Me CHEtOEt Ms HCH.sub.2 CCH H Me CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H Me CHMeOCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H Me CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CCH H Me CHMeNMe.sub.2 Ms HCH.sub.2 CCH H Me CH.sub.2 CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CCH H Me CH.sub.2 OCH.sub. 2 Ph Ms HCH.sub.2 CCH H Me CHMeOCH.sub.2 Ph Ms HCH.sub.2 CCH H Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HCH.sub.2 CCH H Me CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HCH.sub.2 CCH H Me CH.sub.2 OCHMeCO.sub.2 Me Ms HCH.sub.2 CCH H Me CH.sub.2 CN Ms HCH.sub.2 CCH H Me CH.sub.2 SMe Ms HCH.sub.2 CCH H Me CH.sub.2 SEt Ms HCH.sub.2 CCH H Me CH.sub.2 SOMe Ms HCH.sub.2 CCH H Me CH.sub.2 SO.sub.2 Me Ms HCH.sub.2 C CH H Me CH.sub.2 SO.sub.2 Et Ms HCH.sub.2 CCH H Me CHMeSMe Ms HCH.sub.2 CCH H Me CHMeSO.sub.2 Me Ms HCH.sub.2 CCH H Me CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H Me CH.sub.2 OCOMe Ms HCH.sub.2 CCH H Me CHMeOCOMe Ms HCH.sub.2 CCH H Me CH.sub.2 OSO.sub.2 Me Ms HCH.sub.2 CCH H Me CHMeOSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OH Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OMe Cl HCH.sub.2 CHCH.sub. 2 H Cl CH.sub.2 OMe MeS HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OMe MeSO HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OEt Cl HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OEt MeS HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OEt MeSO HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OPri Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OPrn Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCH.sub.2 CCH Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOH Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOMe Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOMe Cl HCH.sub.2 CHCH.sub.2 H Cl CHMeOMe MeS HCH.sub.2 CHCH.sub.2 H Cl CHMeOMe MeSO HCH.sub.2 CHCH.sub.2 H Cl CHMeOEt Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOCH.sub.2 CCH Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CHCH.sub.2 H Cl CMe.sub.2 OH Ms HCH.sub.2 CHCH.sub.2 H Cl CMe.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Cl CMe.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 CH.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H Cl CHEtOH Ms HCH.sub.2 CHCH.sub.2 H Cl CHEtOMe Ms HCH.sub.2 CHCH.sub.2 H Cl CHEtOEt Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub. 2 OCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeNMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCH.sub.2 Ph Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOCH.sub.2 Ph Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCHMeCO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 CN Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 SMe Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 SEt Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 SOMe Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 SO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 SO.sub.2 Et Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeSMe Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OCOMe Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOCOMe Ms HCH.sub.2 CHCH.sub.2 H Cl CH.sub.2 OSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H Cl CHMeOSO.sub.2 Me Ms HCH.sub.2 CCH H Cl CH.sub.2 OH Ms HCH.sub.2 CCH H Cl CH.sub.2 OMe Ms HCH.sub.2 CCH H Cl CH.sub.2 OMe Cl HCH.sub.2 CCH H Cl CH.sub.2 OMe MeS HCH.sub.2 CCH H Cl CH.sub.2 OMe MeSO HCH.sub.2 C CH H Cl CH.sub.2 OEt Ms HCH.sub.2 CCH H Cl CH.sub.2 OEt Cl HCH.sub.2 CCH H Cl CH.sub.2 OEt MeS HCH.sub.2 CCH H Cl CH.sub.2 OEt MeSO HCH.sub.2 CCH H Cl CH.sub.2 OPri Ms HCH.sub.2 CCH H Cl CH.sub.2 OPrn Ms HCH.sub.2 CCH H Cl CH.sub.2 OCHCH.sub.2 Ms HCH.sub.2 CCH H Cl CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CCH H Cl CH.sub.2 OCH.sub.2 CCH Ms HCH.sub.2 C CH H Cl CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CCH H Cl CHMeOH Ms HCH.sub.2 CCH H Cl CHMeOMe Ms HCH.sub.2 CCH H Cl CHMeOMe Cl HCH.sub.2 CCH H Cl CHMeOMe MeS HCH.sub.2 CCH H Cl CHMeOMe MeSO HCH.sub.2 CCH H Cl CHMeOEt Ms HCH.sub.2 CCH H Cl CHMeOCHCH.sub.2 Ms HCH.sub.2 CCH H Cl CHMeOCHCH.sub.2 Ms HCH.sub.2 CCH H Cl CHMeOCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 C CH H Cl CHMeOCH.sub.2 CCH Ms HCH.sub.2 CCH H Cl CHMeOCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CCH H Cl CMe.sub.2 OH Ms HCH.sub.2 CCH H Cl CMe.sub.2 OMe Ms HCH.sub.2 CCH H Cl CMe.sub.2 OEt Ms H
TABLE 5__________________________________________________________________________ ##STR45##A B X Y Z Q__________________________________________________________________________CH.sub.2 CCH H Cl CH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H Cl CH.sub.2 CH.sub.2 OEt Ms HCH.sub.2 CCH H Cl CHEtOH Ms HCH.sub.2 CCH H Cl CHEtOMe Ms HCH.sub.2 CCH H Cl CHEtOEt Ms HCH.sub.2 CCH H Cl CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H Cl CHMeOCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H Cl CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CCH H Cl CHMeNMe.sub.2 Ms HCH.sub.2 CCH H Cl CH.sub.2 CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CCH H Cl CH.sub.2 OCH.sub.2 Ph Ms HCH.sub.2 CCH H Cl CHMeOCH.sub.2 Ph Ms HCH.sub.2 CCH H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HCH.sub.2 CCH H Cl CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HCH.sub.2 CCH H Cl CH.sub.2 OCHMeCO.sub.2 Me Ms HCH.sub.2 C CH H Cl CH.sub.2 CN Ms HCH.sub.2 CCH H Cl CH.sub.2 SMe Ms HCH.sub.2 CCH H Cl CH.sub.2 SEt Ms HCH.sub.2 CCH H Cl CH.sub.2 SOMe Ms HCH.sub.2 CCH H Cl CH.sub.2 SO.sub.2 Me Ms HCH.sub.2 CCH H Cl CH.sub.2 SO.sub.2 Et Ms HCH.sub.2 CCH H Cl CHMeSMe Ms HCH.sub.2 CCH H Cl CHMeSO.sub.2 Me Ms HCH.sub.2 CCH H Cl CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H Cl CH.sub.2 OCOMe Ms HCH.sub.2 CCH H Cl CHMeOCOMe Ms HCH.sub.2 CCH H Cl CH.sub.2 OSO.sub.2 Me Ms HCH.sub.2 CCH H Cl CHMeOSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OH Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OMe Cl HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OMe MeS HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OMe MeSO HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OEt Cl HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OEt MeS HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OEt MeSO HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OPri Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OPrn Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCH.sub.2 CCH Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOH Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOMe Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOMe Cl HCH.sub.2 CHCH.sub.2 H MeO CHMeOMe MeS HCH.sub.2 CHCH.sub.2 H MeO CHMeOMe MeSO HCH.sub.2 CHCH.sub.2 H MeO CHMeOEt Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOCHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOCH.sub.2 CCH Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOCH.sub.2 CH.sub.2 Cl Ms HCH.sub. 2 CHCH.sub.2 H MeO CMe.sub.2 OH Ms HCH.sub.2 CHCH.sub.2 H MeO CMe.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H MeO CMe.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 CH.sub.2 OEt Ms HCH.sub.2 CHCH.sub.2 H MeO CHEtOH Ms HCH.sub.2 CHCH.sub.2 H MeO CHEtOMe Ms HCH.sub.2 CHCH.sub.2 H MeO CHEtOEt Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeNMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCH.sub.2 Ph Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOCH.sub.2 Ph Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCH.sub.2 CO.sub. 2 Me Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCHMeCO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 CN Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 SMe Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 SEt Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 SOMe Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 SO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 SO.sub.2 Et Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeSMe Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OCOMe Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOCOMe Ms HCH.sub.2 CHCH.sub.2 H MeO CH.sub.2 OSO.sub.2 Me Ms HCH.sub.2 CHCH.sub.2 H MeO CHMeOSO.sub.2 Me Ms HCH.sub.2 C CH H MeO CH.sub.2 OH Ms HCH.sub.2 CCH H MeO CH.sub.2 OMe Ms HCH.sub.2 CCH H MeO CH.sub.2 OMe Cl HCH.sub.2 CCH H MeO CH.sub.2 OMe MeS HCH.sub.2 CCH H MeO CH.sub.2 OMe MeSO HCH.sub.2 CCH H MeO CH.sub.2 OEt Ms HCH.sub.2 CCH H MeO CH.sub.2 OEt Cl HCH.sub.2 CCH H MeO CH.sub.2 OEt MeS HCH.sub.2 CCH H MeO CH.sub.2 OEt MeSO HCH.sub.2 CCH H MeO CH.sub.2 OPri Ms HCH.sub.2 C CH H MeO CH.sub.2 OPrn Ms HCH.sub.2 CCH H MeO CH.sub.2 OCHCH.sub.2 Ms HCH.sub.2 CCH H MeO CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CCH H MeO CH.sub.2 OCH.sub.2 CCH Ms HCH.sub.2 CCH H MeO CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CCH H MeO CHMeOH Ms HCH.sub.2 CCH H MeO CHMeOMe Ms HCH.sub.2 CCH H MeO CHMeOMe Cl HCH.sub.2 CCH H MeO CHMeOMe MeS HCH.sub.2 C CH H MeO CHMeOMe MeSO HCH.sub.2 CCH H MeO CHMeOEt Ms HCH.sub.2 CCH H MeO CHMeOCHCH.sub.2 Ms HCH.sub.2 CCH H MeO CHMeOCHCH.sub.2 Ms HCH.sub.2 CCH H MeO CHMeOCH.sub.2 CHCH.sub.2 Ms HCH.sub.2 CCH H MeO CHMeOCH.sub.2 CCH Ms HCH.sub.2 CCH H MeO CHMeOCH.sub.2 CH.sub.2 Cl Ms HCH.sub.2 CCH H MeO CMe.sub.2 OH Ms HCH.sub.2 CCH H MeO CMe.sub.2 OMe Ms HCH.sub.2 CCH H MeO CMe.sub.2 OEt Ms HCH.sub.2 CCH H MeO CH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H MeO CH.sub.2 CH.sub.2 OEt Ms HCH.sub.2 CCH H MeO CHEtOH Ms HCH.sub.2 CCH H MeO CHEtOMe Ms HCH.sub.2 CCH H MeO CHEtOEt Ms HCH.sub.2 CCH H MeO CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H MeO CHMeOCH.sub.2 CH.sub.2 OMe Ms HCH.sub.2 CCH H MeO CH.sub.2 NMe Ms HCH.sub.2 CCH H MeO CHMeNMe.sub.2 Ms HCH.sub.2 CCH H MeO CH.sub.2 CH.sub.2 NMe.sub.2 Ms HCH.sub.2 CCH H MeO CH.sub.2 OCH.sub.2 Ph Ms HCH.sub.2 CCH H MeO CHMeOCH.sub.2 Ph Ms HCH.sub.2 CCH H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HCH.sub.2 CCH H MeO CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HCH.sub.2 CCH H MeO CH.sub.2 OCHMeCO.sub.2 Me Ms HCH.sub.2 CCH H MeO CH.sub.2 CN Ms HCH.sub.2 CCH H MeO CH.sub.2 SMe Ms HCH.sub.2 CCH H MeO CH.sub.2 SEt Ms HCH.sub.2 CCH H MeO CH.sub.2 SOMe Ms HCH.sub.2 CCH H MeO CH.sub.2 SO.sub.2 Me Ms HCH.sub.2 CCH H MeO CH.sub.2 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OCOMe Ms HEt CF.sub.3 Cl CHMeOCOMe Ms HEt CF.sub.3 Cl CH.sub.2 OSO.sub.2 Me Ms HEt CF.sub.3 Cl CHMeOSO.sub.2 Me Ms HPri CF.sub.3 Cl CH.sub.2 OMe Ms HPri CF.sub.3 Cl CH.sub.2 OEt Ms HPri CF.sub.3 Cl CHMeOMe Ms HPri CF.sub.3 Cl CHMeOEt Ms HPri CF.sub.3 Cl CH.sub.2 CH.sub.2 OMe Ms HPri CF.sub.3 Cl CH.sub.2 CH.sub.2 OEt Ms HPri CF.sub.3 Cl CHEtOMe Ms HPri CF.sub.3 Cl CHEtOEt Ms HPri CF.sub.3 Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri CF.sub.3 Cl CH.sub.2 SMe Ms HPri CF.sub.3 Cl CH.sub.2 SEt Ms HPri CF.sub.3 Cl CH.sub.2 SO.sub.2 Me Ms HPri CF.sub.3 Cl CH.sub.2 OCOMe Ms HPri CF.sub.3 Cl CHMeOCOMe Ms HPri CF.sub.3 Cl CH.sub.2 OSO.sub.2 Me Ms HPri CF.sub.3 Cl CHMeOSO.sub.2 Me Ms HMe Et Me CH.sub.2 OMe Ms HMe Et Me CH.sub.2 OEt Ms HMe Et Me CHMeOMe Ms HMe Et Me CHMeOEt Ms HMe Et Me CH.sub.2 CH.sub.2 OMe Ms HMe Et Me CH.sub.2 CH.sub.2 OEt Ms HMe Et Me CHEtOMe Ms HMe Et Me CHEtOEt Ms HMe Et Me CH.sub. 2 OCH.sub.2 CO.sub.2 Me Ms HMe Et Me CH.sub.2 SMe Ms HMe Et Me CH.sub.2 SEt Ms HMe Et Me CH.sub.2 SO.sub.2 Me Ms HMe Et Me CH.sub.2 OCOMe Ms HMe Et Me CHMeOCOMe Ms HMe Et Me CH.sub.2 OSO.sub.2 Me Ms HMe Et Me CHMeOSO.sub.2 Me Ms HEt Et Me CH.sub.2 OMe Ms HEt Et Me CH.sub.2 OEt Ms HEt Et Me CHMeOMe Ms HEt Et Me CHMeOEt Ms HEt Et Me CH.sub.2 CH.sub.2 OMe Ms HEt Et Me CH.sub.2 CH.sub.2 OEt Ms HEt Et Me CHEtOMe Ms HEt Et Me CHEtOEt Ms HEt Et Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Et Me CH.sub.2 SMe Ms HEt Et Me CH.sub.2 SEt Ms HEt Et Me CH.sub.2 SO.sub.2 Me Ms HEt Et Me CH.sub.2 OCOMe Ms HEt Et Me CHMeOCOMe Ms HEt Et Me CH.sub.2 OSO.sub.2 Me Ms HEt Et Me CHMeOSO.sub.2 Me Ms HPri Et Me CH.sub.2 OMe Ms HPri Et Me CH.sub.2 OEt Ms HPri Et Me CHMeOMe Ms HPri Et Me CHMeOEt Ms HPri Et Me CH.sub.2 CH.sub.2 OMe Ms HPri Et Me CH.sub.2 CH.sub.2 OEt Ms HPri Et Me CHEtOMe Ms HPri Et Me CHEtOEt Ms HPri Et Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Et Me CH.sub.2 SMe Ms HPri Et Me CH.sub.2 SEt Ms HPri Et Me CH.sub.2 SO.sub.2 Me Ms HPri Et Me CH.sub.2 OCOMe Ms HPri Et Me CHMeOCOMe Ms HPri Et Me CH.sub.2 OSO.sub.2 Me Ms HPri Et Me CHMeOSO.sub.2 Me Ms HMe Et Cl CH.sub.2 OMe Ms HMe Et Cl CH.sub.2 OEt Ms HMe Et Cl CHMeOMe Ms HMe Et Cl CHMeOEt Ms HMe Et Cl CH.sub.2 CH.sub.2 OMe Ms HMe Et Cl CH.sub.2 CH.sub.2 OEt Ms HMe Et Cl CHEtOMe Ms HMe Et Cl CHEtOEt Ms HMe Et Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe Et Cl CH.sub.2 SMe Ms HMe Et Cl CH.sub.2 SEt Ms HMe Et Cl CH.sub.2 SO.sub.2 Me Ms HMe Et Cl CH.sub.2 OCOMe Ms HMe Et Cl CHMeOCOMe Ms HMe Et Cl CH.sub.2 OSO.sub.2 Me Ms HMe Et Cl CHMeOSO.sub.2 Me Ms H
TABLE 5__________________________________________________________________________ ##STR46##A B X Y Z Q__________________________________________________________________________Et Et Cl CH.sub.2 OMe Ms HEt Et Cl CH.sub.2 OEt Ms HEt Et Cl CHMeOMe Ms HEt Et Cl CHMeOEt Ms HEt Et Cl CH.sub.2 CH.sub.2 OMe Ms HEt Et Cl CH.sub.2 CH.sub.2 OEt Ms HEt Et Cl CHEtOMe Ms HEt Et Cl CHEtOEt Ms HEt Et Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Et Cl CH.sub.2 SMe Ms HEt Et Cl CH.sub.2 SEt Ms HEt Et Cl CH.sub.2 SO.sub.2 Me Ms HEt Et Cl CH.sub.2 OCOMe Ms HEt Et Cl CHMeOCOMe Ms HEt Et Cl CH.sub.2 OSO.sub.2 Me Ms HEt Et Cl CHMeOSO.sub.2 Me Ms HPri Et Cl CH.sub.2 OMe Ms HPri Et Cl CH.sub.2 OEt Ms HPri Et Cl CHMeOMe Ms HPri Et Cl CHMeOEt Ms HPri Et Cl CH.sub.2 CH.sub.2 OMe Ms HPri Et Cl CH.sub.2 CH.sub.2 OEt Ms HPri Et Cl CHEtOMe Ms HPri Et Cl CHEtOEt Ms HPri Et Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Et Cl CH.sub.2 SMe Ms HPri Et Cl CH.sub.2 SEt Ms HPri Et Cl CH.sub.2 SO.sub.2 Me Ms HPri Et Cl CH.sub.2 OCOMe Ms HPri Et Cl CHMeOCOMe Ms HPri Et Cl CH.sub.2 OSO.sub.2 Me Ms HPri Et Cl CHMeOSO.sub.2 Me Ms HMe CH.sub.2 OMe Me CH.sub.2 OMe Ms HMe CH.sub.2 OMe Me CH.sub.2 OEt Ms HMe CH.sub.2 OMe Me CHMeOMe Ms HMe CH.sub.2 OMe Me CHMeOEt Ms HMe CH.sub.2 OMe Me CH.sub.2 CH.sub.2 OMe Ms HMe CH.sub.2 OMe Me CH.sub.2 CH.sub.2 OEt Ms HMe CH.sub.2 OMe Me CHEtOMe Ms HMe CH.sub.2 OMe Me CHEtOEt Ms HMe CH.sub.2 OMe Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe CH.sub.2 OMe Me CH.sub.2 SMe Ms HMe CH.sub.2 OMe Me CH.sub.2 SEt Ms HMe CH.sub.2 OMe Me CH.sub.2 SO.sub.2 Me Ms HMe CH.sub.2 OMe Me CH.sub.2 OCOMe Ms HMe CH.sub.2 OMe Me CHMeOCOMe Ms HMe CH.sub.2 OMe Me CH.sub.2 OSO.sub.2 Me Ms HMe CH.sub.2 OMe Me CHMeOSO.sub.2 Me Ms HEt CH.sub.2 OMe Me CH.sub.2 OMe Ms HEt CH.sub.2 OMe Me CH.sub.2 OEt Ms HEt CH.sub.2 OMe Me CHMeOMe Ms HEt CH.sub.2 OMe Me CHMeOEt Ms HEt CH.sub.2 OMe Me CH.sub.2 CH.sub.2 OMe Ms HEt CH.sub.2 OMe Me CH.sub.2 CH.sub.2 OEt Ms HEt CH.sub.2 OMe Me CHEtOMe Ms HEt CH.sub.2 OMe Me CHEtOEt Ms HEt CH.sub.2 OMe Me CH.sub.2 OCH.sub.2 CO.sub. 2 Me Ms HEt CH.sub.2 OMe Me CH.sub.2 SMe Ms HEt CH.sub.2 OMe Me CH.sub.2 SEt Ms HEt CH.sub.2 OMe Me CH.sub.2 SO.sub.2 Me Ms HEt CH.sub.2 OMe Me CH.sub.2 OCOMe Ms HEt CH.sub.2 OMe Me CHMeOCOMe Ms HEt CH.sub.2 OMe Me CH.sub.2 OSO.sub.2 Me Ms HEt CH.sub.2 OMe Me CHMeOSO.sub.2 Me Ms HPri CH.sub.2 OMe Me CH.sub.2 OMe Ms HPri CH.sub.2 OMe Me CH.sub.2 OEt Ms HPri CH.sub.2 OMe Me CHMeOMe Ms HPri CH.sub.2 OMe Me CHMeOEt Ms HPri CH.sub.2 OMe Me CH.sub.2 CH.sub.2 OMe Ms HPri CH.sub.2 OMe Me CH.sub.2 CH.sub.2 OEt Ms HPri CH.sub.2 OMe Me CHEtOMe Ms HPri CH.sub.2 OMe Me CHEtOEt Ms HPri CH.sub.2 OMe Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri CH.sub.2 OMe Me CH.sub.2 SMe Ms HPri CH.sub.2 OMe Me CH.sub.2 SEt Ms HPri CH.sub. 2 OMe Me CH.sub.2 SO.sub.2 Me Ms HPri CH.sub.2 OMe Me CH.sub.2 OCOMe Ms HPri CH.sub.2 OMe Me CHMeOCOMe Ms HPri CH.sub.2 OMe Me CH.sub.2 OSO.sub.2 Me Ms HPri CH.sub.2 OMe Me CHMeOSO.sub.2 Me Ms HMe CH.sub.2 OMe Cl CH.sub.2 OMe Ms HMe CH.sub.2 OMe Cl CH.sub.2 OEt Ms HMe CH.sub.2 OMe Cl CHMeOMe Ms HMe CH.sub.2 OMe Cl CHMeOEt Ms HMe CH.sub.2 OMe Cl CH.sub.2 CH.sub.2 OMe Ms HMe CH.sub.2 OMe Cl CH.sub.2 CH.sub.2 OEt Ms HMe CH.sub.2 OMe Cl CHEtOMe Ms HMe CH.sub.2 OMe Cl CHEtOEt Ms HMe CH.sub.2 OMe Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe CH.sub.2 OMe Cl CH.sub.2 SMe Ms HMe CH.sub.2 OMe Cl CH.sub.2 SEt Ms HMe CH.sub.2 OMe Cl CH.sub.2 SO.sub.2 Me Ms HMe CH.sub.2 OMe Cl CH.sub.2 OCOMe Ms HMe CH.sub.2 OMe Cl CHMeOCOMe Ms HMe CH.sub.2 OMe Cl CH.sub. 2 OSO.sub.2 Me Ms HMe CH.sub.2 OMe Cl CHMeOSO.sub.2 Me Ms HEt CH.sub.2 OMe Cl CH.sub.2 OMe Ms HEt CH.sub.2 OMe Cl CH.sub.2 OEt Ms HEt CH.sub.2 OMe Cl CHMeOMe Ms HEt CH.sub.2 OMe Cl CHMeOEt Ms HEt CH.sub.2 OMe Cl CH.sub.2 CH.sub.2 OMe Ms HEt CH.sub.2 OMe Cl CH.sub.2 CH.sub.2 OEt Ms HEt CH.sub.2 OMe Cl CHEtOMe Ms HEt CH.sub.2 OMe Cl CHEtOEt Ms HEt CH.sub.2 OMe Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt CH.sub.2 OMe Cl CH.sub.2 SMe Ms HEt CH.sub.2 OMe Cl CH.sub.2 SEt Ms HEt CH.sub.2 OMe Cl CH.sub.2 SO.sub.2 Me Ms HEt CH.sub.2 OMe Cl CH.sub.2 OCOMe Ms HEt CH.sub.2 OMe Cl CHMeOCOMe Ms HEt CH.sub.2 OMe Cl CH.sub.2 OSO.sub.2 Me Ms HEt CH.sub.2 OMe Cl CHMeOSO.sub.2 Me Ms HPri CH.sub.2 OMe Cl CH.sub.2 OMe Ms HPri CH.sub.2 OMe Cl CH.sub.2 OEt Ms HPri CH.sub.2 OMe Cl CHMeOMe Ms HPri CH.sub.2 OMe Cl CHMeOEt Ms HPri CH.sub.2 OMe Cl CH.sub.2 CH.sub.2 OMe Ms HPri CH.sub.2 OMe Cl CH.sub.2 CH.sub.2 OEt Ms HPri CH.sub.2 OMe Cl CHEtOMe Ms HPri CH.sub.2 OMe Cl CHEtOEt Ms HPri CH.sub.2 OMe Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri CH.sub.2 OMe Cl CH.sub.2 SMe Ms HPri CH.sub.2 OMe Cl CH.sub.2 SEt Ms HPri CH.sub.2 OMe Cl CH.sub.2 SO.sub.2 Me Ms HPri CH.sub.2 OMe Cl CH.sub.2 OCOMe Ms HPri CH.sub.2 OMe Cl CHMeOCOMe Ms HPri CH.sub.2 OMe Cl CH.sub.2 OSO.sub.2 Me Ms HPri CH.sub.2 OMe Cl CHMeOSO.sub.2 Me Ms HMe OMe Me CH.sub.2 OMe Ms HMe OMe Me CH.sub.2 OEt Ms HMe OMe Me CHMeOMe Ms HMe OMe Me CHMeOEt Ms HMe OMe Me CH.sub.2 CH.sub.2 OMe Ms HMe OMe Me CH.sub.2 CH.sub. 2 OEt Ms HMe OMe Me CHEtOMe Ms HMe OMe Me CHEtOEt Ms HMe OMe Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe OMe Me CH.sub.2 SMe Ms HMe OMe Me CH.sub.2 SEt Ms HMe OMe Me CH.sub.2 SO.sub.2 Me Ms HMe OMe Me CH.sub.2 OCOMe Ms HMe OMe Me CHMeOCOMe Ms HMe OMe Me CH.sub.2 OSO.sub.2 Me Ms HMe OMe Me CHMeOSO.sub.2 Me Ms HEt OMe Me CH.sub.2 OMe Ms HEt OMe Me CH.sub.2 OEt Ms HEt OMe Me CHMeOMe Ms HEt OMe Me CHMeOEt Ms HEt OMe Me CH.sub.2 CH.sub.2 OMe Ms HEt OMe Me CH.sub.2 CH.sub.2 OEt Ms HEt OMe Me CHEtOMe Ms HEt OMe Me CHEtOEt Ms HEt OMe Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt OMe Me CH.sub.2 SMe Ms HEt OMe Me CH.sub.2 SEt Ms HEt OMe Me CH.sub.2 SO.sub.2 Me Ms HEt OMe Me CH.sub.2 OCOMe Ms HEt OMe Me CHMeOCOMe Ms HEt OMe Me CH.sub.2 OSO.sub.2 Me Ms HEt OMe Me CHMeOSO.sub.2 Me Ms HPri OMe Me CH.sub.2 OMe Ms HPri OMe Me CH.sub.2 OEt Ms HPri OMe Me CHMeOMe Ms HPri OMe Me CHMeOEt Ms HPri OMe Me CH.sub.2 CH.sub.2 OMe Ms HPri OMe Me CH.sub.2 CH.sub.2 OEt Ms HPri OMe Me CHEtOMe Ms HPri OMe Me CHEtOEt Ms HPri OMe Me CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri OMe Me CH.sub.2 SMe Ms HPri OMe Me CH.sub.2 SEt Ms HPri OMe Me CH.sub.2 SO.sub.2 Me Ms HPri OMe Me CH.sub.2 OCOMe Ms HPri OMe Me CHMeOCOMe Ms HPri OMe Me CH.sub.2 OSO.sub.2 Me Ms HPri OMe Me CHMeOSO.sub.2 Me Ms HMe OMe Cl CH.sub.2 OMe Ms HMe OMe Cl CH.sub.2 OEt Ms HMe OMe Cl CHMeOMe Ms HMe OMe Cl CHMeOEt Ms HMe OMe Cl CH.sub.2 CH.sub.2 OMe Ms HMe OMe Cl CH.sub.2 CH.sub.2 OEt Ms HMe OMe Cl CHEtOMe Ms HMe OMe Cl CHEtOEt Ms HMe OMe Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe OMe Cl CH.sub.2 SMe Ms HMe OMe Cl CH.sub.2 SEt Ms HMe OMe Cl CH.sub.2 SO.sub.2 Me Ms HMe OMe Cl CH.sub.2 OCOMe Ms HMe OMe Cl CHMeOCOMe Ms HMe OMe Cl CH.sub.2 OSO.sub.2 Me Ms HMe OMe Cl CHMeOSO.sub.2 Me Ms HEt OMe Cl CH.sub.2 OMe Ms HEt OMe Cl CH.sub.2 OEt Ms HEt OMe Cl CHMeOMe MS HEt OMe Cl CHMeOEt Ms HEt OMe Cl CH.sub.2 CH.sub.2 OMe Ms HEt OMe Cl CH.sub.2 CH.sub.2 OEt Ms HEt OMe Cl CHEtOMe Ms HEt OMe Cl CHEtOEt Ms HEt OMe Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt OMe Cl CH.sub.2 SMe Ms HEt OMe Cl CH.sub.2 SEt Ms HEt OMe Cl CH.sub.2 SO.sub.2 Me Ms HEt OMe Cl CH.sub.2 OCOMe Ms HEt OMe Cl CHMeOCOMe Ms HEt OMe Cl CH.sub.2 OSO.sub.2 Me Ms HEt OMe Cl CHMeOSO.sub.2 Me Ms HPri OMe Cl CH.sub.2 OMe Ms HPri OMe Cl CH.sub.2 OEt Ms HPri OMe Cl CHMeOMe Ms HPri OMe Cl CHMeOEt Ms HPri OMe Cl CH.sub.2 CH.sub.2 OMe Ms HPri OMe Cl CH.sub.2 CH.sub.2 OEt Ms HPri OMe Cl CHEtOMe Ms HPri OMe Cl CHEtOEt Ms HPri OMe Cl CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri OMe Cl CH.sub.2 SMe Ms HPri OMe Cl CH.sub.2 SEt Ms HPri OMe Cl CH.sub.2 SO.sub.2 Me Ms HPri OMe Cl CH.sub.2 OCOMe Ms HPri OMe Cl CHMeOCOMe Ms HPri OMe Cl CH.sub.2 OSO.sub.2 Me Ms HPri OMe Cl CHMeOSO.sub.2 Me Ms HMe SMe Me CH.sub.2 OMe Ms HMe SMe Me CH.sub.2 OEt Ms HMe SMe Me CHMeOMe Ms HMe SMe Me CHMeOEt Ms HMe SMe Me CHEtOMe Ms HMe SMe Me CHEtOEt Ms HMe SMe Me CH.sub.2 OMe Ms HMe SMe Me CH.sub.2 OEt Ms HMe SMe Me CHMeOMe Ms HMe SMe Me CHMeOEt Ms HEt SMe Me CH.sub.2 OMe Ms HEt SMe Me CH.sub.2 OEt Ms HEt SMe Me CHMeOMe Ms HEt SMe Me CHMeOEt Ms HEt SMe Me CHEtOMe Ms HEt SMe Me CHEtOEt Ms HEt SMe Cl CH.sub.2 OMe Ms HEt SMe Cl CH.sub.2 OEt Ms HEt SMe Cl CHMeOMe Ms HEt SMe Cl CHMeOEt Ms HPri SMe Me CH.sub.2 OMe Ms HPri SMe Me CH.sub.2 OEt Ms HPri SMe Me CHMeOMe Ms HPri SMe Me CHMeOEt Ms HPri SMe Me CHEtOMe Ms HPri SMe Me CHEtOEt Ms HPri SMe Cl CH.sub.2 OMe Ms HPri SMe Cl CH.sub.2 OEt Ms HPri SMe Cl CHMeOMe Ms HPri SMe Cl CHMeOEt Ms HMe CH.sub.2 SMe Me CH.sub.2 OMe Ms HMe CH.sub.2 SMe Me CH.sub.2 OEt Ms HMe CH.sub.2 SMe Me CHMeOMe Ms HMe CH.sub.2 SMe Me CHMeOEt Ms HMe CH.sub.2 SMe Me CHEtOMe Ms HMe CH.sub.2 SMe Me CHEtOEt Ms HMe CH.sub.2 SMe Cl CH.sub.2 OMe Ms HMe CH.sub.2 SMe Cl CH.sub.2 OEt Ms HMe CH.sub.2 SMe Cl CHMeOMe Ms HMe CH.sub.2 SMe Cl CHMeOEt Ms HEt CH.sub.2 SMe Me CH.sub.2 OMe Ms HEt CH.sub.2 SMe Me CH.sub.2 OEt Ms HEt CH.sub.2 SMe Me CHMeOMe Ms HEt CH.sub.2 SMe Me CHMeOEt Ms HEt CH.sub.2 SMe Me CHEtOMe Ms HEt CH.sub.2 SMe Me CHEtOEt Ms HEt CH.sub.2 SMe Cl CH.sub.2 OMe Ms HEt CH.sub.2 SMe Cl CH.sub.2 OEt Ms HEt CH.sub.2 SMe Cl CHMeOMe Ms HEt CH.sub.2 SMe Cl CHMeOEt Ms HPri CH.sub.2 SMe Me CH.sub.2 OMe Ms HPri CH.sub.2 SMe Me CH.sub.2 OEt Ms HPri CH.sub.2 SMe Me CHMeOMe Ms HPri CH.sub.2 SMe Me CHMeOEt Ms HPri CH.sub.2 SMe Me CHEtOMe Ms HPri CH.sub.2 SMe Me CHEtOEt Ms HPri CH.sub.2 SMe Cl CH.sub.2 OMe Ms HPri CH.sub.2 SMe Cl CH.sub.2 OEt Ms HPri CH.sub.2 SMe Cl CHMeOMe Ms HPri CH.sub.2 SMe Cl CHMeOEt Ms HMe CH.sub.2 Cl Me CH.sub.2 OMe Ms HMe CH.sub.2 Cl Me CH.sub.2 OEt Ms HMe CH.sub.2 Cl Me CHMeOMe Ms HMe CH.sub.2 Cl Me CHMeOEt Ms HMe CH.sub.2 Cl Me CHEtOMe Ms HMe CH.sub.2 Cl Me CHEtOEt Ms HMe CH.sub.2 Cl Cl CH.sub.2 OMe Ms HMe CH.sub.2 Cl Cl CH.sub.2 OEt Ms HMe CH.sub.2 Cl Cl CHMeOMe Ms HMe CH.sub.2 Cl Cl CHMeOEt Ms HEt CH.sub.2 Cl Me CH.sub.2 OMe Ms HEt CH.sub.2 Cl Me CH.sub.2 OEt Ms HEt CH.sub.2 Cl Me CHMeOMe Ms HEt CH.sub.2 Cl Me CHMeOEt Ms HEt CH.sub.2 Cl Me CHEtOMe Ms HEt CH.sub.2 Cl Me CHEtOEt Ms HEt CH.sub.2 Cl Cl CH.sub.2 OMe Ms HEt CH.sub.2 Cl Cl CH.sub.2 OEt Ms HEt CH.sub.2 Cl Cl CHMeOMe Ms HEt CH.sub.2 Cl Cl CHMeOEt Ms HPri CH.sub.2 Cl Me CH.sub.2 OMe Ms HPri CH.sub.2 Cl Me CH.sub.2 OEt Ms HPri CH.sub.2 Cl Me CHMeOMe Ms HPri CH.sub.2 Cl Me CHMeOEt Ms HPri CH.sub.2 Cl Me CHEtOMe Ms HPri CH.sub.2 Cl Me CHEtOEt Ms HPri CH.sub.2 Cl Cl CH.sub.2 OMe Ms HPri CH.sub.2 Cl Cl CH.sub.2 OEt Ms HPri CH.sub.2 Cl Cl CHMeOMe Ms HPri CH.sub.2 Cl Cl CHMeOEt Ms HMe H CH.sub.2 OMe CH.sub.2 OH Ms HMe H CH.sub.2 OMe CH.sub.2 OMe Ms HMe H CH.sub.2 OMe CH.sub.2 OMe Cl HMe H CH.sub.2 OMe CH.sub.2 OMe MeS HMe H CH.sub.2 OMe CH.sub.2 OMe MeSO HMe H CH.sub.2 OMe CH.sub.2 OEt Ms HMe H CH.sub.2 OMe CH.sub.2 OEt Cl HMe H CH.sub.2 OMe CH.sub.2 OEt MeS HMe H CH.sub.2 OMe CH.sub.2 OEt MeSO HMe H CH.sub.2 OMe CH.sub.2 OPri Ms HMe H CH.sub.2 OMe CH.sub.2 OPrn Ms HMe H CH.sub.2 OMe CH.sub.2 OCHCH.sub.2 Ms HMe H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CCH Ms HMe H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe H CH.sub.2 OMe CHMeOH Ms HMe H CH.sub.2 OMe CHMeOMe Ms HMe H CH.sub.2 OMe CHMeOMe Cl HMe H CH.sub.2 OMe CHMeOMe MeS HMe H CH.sub.2 OMe CHMeOMe MeSO HMe H CH.sub.2 OMe CHMeOEt Ms HMe H CH.sub.2 OMe CHMeOCHCH.sub.2 Ms HMe H CH.sub.2 OMe CHMeOCHCH.sub.2 Ms HMe H CH.sub.2 OMe CHMeOCH.sub.2 CHCH.sub.2 Ms HMe H CH.sub.2 OMe CHMeOCH.sub.2 CH CH Ms HMe H CH.sub.2 OMe CHMeOCH.sub.2 CH.sub.2 Cl Ms HMe H CH.sub.2 OMe CMe.sub.2 OH Ms HMe H CH.sub.2 OMe CMe.sub.2 OMe Ms HMe H CH.sub.2 OMe CMe.sub.2 OEt Ms HMe H CH.sub.2 OMe CH.sub.2 CH.sub.2 OMe Ms HMe H CH.sub.2 OMe CH.sub.2 CH.sub.2 OEt Ms HMe H CH.sub.2 OMe CHEtOH Ms HMe H CH.sub.2 OMe CHEtOMe Ms HMe H CH.sub.2 OMe CHEtOEt Ms HMe H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe H CH.sub.2 OMe CHMeOCH.sub.2 CH.sub.2 OMe Ms HMe H CH.sub.2 OMe CH.sub.2 NMe.sub.2 Ms HMe H CH.sub.2 OMe CHMeNMe.sub.2 Ms HMe H CH.sub.2 OMe CH.sub.2 CH.sub.2 NMe.sub.2 Ms HMe H CH.sub.2 OMe CH.sub.2 OCH.sub.2 Ph Ms HMe H CH.sub.2 OMe CHMeOCH.sub.2 Ph Ms HMe H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe H CH.sub.2 OMe CH.sub.2 OCHMeCO.sub.2 Me Ms HMe H CH.sub.2 OMe CH.sub.2 CN Ms HMe H CH.sub.2 OMe CH.sub.2 SMe Ms HMe H CH.sub.2 OMe CH.sub.2 SEt Ms HMe H CH.sub.2 OMe CH.sub.2 SOMe Ms HMe H CH.sub.2 OMe CH.sub.2 SO.sub.2 Me Ms HMe H CH.sub.2 OMe CH.sub.2 SO.sub.2 Et Ms HMe H CH.sub.2 OMe CHMeSMe Ms HMe H CH.sub.2 OMe CHMeSO.sub.2 ME Ms HMe H CH.sub.2 OMe CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe H CH.sub.2 OMe CH.sub.2 OCOMe Ms HMe H CH.sub.2 OMe CHMeOCOMe Ms HMe H CH.sub.2 OMe CH.sub.OSO.sub.2 Me Ms HMe H CH.sub.2 OMe CHMeOSO.sub.2 Me Ms HEt H CH.sub.2 OMe CH.sub.2 OH Ms HEt H CH.sub.2 OMe CH.sub.2 OMe Ms HEt H CH.sub.2 OMe CH.sub.2 OMe Cl HEt H CH.sub.2 OMe CH.sub.2 OMe MeS HEt H CH.sub.2 OMe CH.sub.2 OMe MeSO HEt H CH.sub.2 OMe CH.sub.2 OEt Ms HEt H CH.sub.2 OMe CH.sub.2 OEt Cl HEt H CH.sub.2 OMe CH.sub.2 OEt MeS HEt H CH.sub.2 OMe CH.sub.2 OEt MeSO HEt H CH.sub.2 OMe CH.sub.2 OPri Ms HEt H CH.sub.2 OMe CH.sub.2 OPrn Ms HEt H CH.sub.2 OMe CH.sub.2 OCHCH.sub.2 Ms HEt H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HEt H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CCH Ms HEt H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt H CH.sub.2 OMe CHMeOH Ms HEt H CH.sub.2 OMe CHMeOMe Ms HEt H CH.sub.2 OMe CHMeOMe Cl HEt H CH.sub.2 OMe CHMeOMe MeS HEt H CH.sub.2 OMe CHMeOMe MeSO HEt H CH.sub.2 OMe CHMeOEt Ms HEt H CH.sub.2 OMe CHMeOCHCH.sub.2 Ms HEt H CH.sub.2 OMe CHMeOCHCH.sub.2 Ms HEt H CH.sub.2 OMe CHMeOCH.sub.2 CH CH.sub.2 Ms HEt H CH.sub.2 OMe CHMeOCH.sub.2 CCH Ms HEt H CH.sub.2 OMe CHMeOCH.sub.2 CH.sub.2 Cl Ms HEt H CH.sub.2 OMe CMe.sub.2 OH Ms HEt H CH.sub.2 OMe CMe.sub.2 OMe Ms HEt H CH.sub.2 OMe CMe.sub.2 OEt Ms HEt H CH.sub.2 OMe CH.sub.2 CH.sub.2 OMe Ms HEt H CH.sub.2 OMe CH.sub.2 CH.sub.2 OEt Ms HEt H CH.sub.2 OMe CHEtOH Ms HEt H CH.sub.2 OMe CHEtOMe Ms HEt H CH.sub.2 OMe CHEtOEt Ms HEt H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt H CH.sub.2 OMe CHMeOCH.sub.2 CH.sub.2 OMe Ms HEt H CH.sub.2 OMe CH.sub.2 NMe.sub.2 Ms HEt H CH.sub.2 OMe CHMeNMe.sub.2 Ms HEt H CH.sub.2 OMe CH.sub.2 CH.sub.2 NMe.sub.2 Ms HEt H CH.sub.2 OMe CH.sub.2 OCH.sub.2 Ph Ms HEt H CH.sub.2 OMe CHMeOCH.sub.2 Ph Ms HEt H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt H CH.sub.2 OMe CH.sub.2 OCHMeCO.sub.2 Me Ms HEt H CH.sub.2 OMe CH.sub.2 CN Ms HEt H CH.sub.2 OMe CH.sub.2 SMe Ms HEt H CH.sub.2 OMe CH.sub.2 SEt Ms HEt H CH.sub.2 OMe CH.sub.2 SOMe Ms HEt H CH.sub.2 OMe CH.sub.2 SO.sub.2 Me Ms HEt H CH.sub.2 OMe CH.sub.2 SO.sub.2 Et Ms HEt H CH.sub.2 OMe CHMeSMe Ms HEt H CH.sub.2 OMe CHMeSO.sub.2 Me Ms HEt H CH.sub.2 OMe CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt H CH.sub.2 OMe CH.sub.2 OCOMe Ms HEt H CH.sub.2 OMe CHMeOCOMe Ms HEt H CH.sub.2 OMe CH.sub.2 OSO.sub.2 Me Ms HEt H CH.sub.2 OMe CHMeOSO.sub.2 Me Ms HPri H CH.sub.2 OMe CH.sub.2 OH Ms HPri H CH.sub.2 OMe CH.sub.2 OMe Ms HPri H CH.sub.2 OMe CH.sub. 2 OMe Cl HPri H CH.sub.2 OMe CH.sub.2 OMe MeS HPri H CH.sub.2 OMe CH.sub.2 OMe MeSO HPri H CH.sub.2 OMe CH.sub.2 OEt Ms HPri H CH.sub.2 OMe CH.sub.2 OEt Cl HPri H CH.sub.2 OMe CH.sub.2 OEt MeS HPri H CH.sub.2 OMe CH.sub.2 OEt MeSO HPri H CH.sub.2 OMe CH.sub.2 OPri Ms HPri H CH.sub.2 OMe CH.sub.2 OPrn Ms HPri H CH.sub.2 OMe CH.sub.2 OCHCH.sub.2 Ms HPri H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CCH Ms HPri H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri H CH.sub.2 OMe CHMeOH Ms HPri H CH.sub.2 OMe CHMeOMe Ms HPri H CH.sub.2 OMe CHMeOMe Cl HPri H CH.sub.2 OMe CHMeOMe MeS HPri H CH.sub. 2 OMe CHMeOMe MeSO HPri H CH.sub.2 OMe CHMeOEt Ms HPri H CH.sub.2 OMe CHMeOCHCH.sub.2 Ms HPri H CH.sub.2 OMe CHMeOCHCH.sub.2 Ms HPri H CH.sub.2 OMe CHMeOCH.sub.2 CHCH.sub.2 Ms HPri H CH.sub.2 OMe CHMeOCH.sub.2 CCH Ms HPri H CH.sub.2 OMe CHMeOCH.sub.2 CH.sub.2 Cl Ms HPri H CH.sub.2 OMe CMe.sub.2 OH Ms HPri H CH.sub.2 OMe CMe.sub.2 OMe Ms HPri H CH.sub.2 OMe CMe.sub.2 OEt Ms HPri H CH.sub.2 OMe CH.sub.2 CH.sub.2 OMe Ms HPri H CH.sub.2 OMe CH.sub.2 CH.sub.2 OEt Ms HPri H CH.sub.2 OMe CHEtOH Ms HPri H CH.sub.2 OMe CHEtOMe Ms HPri H CH.sub.2 OMe CHEtOEt Ms HPri H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri H CH.sub.2 OMe CHMeOCH.sub.2 CH.sub.2 OMe Ms HPri H CH.sub.2 OMe CH.sub.2 NMe.sub.2 Ms HPri H CH.sub.2 OMe CHMeNMe.sub.2 Ms HPri H CH.sub.2 OMe CH.sub.2 CH.sub.2 NMe.sub.2 Ms HPri H CH.sub.2 OMe CH.sub.2 OCH.sub.2 Ph Ms HPri H CH.sub.2 OMe CHMeOCH.sub.2 Ph Ms HPri H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri H CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri H CH.sub.2 OMe CH.sub.2 OCHMeCO.sub.2 ME Ms HPri H CH.sub.2 OMe CH.sub.2 CN Ms HPri H CH.sub.2 OMe CH.sub.2 SMe Ms HPri H CH.sub.2 OMe CH.sub.2 SEt Ms HPri H CH.sub.2 OMe CH.sub.2 SOMe Ms HPri H CH.sub.2 OMe CH.sub.2 SO.sub.2 Me Ms HPri H CH.sub.2 OMe CH.sub.2 SO.sub.2 Et Ms HPri H CH.sub.2 OMe CHMeSMe Ms HPri H CH.sub.2 OMe CHMeSO.sub.2 Me Ms HPri H CH.sub.2 OMe CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HPri H CH.sub.2 OMe CH.sub.2 OCOMe Ms HPri H CH.sub.2 OMe CHMeOCOMe Ms HPri H CH.sub.2 OMe CH.sub.2 OSO.sub.2 Me Ms HPri H CH.sub.2 OMe CHMeOSO.sub.2 Me Ms HMe Me CH.sub.2 OMe CH.sub.2 OH Ms HMe Me CH.sub.2 OMe CH.sub.2 OMe Ms HMe Me CH.sub.2 OMe CH.sub.2 OMe Cl HMe Me CH.sub.2 OMe CH.sub.2 OMe MeS HMe Me CH.sub.2 OMe CH.sub.2 OMe MeSO HMe Me CH.sub.2 OMe CH.sub.2 OEt Ms HMe Me CH.sub.2 OMe CH.sub.2 OEt Cl HMe Me CH.sub.2 OMe CH.sub.2 OEt MeS HMe Me CH.sub.2 OMe CH.sub.2 OEt MeSO HMe Me CH.sub.2 OMe CH.sub.2 OPri Ms HMe Me CH.sub.2 OMe CH.sub.2 OPrn Ms HMe Me CH.sub.2 OMe CH.sub.2 OCHCH.sub.2 Ms HMe Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HMe Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 C CH Ms HMe Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HMe Me CH.sub.2 OMe CHMeOH Ms HMe Me CH.sub.2 OMe CHMeOMe Ms HMe Me CH.sub.2 OMe CHMeOMe Cl HMe Me CH.sub.2 OMe CHMeOMe MeS HMe Me CH.sub.2 OMe CHMeOMe MeSO HMe Me CH.sub.2 OMe CHMeOEt Ms HMe Me CH.sub.2 OMe CH.sub.2 CH.sub.2 OMe Ms HMe Me CH.sub.2 OMe CH.sub.2 CH.sub.2 OEt Ms HMe Me CH.sub.2 OMe CHEtOH Ms HMe Me CH.sub.2 OMe CHEtOMe Ms HMe Me CH.sub.2 OMe CHEtOEt Ms HMe Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HMe Me CH.sub.2 OMe CH.sub.2 NMe.sub.2 Ms HMe Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 Ph Ms HMe Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HMe Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HMe Me CH.sub.2 OMe CH.sub.2 OCHMeCO.sub.2 Me Ms HMe Me CH.sub.2 OMe CH.sub.2 CN Ms HMe Me CH.sub.2 OMe CH.sub.2 SMe Ms HMe Me CH.sub.2 OMe CH.sub.2 SEt Ms HMe Me CH.sub.2 OMe CH.sub.2 SO.sub.2 Me Ms HMe Me CH.sub.2 OMe CH.sub.2 SO.sub.2 Et Ms HMe Me CH.sub.2 OMe CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HMe Me CH.sub.2 OMe CH.sub.2 OCOMe Ms HMe Me CH.sub.2 OMe CHMeOCOMe Ms H
TABLE 5__________________________________________________________________________ ##STR47##A B X Y Z Q__________________________________________________________________________Me Me CH.sub.2 OMe CH.sub.2 OSO.sub.2 Me Ms HMe Me CH.sub.2 OMe CHMeOSO.sub.2 Me Ms HEt Me CH.sub.2 OMe CH.sub.2 OH Ms HEt Me CH.sub.2 OMe CH.sub.2 OMe Ms HEt Me CH.sub.2 OMe CH.sub.2 OMe Cl HEt Me CH.sub.2 OMe CH.sub.2 OMe MeS HEt Me CH.sub.2 OMe CH.sub.2 OMe MeSO HEt Me CH.sub.2 OMe CH.sub.2 OEt Ms HEt Me CH.sub.2 OMe CH.sub.2 OEt Cl HEt Me CH.sub.2 OMe CH.sub.2 OEt MeS HEt Me CH.sub.2 OMe CH.sub.2 OEt MeSO HEt Me CH.sub.2 OMe CH.sub.2 OPri Ms HEt Me CH.sub.2 OMe CH.sub.2 OPrn Ms HEt Me CH.sub.2 OMe CH.sub.2 OCHCH.sub.2 Ms HEt Me CH.sub.2 OMe CH.sub.2 CHCH.sub.2 Ms HEt Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CCH Ms HEt Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HEt Me CH.sub.2 OMe CHMeOH Ms HEt Me CH.sub.2 OMe CHMeOMe Ms HEt Me CH.sub.2 OMe CHMeOMe Cl HEt Me CH.sub.2 OMe CHMeOMe MeS HEt Me CH.sub.2 OMe CHMeOMe MeSO HEt Me CH.sub.2 OMe CHMeOEt Ms HEt Me CH.sub.2 OMe CH.sub.2 CH.sub.2 OMe Ms HEt Me CH.sub.2 OMe CH.sub.2 CH.sub.2 OEt Ms HEt Me CH.sub.2 OMe CHEtOH Ms HEt Me CH.sub.2 OMe CHEtOMe Ms HEt Me CH.sub.2 OMe CHEtOEt Ms HEt Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HEt Me CH.sub.2 OMe CH.sub.2 NMe.sub.2 Ms HEt Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 Ph Ms HEt Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HEt Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HEt Me CH.sub.2 OMe CH.sub.2 OCHMeCO.sub.2 Me Ms HEt Me CH.sub.2 OMe CH.sub.2 CN Ms HEt Me CH.sub.2 OMe CH.sub.2 SMe Ms HEt Me CH.sub.2 OMe CH.sub.2 SEt Ms HEt Me CH.sub.2 OMe CH.sub.2 SO.sub.2 Me Ms HEt Me CH.sub.2 OMe CH.sub.2 SO.sub.2 Et Ms HEt Me CH.sub.2 OMe CH.sub.2 SCH.sub.2 CH.sub.2 OMe Ms HEt Me CH.sub.2 OMe CH.sub.2 OCOMe Ms HEt Me CH.sub.2 OMe CHMeOCOMe Ms HEt Me CH.sub.2 OMe CH.sub.2 OSO.sub.2 Me Ms HEt Me CH.sub.2 OMe CHMeOSO.sub.2 Me Ms HPri Me CH.sub.2 OMe CH.sub.2 OH Ms HPri Me CH.sub.2 OMe CH.sub.2 OMe Ms HPri Me CH.sub.2 OMe CH.sub.2 OMe Cl HPri Me CH.sub.2 OMe CH.sub.2 OMe MeS HPri Me CH.sub.2 OMe CH.sub.2 OMe MeSO HPri Me CH.sub.2 OMe CH.sub.2 OEt Ms HPri Me CH.sub.2 OMe CH.sub.2 OEt Cl HPri Me CH.sub.2 OMe CH.sub.2 OEt MeS HPri Me CH.sub.2 OMe CH.sub.2 OEt MeSO HPri Me CH.sub.2 OMe CH.sub.2 OPri Ms HPri Me CH.sub.2 OMe CH.sub.2 OPrn Ms HPri Me CH.sub.2 OMe CH.sub.2 OCHCH.sub.2 Ms HPri Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CHCH.sub.2 Ms HPri Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CCH Ms HPri Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 Cl Ms HPri Me CH.sub.2 OMe CHMeOH Ms HPri Me CH.sub.2 OMe CHMeOMe Ms HPri Me CH.sub.2 OMe CHMeOMe Cl HPri Me CH.sub.2 OMe CHMeOMe MeS HPri Me CH.sub.2 OMe CHMeOMe MeSO HPri Me CH.sub.2 OMe CHMeOEt Ms HPri Me CH.sub.2 OMe CH.sub.2 CH.sub.2 OMe Ms HPri Me CH.sub.2 OMe CH.sub.2 CH.sub.2 OEt Ms HPri Me CH.sub.2 OMe CHEtOH Ms HPri Me CH.sub.2 OMe CHEtOMe Ms HPri Me CH.sub.2 OMe CHEtOEt Ms HPri Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CH.sub.2 OMe Ms HPri Me CH.sub.2 OMe CH.sub.2 NMe.sub.2 Ms HPri Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 Ph Ms HPri Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Me Ms HPri Me CH.sub.2 OMe CH.sub.2 OCH.sub.2 CO.sub.2 Et Ms HPri Me CH.sub.2 OMe CH.sub.2 OCHMeCO.sub.2 Me Ms HPri Me CH.sub.2 OMe CH.sub.2 CN Ms HPri Me CH.sub.2 OMe CH.sub.2 SMe Ms HPri Me CH.sub.2 OMe CH.sub.2 SEt Ms HPri Me CH.sub.2 OMe CH.sub.2 SO.sub.2 Me Ms HPri Me CH.sub.2 OMe CH.sub.2 SO.sub.2 Et Ms HPri Me CH.sub.2 OMe CH.sub.2 SCH.sub.2 CH.sub. 2 OMe Ms HPri Me CH.sub.2 OMe CH.sub.2 OCOMe Ms HPri Me CH.sub.2 OMe CHMeOCOMe Ms HPri Me CH.sub.2 OMe CH.sub.2 OSO.sub.2 Me Ms HPri Me CH.sub.2 OMe CHMeOSO.sub.2 Me Ms HMe H Pri CH.sub.2 OMe Ms HMe H Pri CH.sub.2 OEt Ms HMe H Pri CHMeOMe Ms HMe H Pri CHMeOEt Ms HMe H Pri CHEtOMe Ms HMe H Pri CHEtOEt Ms HMe H Pri CH.sub.2 SMe Ms HMe H Pri CH.sub.2 SEt Ms HMe H Pri CH.sub.2 SO.sub.2 Me Ms HMe H Pri CH.sub.2 OCOMe Ms HMe H Pri CHMeOCOMe Ms HMe H Pri CH.sub.2 OSO.sub.2 Me Ms HMe H Pri CHMeOSO.sub.2 Me Ms HEt H Pri CH.sub.2 OMe Ms HEt H Pri CH.sub.2 OEt Ms HEt H Pri CHMeOMe Ms HEt H Pri CHMeOEt Ms HEt H Pri CHEtOMe Ms HEt H Pri CHEtOEt Ms HEt H Pri CH.sub.2 SMe Ms HEt H Pri CH.sub.2 SEt Ms HEt H Pri CH.sub.2 SO.sub.2 Me Ms HEt H Pri CH.sub.2 OCOMe Ms HEt H Pri CHMeOCOMe Ms HEt H Pri CH.sub.2 OSO.sub.2 Me Ms HEt H Pri CHMeOSO.sub.2 Me Ms HPri H Pri CH.sub.2 OMe Ms HPri H Pri CH.sub.2 OEt Ms HPri H Pri CHMeOMe Ms HPri H Pri CHMeOEt Ms HPri H Pri CHEtOMe Ms HPri H Pri CHEtOEt Ms HPri H Pri CH.sub.2 SMe Ms HPri H Pri CH.sub.2 SEt Ms HPri H Pri CH.sub.2 SO.sub.2 Me Ms HPri H Pri CH.sub.2 OCOMe Ms HPri H Pri CHMeOCOMe Ms HPri H Pri CH.sub.2 OSO.sub.2 Me Ms HPri H Pri CHMeOSO.sub.2 Me Ms HMe Me Pri CH.sub.2 OMe Ms HMe Me Pri CH.sub.2 OEt Ms HMe Me Pri CHMeOMe Ms HMe Me Pri CHMeOEt Ms HMe Me Pri CH.sub.2 SMe Ms HMe Me Pri CH.sub.2 SO.sub.2 Me Ms HEt Me Pri CH.sub.2 OMe Ms HEt Me Pri CH.sub.2 OEt Ms HEt Me Pri CHMeOMe Ms HEt Me Pri CHMeOEt Ms HEt Me Pri CH.sub.2 SMe Ms HEt Me Pri CH.sub.2 SO.sub.2 Me Ms HPri Me Pri CH.sub.2 OMe Ms HPri Me Pri CH.sub.2 OEt Ms HPri Me Pri CHMeOMe Ms HPri Me Pri CHMeOEt Ms HPri Me Pri CH.sub.2 SMe Ms HPri Me Pri CH.sub.2 SO.sub.2 Me Ms HMe H F CH.sub.2 OMe Ms HMe H F CH.sub.2 OEt Ms HMe H F CHMeOMe Ms HEt H F CH.sub.2 OMe Ms HEt H F CH.sub.2 OEt Ms HEt H F CHMeOMe Ms HEt H F CHMeOEt Ms HPri H F CH.sub.2 OMe Ms HPri H F CH.sub.2 OEt Ms HPri H F CHMeOMe Ms HMe Me F CH.sub.2 OMe Ms HMe Me F CH.sub.2 OEt Ms HEt Me F CH.sub.2 OMe Ms HEt Me F CH.sub.2 OEt Ms HEt Me F CHMeOMe Ms HPri Me F CH.sub.2 OMe Ms HPri Me F CH.sub.2 OEt Ms HMe H NO.sub.2 CH.sub.2 OMe Ms HMe H NO.sub.2 CH.sub.2 OEt Ms HMe H NO.sub.2 CHMeOMe Ms HEt H NO.sub.2 CH.sub.2 OMe Ms HEt H NO.sub.2 CH.sub.2 OEt Ms HEt H NO.sub.2 CHMeOMe Ms HEt H NO.sub.2 CHMeOEt Ms HPri H NO.sub.2 CH.sub.2 OMe Ms HPri H NO.sub.2 CH.sub.2 OEt Ms HPri H NO.sub.2 CHMeOMe Ms HMe Me NO.sub.2 CH.sub.2 OMe Ms HMe Me NO.sub.2 CH.sub.2 OEt Ms HEt Me NO.sub.2 CH.sub.2 OMe Ms HEt Me NO.sub.2 CH.sub.2 OEt Ms HEt Me NO.sub.2 CHMeOMe Ms HPri Me NO.sub.2 CH.sub.2 OMe Ms HPri Me NO.sub.2 CH.sub.2 OEt Ms HMe H CF.sub.3 CH.sub.2 OMe Ms HMe H CF.sub.3 CH.sub.2 OEt Ms HMe H CF.sub.3 CHMeOMe Ms HEt H CF.sub.3 CH.sub.2 OMe Ms HEt H CF.sub.3 CH.sub.2 OEt Ms HEt H CF.sub.3 CHMeOMe Ms HEt H CF.sub.3 CHMeOEt Ms HPri H CF.sub.3 CH.sub.2 OMe Ms HPri H CF.sub.3 CH.sub.2 OEt Ms HPri H CF.sub.3 CHMeOMe Ms HMe Me CF.sub.3 CH.sub.2 OMe Ms HMe Me CF.sub.3 CH.sub.2 OEt Ms HEt Me CF.sub.3 CH.sub.2 OMe Ms HEt Me CF.sub.3 CH.sub.2 OEt Ms HEt Me CF.sub.3 CHMeOMe Ms HPri Me CF.sub.3 CH.sub.2 OMe Ms HPri Me CF.sub.3 CH.sub.2 OEt Ms HMe H COCH.sub.3 CH.sub.2 OMe Ms HMe H COCH.sub.3 CH.sub.2 OEt Ms HEt H COCH.sub.3 CH.sub.2 OMe Ms HEt H COCH.sub.3 CH.sub.2 OEt Ms HEt H COCH.sub.3 CHMeOMe Ms HPri H COCH.sub.3 CH.sub.2 OMe Ms HPri H COCH.sub.3 CH.sub.2 OEt Ms HMe Me COCH.sub.3 CH.sub.2 OMe Ms HEt Me COCH.sub.3 CH.sub.2 OMe Ms HEt Me COCH.sub.3 CH.sub.2 OEt Ms HPri Me COCH.sub.3 CH.sub.2 OMe Ms HMe H SCH.sub.3 CH.sub.2 OMe Ms HMe H SCH.sub.3 CH.sub.2 OEt Ms HEt H SCH.sub.3 CH.sub.2 OMe Ms HEt H SCH.sub.3 CH.sub.2 OEt Ms HEt H SCH.sub.3 CHMeOEt Ms HPri H SCH.sub.3 CH.sub.2 OMe Ms HMe Me SCH.sub.3 CH.sub.2 OMe Ms HEt Me SCH.sub.3 CH.sub.2 OMe Ms HEt Me SCH.sub.3 CH.sub.2 OEt Ms HPri Me SCH.sub.3 CH.sub.2 OMe Ms HMe H OCHF.sub.2 CH.sub.2 OMe Ms HMe H OCHF.sub.2 CH.sub.2 OEt Ms HEt H OCHF.sub.2 CH.sub.2 OMe Ms HEt H OCHF.sub.2 CH.sub.2 OEt Ms HEt H OCHF.sub.2 CHMeOEt Ms HPri H OCHF.sub.2 CH.sub.2 OMe Ms HPri H OCHF.sub.2 CH.sub.2 OEt Ms HMe Me OCHF.sub.2 CH.sub.2 OMe Ms HMe Me OCHF.sub.2 CH.sub.2 OEt Ms HEt Me OCHF.sub.2 CH.sub.2 OMe Ms HEt Me OCHF.sub.2 CH.sub.2 OEt Ms HPri Me OCHF.sub.2 CH.sub.2 OMe Ms HPri Me OCHF.sub.2 CH.sub.2 OEt Ms HMe H OCF.sub.3 CH.sub.2 OMe Ms HMe H OCF.sub.3 CH.sub.2 OEt Ms HEt H OCF.sub.3 CH.sub.2 OMe Ms HEt H OCF.sub.3 CH.sub.2 OEt Ms HEt H OCF.sub.3 CHMeOEt Ms HPri H OCF.sub.3 CH.sub.2 OMe Ms HPri H OCF.sub.3 CH.sub.2 OEt Ms HMe Me OCF.sub.3 CH.sub.2 OMe Ms HEt Me OCF.sub.3 CH.sub.2 OMe Ms HEt Me OCF.sub.3 CH.sub.2 OEt Ms HPri Me OCF.sub.3 CH.sub.2 OMe Ms HMe H CH.sub.2 SMe CH.sub.2 OMe Ms HEt H CH.sub.2 SMe CH.sub.2 OMe Ms HEt H CH.sub.2 SMe CH.sub.2 OEt Ms HEt H CH.sub.2 SMe CHMeOEt Ms HPri H CH.sub.2 SMe CH.sub.2 OMe Ms HPri H CH.sub.2 SMe CHMeOMe Ms HMe Me CH.sub.2 SMe CH.sub.2 OMe Ms HEt Me CH.sub.2 SMe CH.sub.2 OMe Ms HEt Me CH.sub.2 SMe CH.sub.2 OEt Ms HPri Me CH.sub.2 SMe CH.sub.2 OMe Ms HMe H CN CH.sub.2 OMe Ms HEt H CN CH.sub.2 OMe Ms HEt H CN CH.sub.2 OEt Ms HPri H CN CH.sub.2 OMe Ms HMe Me CN CH.sub.2 OMe Ms HEt Me CN CH.sub.2 OMe Ms HPri Me CN CH.sub.2 OMe Ms HMe H CO.sub.2 Me CH.sub.2 OMe Ms HEt H CO.sub.2 Me CH.sub.2 OMe Ms HEt H CO.sub.2 Me CH.sub.2 OEt Ms HPri H CO.sub.2 Me CH.sub.2 OMe Ms HMe Me CO.sub.2 Me CH.sub.2 OMe Ms HEt Me CO.sub.2 Me CH.sub.2 OMe Ms HPri Me CO.sub.2 Me CH.sub.2 OMe Ms HMe H CONMe.sub.2 CH.sub.2 OMe Ms HEt H CONMe.sub.2 CH.sub.2 OMe Ms HPri H CONMe.sub.2 CH.sub.2 OMe Ms HMe H Me CH.sub.2 OMe NO.sub.2 HMe H Me CH.sub.2 OEt NO.sub.2 HEt H Me CH.sub.2 OMe NO.sub.2 HEt H Me CH.sub.2 OEt NO.sub.2 HEt H Me CHMeOMe NO.sub.2 HPri H Me CH.sub.2 OMe NO.sub.2 HPri H Me CH.sub.2 OEt NO.sub.2 HMe H Cl CH.sub.2 OMe NO.sub.2 HMe H Cl CH.sub.2 OEt NO.sub.2 HEt H Cl CH.sub.2 OMe NO.sub.2 HEt H Cl CH.sub.2 OEt NO.sub.2 HEt H Cl CHMeOMe NO.sub.2 HPri H Cl CH.sub.2 OMe NO.sub.2 HPri H Cl CH.sub.2 OEt NO.sub.2 HMe Me Me CH.sub.2 OMe NO.sub.2 HEt Me Me CH.sub.2 OMe NO.sub.2 HEt Me Me CH.sub.2 OEt NO.sub. 2 HPri Me Me CH.sub.2 OMe NO.sub.2 HMe Me Cl CH.sub.2 OMe NO.sub.2 HEt Me Cl CH.sub.2 OMe NO.sub.2 HEt Me Cl CH.sub.2 OEt NO.sub.2 HEt Me Cl CHMeOMe NO.sub.2 HPri Me Cl CH.sub.2 OMe NO.sub.2 HMe H Me CH.sub.2 OMe CF.sub.3 HMe H Me CH.sub.2 OEt CF.sub.3 HEt H Me CH.sub.2 OMe CF.sub.3 HEt H Me CH.sub.2 OEt CF.sub.3 HEt H Me CHMeOMe CF.sub.3 HPri H Me CH.sub.2 OMe CF.sub.3 HPri H Me CH.sub.2 OEt CF.sub.3 HMe H Cl CH.sub.2 OMe CF.sub.3 HMe H Cl CH.sub.2 OEt CF.sub.3 HEt H Cl CH.sub.2 OMe CF.sub.3 HEt H Cl CH.sub.2 OEt CF.sub.3 HEt H Cl CHMeOMe CF.sub.3 HPri H Cl CH.sub.2 OMe CF.sub.3 HPri H Cl CH.sub.2 OEt CF.sub.3 HMe Me Me CH.sub.2 OMe CF.sub.3 HEt Me Me CH.sub.2 OMe CF.sub.3 HEt Me Me CH.sub.2 OEt CF.sub.3 HPri Me Me CH.sub.2 OMe CF.sub.3 HMe Me Cl CH.sub.2 OMe CF.sub.3 HEt Me Cl CH.sub.2 OMe CF.sub.3 HEt Me Cl CH.sub.2 OEt CF.sub.3 HEt Me Cl CHMeOMe CF.sub.3 HPri Me Cl CH.sub.2 OMe CF.sub.3 HMe H Me CH.sub.2 OMe CN HMe H Me CH.sub.2 OEt CN HEt H Me CH.sub.2 OMe CN HEt H Me CH.sub.2 OEt CN HEt H Me CHMeOMe CN HPri H Me CH.sub.2 OMe CN HPri H Me CH.sub.2 OEt CN HMe H Cl CH.sub.2 OMe CN HMe H Cl CH.sub.2 OEt CN HEt H Cl CH.sub.2 OMe CN HEt H Cl CH.sub.2 OEt CN HEt H Cl CHMeOMe CN HPri H Cl CH.sub.2 OMe CN HPri H Cl CH.sub.2 OEt CN HMe Me Me CH.sub.2 OMe CN HEt Me Me CH.sub.2 OMe CN HEt Me Me CH.sub.2 OEt CN HPr i Me Me CH.sub.2 OMe CN HMe Me Cl CH.sub.2 OMe CN HEt Me Cl CH.sub.2 OMe CN HEt Me Cl CH.sub.2 OEt CN HEt Me Cl CHMeOMe CN HPri Me Cl CH.sub.2 OMe CN HMe H Me CH.sub.2 OMe OMe HMe H Me CH.sub.2 OEt OMe HEt H Me CH.sub.2 OMe OMe HEt H Me CH.sub.2 OEt OMe HEt H Me CHMeOMe OME HPri H Me CH.sub.2 OMe OMe HPri H Me CH.sub.2 OEt OMe HMe H Cl CH.sub.2 OMe OMe HMe H Cl CH.sub.2 OEt OMe HEt H Cl CH.sub.2 OMe OMe HEt H Cl CH.sub.2 OEt OMe HEt H Cl CHMeOMe OMe HPri H Cl CH.sub.2 OMe OMe HPri H Cl CH.sub.2 OEt OMe HMe Me Me CH.sub.2 OMe OMe HEt Me Me CH.sub.2 OMe OMe HEt Me Me CH.sub.2 OEt OMe HPri Me Me CH.sub.2 OMe OMe HMe Me Cl CH.sub.2 OMe OMe HEt Me Cl CH.sub.2 OMe OMe HEt Me Cl CH.sub.2 OEt OMe HEt Me Cl CHMeOMe OMe HPri Me Cl CH.sub.2 OMe OMe HMe H Me CH.sub.2 OMe Br HMe H Me CH.sub.2 OEt Br HEt H Me CH.sub.2 OMe Br HEt H Me CH.sub.2 OEt Br HEt H Me CHMeOMe Br HPri H Me CH.sub.2 OMe Br HPri H Me CH.sub.2 OEt Br HMe H Cl CH.sub.2 OMe Br HMe H Cl CH.sub.2 OEt Br HEt H Cl CH.sub.2 OMe Br HEt H Cl CH.sub.2 OEt Br HEt H Cl CHMeOMe Br HPri H Cl CH.sub.2 OMe Br HPri H Cl CH.sub.2 OEt Br HMe Me Me CH.sub.2 OMe Br HEt Me Me CH.sub.2 OMe Br HEt Me Me CH.sub.2 OEt Br HPri Me Me CH.sub.2 OMe Br HMe Me Cl CH.sub.2 OMe Br HEt Me Cl CH.sub.2 OMe Br HEt Me Cl CH.sub.2 OEt Br HEt Me Cl CHMeOMe Br HPri Me Cl CH.sub.2 OMe Br HMe H Me CH.sub.2 OMe I HMe H Me CH.sub.2 OEt I HEt H Me CH.sub.2 OMe I HEt H Me CH.sub.2 OEt I HEt H Me CHMeOMe I HPri H Me CH.sub.2 OMe I HPri H Me CH.sub.2 OEt I HMe H Cl CH.sub.2 OMe I HMe H Cl CH.sub.2 OEt I HEt H Cl CH.sub.2 OMe I HEt H Cl CH.sub.2 OEt I HEt H Cl CHMeOMe I HPri H Cl CH.sub.2 OMe I HPri H Cl CH.sub.2 OEt I HMe Me Me CH.sub.2 OMe I HEt Me Me CH.sub.2 OMe I HEt Me Me CH.sub.2 OEt I HPri Me Me CH.sub.2 OMe I HMe Me Cl CH.sub.2 OMe I HEt Me Cl CH.sub.2 OMe I HEt Me Cl CH.sub.2 OEt I HEt Me Cl CHMeOMe I HPri Me Cl CH.sub.2 OMe I HMe H Me CH.sub.2 OMe SCF.sub.3 HMe H Me CH.sub.2 OEt SCF.sub.3 HEt H Me CH.sub.2 OMe SCF.sub.3 HEt H Me CH.sub.2 OEt SCF.sub.3 HEt H Me CHMeOMe SCF.sub.3 HPri H Me CH.sub.2 OMe SCF.sub.3 HPri H Me CH.sub.2 OEt SCF.sub.3 HMe H Cl CH.sub.2 OMe SCF.sub.3 HMe H Cl CH.sub.2 OEt SCF.sub.3 HEt H Cl CH.sub.2 OMe SCF.sub.3 HEt H Cl CH.sub.2 OEt SCF.sub.3 HEt H Cl CHMeOMe SCF.sub.3 HPri H Cl CH.sub.2 OMe SCF.sub.3 HPri H Cl CH.sub.2 OEt SCF.sub.3 HMe Me Me CH.sub.2 OMe SCF.sub.3 HEt Me Me CH.sub.2 OMe SCF.sub.3 HEt Me Me CH.sub.2 OEt SCF.sub.3 HPri Me Me CH.sub.2 OMe SCF.sub.3 HMe Me Cl CH.sub.2 OMe SCF.sub.3 HEt Me Cl CH.sub.2 OMe SCF.sub.3 HEt Me Cl CH.sub.2 OEt SCF.sub.3 HEt Me Cl CHMeOMe SCF.sub.3 HPri Me Cl CH.sub.2 OMe SCF.sub.3 HMe H Me CH.sub.2 OMe SO.sub.2 CF.sub.3 HMe H Me CH.sub.2 OEt SO.sub.2 CF.sub.3 HEt H Me CH.sub.2 OMe SO.sub.2 CF.sub.3 HEt H Me CH.sub.2 OEt SO.sub.2 CF.sub.3 HEt H Me CHMeOMe SO.sub.2 CF.sub.3 HPri H Me CH.sub.2 OMe SO.sub.2 CF.sub.3 HPri H Me CH.sub.2 OEt SO.sub.2 CF.sub.3 HMe H Cl CH.sub.2 OMe SO.sub.2 CF.sub.3 HMe H Cl CH.sub.2 OEt SO.sub.2 CF.sub.3 HEt H Cl CH.sub.2 OMe SO.sub.2 CF.sub.3 HEt H Cl CH.sub.2 OEt SO.sub.2 CF.sub.3 HEt H Cl CHMeOMe SO.sub.2 CF.sub.3 HPri H Cl CH.sub.2 OMe SO.sub.2 CF.sub.3 HPri H Cl CH.sub.2 OEt SO.sub.2 CF.sub.3 HMe Me Me CH.sub.2 OMe SO.sub.2 CF.sub.3 HEt Me Me CH.sub.2 OMe SO.sub.2 CF.sub.3 HEt Me Me CH.sub.2 OEt SO.sub.2 CF.sub.3 HPri Me Me CH.sub.2 OMe SO.sub.2 CF.sub.3 HMe Me Cl CH.sub.2 OMe SO.sub.2 CF.sub.3 HEt Me Cl CH.sub.2 OMe SO.sub.2 CF.sub.3 HEt Me Cl CH.sub.2 OEt SO.sub.2 CF.sub.3 HEt Me Cl CHMeOMe SO.sub.2 CF.sub.3 HPri Me Cl CH.sub.2 OMe SO.sub.2 CF.sub.3 HMe H Me COOMe Ms NaMe H Me COOMe Ms KMe H Me COOMe Ms Ca.sub.1/2Me H Me COOMe Ms Mg.sub.1/2Me H Me COOMe Ms EtN.sup.+ H.sub.3Me H Me COOMe Ms i-PrN.sup.+ H.sub.3Me H Me COOMe Ms Et.sub.2 N.sup.+ H.sub.2Me H Me COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Me COOMe Ms NaEt H Me COOMe Ms KEt H Me COOMe Ms Ca.sub.1/2Et H Me COOMe Ms Mg.sub.1/2Et H Me COOMe Ms EtN.sup.+ H.sub.3Et H Me COOMe Ms i-PrN.sup.+ H.sub.3Et H Me COOMe Ms Et.sub.2 N.sup.+ H.sub. 2Et H Me COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Me COOMe Ms Nai-Pr H Me COOMe Ms Ki-Pr H Me COOMe Ms Ca.sub.1/2i-Pr H Me COOMe Ms Mg.sub.1/2i-Pr H Me COOMe Ms EtN.sup.+ H.sub.3i-Pr H Me COOMe Ms i-PrN.sup.+ H.sub.3i-Pr H Me COOMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Me COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Me COOMe Ms i-PrN.sup.+ H.sub.3Et Me Me COOMe Ms NaEt Me Me COOMe Ms i-PrN.sup.+ H.sub.3i-Pr Me Me COOMe Ms i-PrN.sup.+ H.sub.3Me H Cl COOMe Ms NaMe H Cl COOMe Ms KMe H Cl COOMe Ms Ca.sub.1/2Me H Cl COOMe Ms Mg.sub.1/2Me H Cl COOMe Ms EtN.sup.+ H.sub.3Me H Cl COOMe Ms i-PrN.sup.+ H.sub.3Me H Cl COOMe Ms Et.sub.2 N.sup.+ H.sub.2Me H Cl COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Cl COOMe Ms NaEt H Cl COOMe Ms KEt H Cl COOMe Ms Ca.sub.1/2Et H Cl COOMe Ms Mg.sub.1/2Et H Cl COOMe Ms EtN.sup.+ H.sub.3Et H Cl COOMe Ms i-PrN.sup.+ H.sub.3Et H Cl COOMe Ms Et.sub.2 N.sup.+ H.sub.2Et H Cl COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Cl COOMe Ms Nai-Pr H Cl COOMe Ms Ki-Pr H Cl COOMe Ms Ca.sub.1/2i-Pr H Cl COOMe Ms Mg.sub.1/2i-Pr H Cl COOMe Ms EtN.sup.+ H.sub.3i-Pr H Cl COOMe Ms i-PrN.sup.+ H.sub.3i-Pr H Cl COOMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Cl COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Cl COOMe Ms i-PrN.sup.+ H.sub.3Et Me Cl COOMe Ms NaEt Me Cl COOMe Ms i-PrN.sup.+ H.sub.3i-Pr Me Cl COOMe Ms i-PrN.sup.+ H.sub.3Me H OMe COOMe Ms NaMe H OMe COOMe Ms KMe H OMe COOMe Ms Ca1/2Me H OMe COOMe Ms Mg.sub.1/2Me H OMe COOMe Ms EtN.sup.+ H.sub.3Me H OMe COOMe Ms i-PrN.sup.+ H.sub.3Me H OMe COOMe Ms Et.sub.2 N.sup.+ H.sub.2Me H OMe COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H OMe COOMe Ms NaEt H OMe COOMe Ms KEt H OMe COOMe Ms Ca.sub.1/2Et H OMe COOMe Ms Mg.sub.1/2Et H OMe COOMe Ms EtN.sup.+ H.sub.3Et H OMe COOMe Ms i-PrN.sup.+ H.sub.3Et H OMe COOMe Ms Et.sub.2 N.sup.+ H.sub.2Et H OMe COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H OMe COOMe Ms Nai-Pr H OMe COOMe Ms Ki-Pr H OMe COOMe Ms Ca.sub.1/2i-Pr H OMe COOMe Ms Mg.sub.1/2i-Pr H OMe COOMe Ms EtN.sup.+ H.sub.3i-Pr H OMe COOMe Ms i-PrN.sup.+ H.sub.3i-Pr H OMe COOMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H OMe COOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OH
TABLE 5__________________________________________________________________________ ##STR48##A B X Y Z Q__________________________________________________________________________Et Me OMe COOMe Ms i-PrN.sup.+ H.sub.3Me H Me COOEt Ms NaMe H Me COOEt Ms KMe H Me COOEt Ms Ca.sub.1/2Me H Me COOEt Ms Mg.sub.1/2Me H Me COOEt Ms EtN.sup.+ H.sub.3Me H Me COOEt Ms i-PrN.sup.+ H.sub.3Me H Me COOEt Ms Et.sub.2 N.sup.+ H.sub.2Me H Me COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Me COOEt Ms NaEt H Me COOEt Ms KEt H Me COOEt Ms Ca.sub.1/2Et H Me COOEt Ms Mg.sub.1/2Et H Me COOEt Ms EtN.sup. + H.sub.3Et H Me COOEt Ms i-PrN.sup.+ H.sub.3Et H Me COOEt Ms Et.sub.2 N.sup.+ H.sub.2Et H Me COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Me COOEt Ms Nai-Pr H Me COOEt Ms Ki-Pr H Me COOEt Ms Ca.sub.1/2i-Pr H Me COOEt Ms Mg.sub.1/2i-Pr H Me COOEt Ms EtN.sup.+ H.sub.3i-Pr H Me COOEt Ms i-PrN.sup.+ H.sub.3i-Pr H Me COOEt Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Me COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Me COOEt Ms i-PrN.sup.+ H.sub.3Et Me Me COOEt Ms NaEt Me Me COOEt Ms i-PrN.sup.+ H.sub.3i-Pr Me Me COOEt Ms i-PrN.sup.+ H.sub.3Me H Cl COOEt Ms NaMe H Cl COOEt Ms KMe H Cl COOEt Ms Ca.sub.1/2Me H Cl COOEt Ms Mg.sub.1/2Me H Cl COOEt Ms EtN.sup.+ H.sub.3Me H Cl COOEt Ms i-PrN.sup.+ H.sub.3Me H Cl COOEt Ms Et.sub.2 N.sup.+ H.sub.2Me H Cl COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Cl COOEt Ms NaEt H Cl COOEt Ms KEt H Cl COOEt Ms Ca.sub.1/2Et H Cl COOEt Ms Mg.sub.1/2Et H Cl COOEt Ms EtN.sup.+ H.sub.3Et H Cl COOEt Ms i-PrN.sup.+ H.sub.3Et H Cl COOEt Ms Et.sub.2 N.sup.+ H.sub.2Et H Cl COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Cl COOEt Ms Nai-Pr H Cl COOEt Ms Ki-Pr H Cl COOEt Ms Ca.sub.1/2i-Pr H Cl COOEt Ms Mg.sub.1/2i-Pr H Cl COOEt Ms EtN.sup.+ H.sub.3i-Pr H Cl COOEt Ms i-PrN.sup.+ H.sub.3i-Pr H Cl COOEt Ms Et.sub.2 N.sup.+ H.sub.3i-Pr H Cl COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Cl COOEt Ms i-PrN.sup.+ H.sub.3Et Me Cl COOEt Ms NaEt Me Cl COOEt Ms i-PrN.sup.+ H.sub.3i-Pr Me Cl COOEt Ms i-PrN.sup.+ H.sub.3Me H OMe COOEt Ms NaMe H OMe COOEt Ms KMe H OMe COOEt Ms Ca.sub.1/2Me H OMe COOEt Ms Mg.sub.1/2Me H OMe COOEt Ms EtN.sup.+ H.sub.3Me H OMe COOEt Ms i-PrN.sup.+ H.sub.3Me H OMe COOEt Ms Et.sub.2 N.sup.+ H.sub.2Me H OMe COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H OMe COOEt Ms NaEt H OMe COOEt Ms KEt H OMe COOEt Ms Ca.sub.1/2Et H OMe COOEt Ms Mg.sub.1/2Et H OMe COOEt Ms EtN.sup.+ H.sub.3Et H OMe COOEt Ms i-PrN.sup.+ H.sub.3Et H OMe COOEt Ms Et.sub.2 N.sup.+ H.sub.2Et H OMe COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H OMe COOEt Ms Nai-Pr H OMe COOEt Ms Ki-Pr H OMe COOEt Ms Ca.sub.1/2i-Pr H OMe COOEt Ms Mg.sub.1/2i-Pr H OMe COOEt Ms EtN.sup.+ H.sub.3i-Pr H OMe COOEt Ms i-PrN.sup.+ H.sub.3i-Pr H OMe COOEt Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H OMe COOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt Me OMe COOEt Ms i-PrN.sup.+ H.sub.3Me H Me COOPri Ms NaMe H Me COOPri Ms KMe H Me COOPri Ms Ca.sub.1/2Me H Me COOPri Ms Mg.sub.1/2Me H Me COOPri Ms EtN.sup.+ H.sub.3Me H Me COOPri Ms i-PrN.sup.+ H.sub.3Me H Me COOPri Ms Et.sub.2 N.sup.+ H.sub.2Me H Me COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Me COOPri Ms NaEt H Me COOPri Ms KEt H Me COOPri Ms Ca.sub.1/2Et H Me COOPri Ms Mg.sub.1/2Et H Me COOPri Ms EtN.sup.+ H.sub.3Et H Me COOPri Ms i-PrN.sup.+ H.sub.3Et H Me COOPri Ms Et.sub.2 N.sup.+ H.sub.2Et H Me COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Me COOPri Ms Nai-Pr H Me COOPri Ms Ki-Pr H Me COOPri Ms Ca.sub.1/2i-Pr H Me COOPri Ms Mg.sub.1/2i-Pr H Me COOPri Ms EtN.sup.+ H.sub.3i-Pr H Me COOPri Ms i-PrN.sup.+ H.sub.3i-Pr H Me COOPri Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Me COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Me COOPri Ms i-PrN.sup.+ H.sub.3Et Me Me COOPri Ms NaEt Me Me COOPri Ms i-PrN.sup.+ H.sub.3i-Pr Me Me COOPri Ms i-PrN.sup.+ H.sub.3Me H Cl COOPri Ms NaMe H Cl COOPri Ms KMe H Cl COOPri Ms Ca.sub.1/2Me H Cl COOPri Ms Mg.sub.1/2Me H Cl COOPri Ms EtN.sup.+ H.sub.3Me H Cl COOPri Ms i-PrN.sup.+ H.sub.3Me H Cl COOPri Ms Et.sub.2 N.sup.+ H.sub.2Me H Cl COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Cl COOPri Ms NaEt H Cl COOPri Ms KEt H Cl COOPri Ms Ca.sub.1/2Et H Cl COOPri Ms Mg.sub.1/2Et H Cl COOPri Ms EtN.sup.+ H.sub.3Et H Cl COOPri Ms i-PrN.sup.+ H.sub.3Et H Cl COOPri Ms Et.sub.2 N.sup.+ H.sub.2Et H Cl COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Cl COOPri Ms Nai-Pr H Cl COOPri Ms Ki-Pr H Cl COOPri Ms Ca.sub.1/2i-Pr H Cl COOPri Ms Mg.sub.1/2i-Pr H Cl COOPri Ms EtN.sup.+ H.sub.3i-Pr H Cl COOPri Ms i-PrN.sup.+ H.sub.3i-Pr H Cl COOPri Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Cl COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Cl COOPri Ms i-PrN.sup.+ H.sub.3Et Me Cl COOPri Ms NaEt Me Cl COOPri Ms i-PrN.sup.+ H.sub.3i-Pr Me Cl COOPri Ms i-PrN.sup.+ H.sub.3Me H OMe COOPri Ms NaMe H OMe COOPri Ms KMe H OMe COOPri Ms Ca.sub.1/2Me H OMe COOPri Ms Mg.sub.1/2Me H OMe COOPri Ms EtN.sup.+ 0 H.sub.3Me H OMe COOPri Ms i-PrN.sup.+ H.sub.3Me H OMe COOPri Ms Et.sub.2 N.sup.+ H.sub.2Me H OMe COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H OMe COOPri Ms NaEt H OMe COOPri Ms KEt H OMe COOPr i Ms Ca.sub.1/2Et H OMe COOPri Ms Mg.sub.1/2Et H OMe COOPri Ms EtN.sup.+ H.sub.3Et H OMe COOPri Ms i-PrN.sup.+ H.sub.3Et H OMe COOPri Ms Et.sub.2 N.sup.+ H.sub.2Et H OMe COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H OMe COOPri Ms Nai-Pr H OMe COOPri Ms Ki-Pr H OMe COOPri Ms Ca.sub.1/2i-Pr H OMe COOPri Ms Mg.sub.1/2i-Pr H OMe COOPri Ms EtN.sup.+ H.sub.3i-Pr H OMe COOPri Ms i-PrN.sup.+ H.sub.3i-Pr H OMe COOPri Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H OMe COOPri Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt Me OMe COOPri Ms i-PrN.sup.+ H.sub.3Me H Me COOCH.sub.2 CH.sub.2 OMe Ms NaMe H Me COOCH.sub.2 CH.sub.2 OMe Ms KMe H Me COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2Me H Me COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2Me H Me COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Me H Me COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H Me COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Me H Me COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Me COOCH.sub.2 CH.sub.2 OMe Ms NaEt H Me COOCH.sub.2 CH.sub.2 OMe Ms KEt H Me COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2Et H Me COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2Et H Me COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Et H Me COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et H Me COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Et H Me COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Me COOCH.sub.2 CH.sub.2 OMe Ms Nai-Pr H Me COOCH.sub.2 CH.sub.2 OMe Ms Ki-Pr H Me COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2i-Pr H Me COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2i-Pr H Me COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3i-Pr H Me COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr H Me COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Me COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Me COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et Me Me COOCH.sub.2 CH.sub.2 OMe Ms NaEt Me Me COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr Me Me COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H Cl COOCH.sub.2 CH.sub.2 OMe Ms NaMe H Cl COOCH.sub.2 CH.sub.2 OMe Ms KMe H Cl COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2Me H Cl COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2Me H Cl COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Me H Cl COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H Cl COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Me H Cl COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Cl COOCH.sub.2 CH.sub.2 OMe Ms NaEt H Cl COOCH.sub.2 CH.sub.2 OMe Ms KEt H Cl COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2Et H Cl COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2Et H Cl COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Et H Cl COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et H Cl COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Et H Cl COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Cl COOCH.sub.2 CH.sub.2 OMe Ms Nai-Pr H Cl COOCH.sub.2 CH.sub.2 OMe Ms Ki-Pr H Cl COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2i-Pr H Cl COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2i-Pr H Cl COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3i-Pr H Cl COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr H Cl COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Cl COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Cl COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et Me Cl COOCH.sub.2 CH.sub.2 OMe Ms NaEt Me Cl COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr Me Cl COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H OMe COOCH.sub.2 CH.sub.2 OMe Ms NaMe H OMe COOCH.sub.2 CH.sub.2 OMe Ms KMe H OMe COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2Me H OMe COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2Me H OMe COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Me H OMe COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H OMe COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Me H OMe COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H OMe COOCH.sub.2 CH.sub.2 OMe Ms NaEt H OMe COOCH.sub.2 CH.sub.2 OMe Ms KEt H OMe COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2Et H OMe COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2Et H OMe COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Et H OMe COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et H OMe COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Et H OMe COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H OMe COOCH.sub.2 CH.sub.2 OMe Ms Nai-Pr H OMe COOCH.sub.2 CH.sub.2 OMe Ms Ki-Pr H OMe COOCH.sub.2 CH.sub.2 OMe Ms Ca.sub.1/2i-Pr H OMe COOCH.sub.2 CH.sub.2 OMe Ms Mg.sub.1/2i-Pr H OMe COOCH.sub.2 CH.sub.2 OMe Ms EtN.sup.+ H.sub.3i-Pr H OMe COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr H OMe COOCH.sub.2 CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H OMe COOCH.sub.2 CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt Me OMe COOCH.sub.2 CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H Me CH.sub.2 OMe Ms NaMe H Me CH.sub.2 OMe Ms KMe H Me CH.sub.2 OMe Ms Ca.sub.1/2Me H Me CH.sub.2 OMe Ms Mg.sub.1/2Me H Me CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Me H Me CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H Me CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Me H Me CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Me CH.sub.2 OMe Ms NaEt H Me CH.sub.2 OMe Ms KEt H Me CH.sub.2 OMe Ms Ca.sub.1/2Et H Me CH.sub.2 OMe Ms Mg.sub.1/2Et H Me CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Et H Me CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et H Me CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Et H Me CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Me CH.sub.2 OMe Ms Nai-Pr H Me CH.sub.2 OMe Ms Ki-Pr H Me CH.sub.2 OMe Ms Ca.sub.1/2i-Pr H Me CH.sub.2 OMe Ms Mg.sub.1/2i-Pr H Me CH.sub.2 OMe Ms EtN.sup.+ H.sub.3i-Pr H Me CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr H Me CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Me CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Me CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et Me Me CH.sub.2 OMe Ms NaEt Me Me CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr Me Me CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H Cl CH.sub.2 OMe Ms NaMe H Cl CH.sub.2 OMe Ms KMe H Cl CH.sub.2 OMe Ms Ca.sub.1/2Me H Cl CH.sub.2 OMe Ms Mg.sub.1/2Me H Cl CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Me H Cl CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H Cl CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Me H Cl CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Cl CH.sub.2 OMe Ms NaEt H Cl CH.sub.2 OMe Ms KEt H Cl CH.sub.2 OMe Ms Ca.sub.1/2Et H Cl CH.sub.2 OMe Ms Mg.sub.1/2Et H Cl CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Et H Cl CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et H Cl CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Et H Cl CH.sub. 2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Cl CH.sub.2 OMe Ms Nai-Pr H Cl CH.sub.2 OMe Ms Ki-Pr H Cl CH.sub.2 OMe Ms Ca.sub.1/2i-Pr H Cl CH.sub.2 OMe Ms Mg.sub.1/2i-Pr H Cl CH.sub.2 OMe Ms EtN.sup.+ H.sub.3i-Pr H Cl CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr H Cl CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Cl CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Cl CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et Me Cl CH.sub.2 OMe Ms NaEt Me Cl CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr Me Cl CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H OMe CH.sub.2 OMe Ms NaMe H OMe CH.sub.2 OMe Ms KMe H OMe CH.sub.2 OMe Ms Ca.sub.1/2Me H OMe CH.sub.2 OMe Ms Mg.sub.1/2Me H OMe CH.sub.2 OMe Ms EtN.sup. + H.sub.3Me H OMe CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H OMe CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Me H OMe CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H OMe CH.sub.2 OMe Ms NaEt H OMe CH.sub.2 OMe Ms KEt H OMe CH.sub.2 OMe Ms Ca.sub.1/2Et H OMe CH.sub.2 OMe Ms Mg.sub.1/2Et H OMe CH.sub.2 OMe Ms EtN.sup.+ H.sub.3Et H OMe CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Et H OMe CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2Et H OMe CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H OMe CH.sub.2 OMe Ms Nai-Pr H OMe CH.sub.2 OMe Ms Ki-Pr H OMe CH.sub.2 OMe Ms Ca.sub.1/2i-Pr H OMe CH.sub.2 OMe Ms Mg.sub.1/2i-Pr H OMe CH.sub.2 OMe Ms EtN.sup.+ H.sub.3i-Pr H OMe CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3i-Pr H OMe CH.sub.2 OMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H OMe CH.sub.2 OMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt Me OMe CH.sub.2 OMe Ms i-PrN.sup.+ H.sub.3Me H Me CH.sub.2 OEt Ms NaMe H Me CH.sub.2 OEt Ms KMe H Me CH.sub.2 OEt Ms Ca.sub.1/2Me H Me CH.sub.2 OEt Ms Mg.sub.1/2Me H Me CH.sub.2 OEt Ms EtN.sup.+ H.sub.3Me H Me CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Me H Me CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2Me H Me CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Me CH.sub.2 OEt Ms NaEt H Me CH.sub.2 OEt Ms KEt H Me CH.sub.2 OEt Ms Ca.sub.1/2Et H Me CH.sub.2 OEt Ms Mg.sub.1/2Et H Me CH.sub.2 OEt Ms EtN.sup.+ H.sub.3Et H Me CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Et H Me CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2Et H Me CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Me CH.sub.2 OEt Ms Nai-Pr H Me CH.sub.2 OEt Ms Ki-Pr H Me CH.sub.2 OEt Ms Ca.sub.1/2i-Pr H Me CH.sub.2 OEt Ms Mg.sub.1/2i-Pr H Me CH.sub.2 OEt Ms EtN.sup.+ H.sub.3i-Pr H Me CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3i-Pr H Me CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Me CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Me CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Et Me Me CH.sub.2 OEt Ms NaEt Me Me CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3i-Pr Me Me CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Me H Cl CH.sub.2 OEt Ms NaMe H Cl CH.sub.2 OEt Ms KMe H Cl CH.sub.2 OEt Ms Ca.sub.1/2Me H Cl CH.sub.2 OEt Ms Mg.sub.1/2Me H Cl CH.sub.2 OEt Ms EtN.sup.+ H.sub.3Me H Cl CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Me H Cl CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2Me H Cl CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Cl CH.sub.2 OEt Ms NaEt H Cl CH.sub.2 OEt Ms KEt H Cl CH.sub.2 OEt Ms Ca.sub.1/2Et H Cl CH.sub.2 OEt Ms Mg.sub.1/2Et H Cl CH.sub.2 OEt Ms EtN.sup.+ H.sub.3Et H Cl CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Et H Cl CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2Et H Cl CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Cl CH.sub.2 OEt Ms Nai-Pr H Cl CH.sub.2 OEt Ms Ki-Pr H Cl CH.sub.2 OEt Ms Ca.sub. 1/2i-Pr H Cl CH.sub.2 OEt Ms Mg.sub.1/2i-Pr H Cl CH.sub.2 OEt Ms EtN.sup.+ H.sub.3i-Pr H Cl CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3i-Pr H Cl CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Cl CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Cl CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Et Me Cl CH.sub.2 OEt Ms NaEt Me Cl CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3i-Pr Me Cl CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Me H OMe CH.sub.2 OEt Ms NaMe H OMe CH.sub.2 OEt Ms KMe H OMe CH.sub.2 OEt Ms Ca.sub.1/2Me H OMe CH.sub.2 OEt Ms Mg.sub.1/2Me H OMe CH.sub.2 OEt Ms EtN.sup.+ H.sub.3Me H OMe CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Me H OMe CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2Me H OMe CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H OMe CH.sub.2 OEt Ms NaEt H OMe CH.sub.2 OEt Ms KEt H OMe CH.sub.2 OEt Ms Ca.sub.1/2Et H OMe CH.sub.2 OEt Ms Mg.sub.1/2Et H OMe CH.sub.2 OEt Ms EtN.sup.+ H.sub.3Et H OMe CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Et H OMe CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2Et H OMe CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H OMe CH.sub.2 OEt Ms Nai-Pr H OMe CH.sub.2 OEt Ms Ki-Pr H OMe CH.sub.2 OEt Ms Ca.sub.1/2i-Pr H OMe CH.sub.2 OEt Ms Mg.sub.1/2i-Pr H OMe CH.sub.2 OEt Ms EtN.sup.+ H.sub.3i-Pr H OMe CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3i-Pr H OMe CH.sub.2 OEt Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H OMe CH.sub.2 OEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt Me OMe CH.sub.2 OEt Ms i-PrN.sup.+ H.sub.3Me H Me CHMeOMe Ms NaMe H Me CHMeOMe Ms KMe H Me CHMeOMe Ms Ca.sub.1/2Me H Me CHMeOMe Ms Mg.sub.1/2Me H Me CHMeOMe Ms EtN.sup.+ H.sub.3Me H Me CHMeOMe Ms i-PrN.sup.+ H.sub.3Me H Me CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2Me H Me CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Me CHMeOMe Ms NaEt H Me CHMeOMe Ms KEt H Me CHMeOMe Ms Ca.sub.1/2Et H Me CHMeOMe Ms Mg.sub.1/2Et H Me CHMeOMe Ms EtN.sup.+ H.sub.3Et H Me CHMeOMe Ms i-PrN.sup.+ H.sub.3Et H Me CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2Et H Me CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Me CHMeOMe Ms Nai-Pr H Me CHMeOMe Ms Ki-Pr H Me CHMeOMe Ms Ca.sub.1/2i-Pr H Me CHMeOMe Ms Mg.sub. 1/2i-Pr H Me CHMeOMe Ms EtN.sup.+ H.sub.3i-Pr H Me CHMeOMe Ms i-PrN.sup.+ H.sub.3i-Pr H Me CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Me CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Me CHMeOMe Ms i-PrN.sup.+ H.sub.3Et Me Me CHMeOMe Ms NaEt Me Me CHMeOMe Ms i-PrN.sup.+ H.sub.3i-Pr Me Me CHMeOMe Ms i-PrN.sup.+ H.sub.3Me H Cl CHMeOMe Ms NaMe H Cl CHMeOMe Ms KMe H Cl CHMeOMe Ms Ca.sub.1/2Me H Cl CHMeOMe Ms Mg.sub.1/2Me H Cl CHMeOMe Ms EtN.sup.+ H.sub.3Me H Cl CHMeOMe Ms i-PrN.sup.+ H.sub.3Me H Cl CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2Me H Cl CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Cl CHMeOMe Ms NaEt H Cl CHMeOMe Ms KEt H Cl CHMeOMe Ms Ca.sub.1/2Et H Cl CHMeOMe Ms Mg.sub.1/2Et H Cl CHMeOMe Ms EtN.sup.+ H.sub.3Et H Cl CHMeOMe Ms i-PrN.sup.+ H.sub.3Et H Cl CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2Et H Cl CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Cl CHMeOMe Ms Nai-Pr H Cl CHMeOMe Ms Ki-Pr H Cl CHMeOMe Ms Ca.sub.1/2i-Pr H Cl CHMeOMe Ms Mg.sub.1/2i-Pr H Cl CHMeOMe Ms EtN.sup.+ H.sub.3i-Pr H Cl CHMeOMe Ms i-PrN.sup.+ H.sub.3i-Pr H Cl CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Cl CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Cl CHMeOMe Ms i-PrN.sup.+ H.sub.3Et Me Cl CHMeOMe Ms NaEt Me Cl CHMeOMe Ms i-PrN.sup.+ H.sub.3i-Pr Me Cl CHMeOMe Ms i-PrN.sup.+ H.sub.3Me H OMe CHMeOMe Ms NaMe H OMe CHMeOMe Ms KMe H OMe CHMeOMe Ms Ca.sub.1/2Me H OMe CHMeOMe Ms Mg.sub.1/2Me H OMe CHMeOMe Ms EtN.sup.+ H.sub.3Me H OMe CHMeOMe Ms i-PrN.sup.+ H.sub.3Me H OMe CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2Me H OMe CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H OMe CHMeOMe Ms NaEt H OMe CHMeOMe Ms KEt H OMe CHMeOMe Ms Ca.sub.1/2Et H OMe CHMeOMe Ms Mg.sub.1/2Et H OMe CHMeOMe Ms EtN.sup.+ H.sub.3Et H OMe CHMeOMe Ms i-PrN.sup.+ H.sub.3Et H OMe CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2Et H OMe CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H OMe CHMeOMe Ms Nai-Pr H OMe CHMeOMe Ms Ki-Pr H OMe CHMeOMe Ms Ca.sub.1/2i-Pr H OMe CHMeOMe Ms Mg.sub.1/2i-Pr H OMe CHMeOMe Ms EtN.sup.+ H.sub.3i-Pr H OMe CHMeOMe Ms i-PrN.sup.+ H.sub.3i-Pr H OMe CHMeOMe Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H OMe CHMeOMe Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt Me OMe CHMeOMe Ms i-PrN.sup.+ H.sub.3Me H Me CHMeOEt Ms NaMe H Me CHMeOEt Ms KMe H Me CHMeOEt Ms Ca.sub.1/2Me H Me CHMeOEt Ms Mg.sub.1/2Me H Me CHMeOEt Ms EtN.sup.+ H.sub.3Me H Me CHMeOEt Ms i-PrN.sup.+ H.sub.3Me H Me CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2Me H Me CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Me CHMeOEt Ms NaEt H Me CHMeOEt Ms KEt H Me CHMeOEt Ms Ca.sub.1/2Et H Me CHMeOEt Ms Mg.sub.1/2Et H Me CHMeOEt Ms EtN.sup.+ H.sub.3Et H Me CHMeOEt Ms i-PrN.sup.+ H.sub.3Et H Me CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2Et H Me CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Me CHMeOEt Ms Nai-Pr H Me CHMeOEt Ms Ki-Pr H Me CHMeOEt Ms Ca.sub.1/2i-Pr H Me CHMeOEt Ms Mg.sub. 1/2i-Pr H Me CHMeOEt Ms EtN.sup.+ H.sub.3i-Pr H Me CHMeOEt Ms i-PrN.sup.+ H.sub.3i-Pr H Me CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Me CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Me CHMeOEt Ms i-PrN.sup.+ H.sub.3Et Me Me CHMeOEt Ms NaEt Me Me CHMeOEt Ms i-PrN.sup.+ H.sub.3i-Pr Me Me CHMeOEt Ms i-PrN.sup.+ H.sub.3Me H Cl CHMeOEt Ms NaMe H Cl CHMeOEt Ms KMe H Cl CHMeOEt Ms Ca.sub.1/2Me H Cl CHMeOEt Ms Mg.sub.1/2Me H Cl CHMeOEt Ms EtN.sup.+ H.sub.3Me H Cl CHMeOEt Ms i-PrN.sup.+ H.sub.3Me H Cl CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2Me H Cl CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H Cl CHMeOEt Ms NaEt H Cl CHMeOEt Ms KEt H Cl CHMeOEt Ms Ca.sub.1/2Et H Cl CHMeOEt Ms Mg.sub.1/2Et H Cl CHMeOEt Ms EtN.sup.+ H.sub.3Et H Cl CHMeOEt Ms i-PrN.sup.+ H.sub.3Et H Cl CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2Et H Cl CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H Cl CHMeOEt Ms Nai-Pr H Cl CHMeOEt Ms Ki-Pr H Cl CHMeOEt Ms Ca.sub.1/2i-Pr H Cl CHMeOEt Ms Mg.sub.1/2i-Pr H Cl CHMeOEt Ms EtN.sup.+ H.sub.3i-Pr H Cl CHMeOEt Ms i-PrN.sup.+ H.sub.3i-Pr H Cl CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H Cl CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHMe Me Cl CHMeOEt Ms i-PrN.sup.+ H.sub.3Et Me Cl CHMeOEt Ms NaEt Me Cl CHMeOEt Ms i-PrN.sup.+ H.sub.3i-Pr Me Cl CHMeOEt Ms i-PrN.sup.+ H.sub.3Me H OMe CHMeOEt Ms NaMe H OMe CHMeOEt Ms KMe H OMe CHMeOEt Ms Ca.sub.1/2Me H OMe CHMeOEt Ms Mg.sub.1/2Me H OMe CHMeOEt Ms EtN.sup.+ H.sub.3Me H OMe CHMeOEt Ms i-PrN.sup.+ H.sub.3Me H OMe CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2Me H OMe CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt H OMe CHMeOEt Ms NaEt H OMe CHMeOEt Ms KEt H OMe CHMeOEt Ms Ca.sub.1/2Et H OMe CHMeOEt Ms Mg.sub.1/2Et H OMe CHMeOEt Ms EtN.sup.+ H.sub.3Et H OMe CHMeOEt Ms i-PrN.sup.+ H.sub.3Et H OMe CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2Et H OMe CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHi-Pr H OMe CHMeOEt Ms Nai-Pr H OMe CHMeOEt Ms Ki-Pr H OMe CHMeOEt Ms Ca.sub.1/2i-Pr H OMe CHMeOEt Ms Mg.sub.1/2i-Pr H OMe CHMeOEt Ms EtN.sup.+ H.sub.3i-Pr H OMe CHMeOEt Ms i-PrN.sup.+ H.sub.3i-Pr H OMe CHMeOEt Ms Et.sub.2 N.sup.+ H.sub.2i-Pr H OMe CHMeOEt Ms Me.sub.3 N.sup.+ CH.sub.2 CH.sub.2 OHEt Me OMe CHMeOEt Ms i-PrN.sup.+ H.sub.3__________________________________________________________________________
When the compound of the present invention is to be used as an agricultural or horticultural herbicide, it is usually mixed with a suitable carrier, for instance, a solid carrier such as clay, talc, bentonite or diatomaceous earth, or a liquid carrier such as water, an alcohol (such as methanol or ethanol), an aromatic hydrocarbon (such as benzene, toluene or xylene), a chlorinated hydrocarbon, an ether, a ketone, an ester (such as ethyl acetate) or an acid amide (such as dimethylformamide). If desired, an emulsifier, a dispersing agent, a suspending agent, a penetrating agent, a spreader or a stabilizer may be added to prepare an optional formulation such as a liquid formulation, an emulsifiable concentrate, a wettable powder, a dust, a granule or a flowable.
Further, if desired, other herbicides, various insecticides, bacteriocides, plant regulating agents or synergism agents may be combined at the time of the preparation of the formulations or at a time of the application of the herbicides.
As other herbicides to be combined with the herbicide of the present invention, there may be mentioned, for instance, compounds disclosed in Farm Chemicals Handbook, the 73rd Edition (1987). Among them, there may be mentioned, for example, atrazine, cyanazine, alachlor, metolachlor, EPTC, 2,4-D, butylate, dicamba, bromoxynil and tridiphane. Further, N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-3-chloro-4-methoxycarbonyl-1-methylpyrazole-5-sulfonamide or N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-3-bromo-4-methoxycarbonyl-1-methylpyrazole-5-sulfonamide as disclosed in U.S. Pat. No. 4,668,277 may also be combined with the herbicide of the present invention.
The dose varies depending upon the application site, the season for application, the method for application, the type of the crop plant, etc. In general, however, the dose is usually within a range of from 0.001 to 10 kg per hectare as the amount of the active ingredient.
Now, Formulation Examples of the herbicides containing the compounds of the present invention as active ingredients, will be given. However, it should be understood that the present invention is by no means restricted to such specific Examples. In the following Formulation Examples, "parts" means "parts by weight".
______________________________________FORMULATION EXAMPLE 1: Wettable powder______________________________________Compound No. 3 of the present invention 60 partsZeeklite PFP (tradename for a kaolin-type 33 partsclay, manufactured by Zeeklite Industries,Co., Ltd.)Sorpol 5039 (tradename for a mixture of a 5 partsnonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)Carplex (tradename for a coagulation- 2 partspreventing agent composed of a mixture ofa surfactant and fine silica powder,manufactured by Shionogi PharmaceuticalCo., Ltd.)______________________________________
The above ingredients are homogeneously pulverized and mixed to form a wettable powder.
______________________________________FORMULATION EXAMPLE 2: Wettable powderCompound No. 7 of the present invention 60 partsZeeklite PFP (tradename for a kaolin-type 33 partsclay, manufactured by Zeeklite Industries,Co., Ltd.)Sorpol 5039 (tradename for a mixture of a 5 partsnonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)Carplex (tradename for a coagulation- 2 partspreventing agent composed of a mixture ofa surfactant and fine silica powder,manufactured by Shionogi PharmaceuticalCo., Ltd.)FORMULATION EXAMPLE 3: Wettable powderCompound No. 15 of the present invention 60 partsZeeklite PFP (tradename for a kaolin-type 33 partsclay, manufactured by Zeeklite Industries,Co., Ltd.)Sorpol 5039 (tradename for a mixture of a 5 partsnonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)Carplex (tradename for a coagulation- 2 partspreventing agent composed of a mixture ofa surfactant and fine silica powder,manufactured by Shionogi PharmaceuticalCo., Ltd.)FORMULATION EXAMPLE 4: Wettable powderCompound No. 21 of the present invention 60 partsZeeklite PFP (tradename for a kaolin-type 33 partsclay, manufactured by Zeeklite Industries,Co., Ltd.)Sorpol 5039 (tradename for a mixture of a 5 partsnonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)Carplex (tradename for a coagulation- 2 partspreventing agent composed of a mixture ofa surfactant and fine silica powder,manufactured by Shionogi PharmaceuticalCo., Ltd.)FORMULATION EXAMPLE 5: Wettable powderCompound No. 25 of the present invention 60 partsZeeklite PFP (tradename for a kaolin-type 33 partsclay, manufactured by Zeeklite Industries,Co., Ltd.)Sorpol 5039 (tradename for a mixture of a 5 partsnonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)Carplex (tradename for a coagulation- 2 partspreventing agent composed of a mixture ofa surfactant and fine silica powder,manufactured by Shionogi PharmaceuticalCo., Ltd.)FORMULATION EXAMPLE 6: Wettable powderCompound No. 35 of the present invention 60 partsZeeklite PFP (tradename for a kaolin-type 33 partsclay, manufactured by Zeeklite Industries,Co., Ltd.)Sorpol 5039 (tradename for a mixture of a 5 partsnonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)Carplex (tradename for a coagulation- 2 partspreventing agent composed of a mixture ofa surfactant and fine silica powder,manufactured by Shionogi PharmaceuticalCo., Ltd.)FORMULATION EXAMPLE 7: Emulsifiable concentrateCompound No. 3 of the present invention 1.5 partsXylene 78.5 partsN,N--dimethylformamide 15 partsSorpol 2680 (tradename for a mixture of 5 partsa nonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)______________________________________
The above ingredients are homogeneously mixed to obtain an emulsifiable concentrate.
______________________________________FORMULATION EXAMPLE 8: Emulsifiable concentrateCompound No. 11 of the present invention 1.5 partsXylene 78.5 partsN,N--dimethylformamide 15 partsSorpol 2680 (tradename for a mixture of 5 partsa nonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)FORMULATION EXAMPLE 9: FlowableCompuund No. 3 of the present invention 40 partsAgrizole B-710 (tradename for a nonionic 10 partssurfactant, manufactured by Kao Corporation)Runox 1000C (tradename for an anionic 0.5 partsurfactant, manufactured by Toho ChemicalCo., Ltd.)1% Rodopol water (tradename for a 20 partsthickener, manufactured by Rhone-Poulenc)Water 29.5 parts______________________________________
The above ingredients are homogeneously mixed to form a flowable.
______________________________________FORMULATION EXAMPLE 10: FlowableCompound No. 10 of the present invention 40 partsAgrizole B-710 (tradename for a nonionic 10 partssurfactant, manufactured by Kao Corporation)Runox 1000C (tradename for an anionic 0.5 partsurfactant, manufactured by Toho ChemicalCo., Ltd.)1% Rodopol water (tradename for a 20 partsthickener, manufactured by Rhone-Poulenc)Water 29.5 partsFORMULATION EXAMPLE 11: Liquid formulationCompound No. 39 of the present invention 30 partsNippol (tradename for a nonionic surfactant, 10 partsmanufactured by Nissan Chemical Industries,Ltd.)Water 60 parts______________________________________
The above ingredients are homogeneously mixed to obtain a liquid formulation.
______________________________________FORMULATION EXAMPLE 12: Liquid formulationCompound No. 40 of the present invention 30 partsNippol (tradename for a nonionic surfactant,manufactured by Nissan Chemical Industries,Ltd.) 10 partsWater 60 partsFORMULATION EXAMPLE 13: Liquid formulationCompound No. 46 of the present invention 30 partsNippol (tradename for a nonionic surfactant,manufactured by Nissan Chemical Industries,Ltd.) 10 partsWater 60 partsFORMULATION EXAMPLE 14: Liquid formulationCompound No. 41 of the present invention 10 partsSorpol W-150 (tradename for a nonionicsurfactant, manufactured by TohoChemical Co., Ltd.) 10 partsWater 80 parts______________________________________
The above ingredients are homogeneously mixed to form a liquid formulation.
In their use, the above wettable powders, emulsifiable concentrates, flowables or liquid formulations are diluted with water from 50 to 1,000 times and applied so that the respective active ingredients will be from 0.001 to 5 kg per hectare.
The compounds of the present invention are applicable not only to agricultural and horticultural fields such as upland fields, paddy fields and orchards, but to non-agricultural fields such as athletic fields, vacant fields and railway sides for the control of various weeds. The dose in their application varies depending upon the application site, the season for application, the type of crop plants, etc. However, it is usually within a range of from 0.001 to 5 kg per hectare.
Now, the herbicidal activities of the compounds of the present invention will be described with respect to specific Test Examples.
TEST EXAMPLE 1
Test on the herbicidal effects in soil treatment
A plastic box having a length of 15 cm, a width of 22 cm and a depth of 6 cm was filled with a sterilized diluvium soil, and seeds Echinochloa crus-galli, Setaria viridis, Eleusine indica, Digitaria adscendens, Panicum dichotomiflorum, Abutilon theophrasti, Amaranthus lividus, Polygonum longisetum and Zea mays were sown, and tubers of Cyperus esculentus were further planted. The soil was covered thereon in the thickness of about 1.5 cm, and then a herbicide solution was applied onto the surface of the soil uniformly so that the active ingredient is distributed at a predetermined concentration. The herbicide solution was prepared by diluting the wettable powder, the emulsifiable concentrate, the liquid formulation or the flowable as described in the foregoing Formulation Examples with water and applied onto the entire soil surface by means of a small spray. Three weeks after the application of the herbicidal solution, the herbicidal effects against each weed were determined on the basis of the following standard ratings. The results thereby obtained are shown in Table 6. The Compounds Nos. correspond to the Compound Nos. in Table 3.
Standard ratings:
5: Growth control rate of more than 90% (almost completely withered)
4: Growth control rate of from 70 to 90%
3: Growth control rate of from 40 to 70%
2: Growth control rate of from 20 to 40%
1: Growth control rate of from 5 to 20%
0: Growth control rate of less than 5% (almost non-effective)
The above growth control rates were calculated by the following equation:
Growth control rate (%)=(1-T/N).times.100
where:
T: Weight of the weed growth above the soil surface of the treated area
N: Weight of the weed grown above the soil surface of the non-treated area
TEST EXAMPLE 2
Test on the herbicidal effects in foliage treatment
A plastic box having a length of 15 cm, a width of 22 cm and a depth of 6 cm was filled with a sterilized diluvium soil, and seeds of Echinochloa crus-galli, Setaria viridis, Eleusine indica, Digitaria adscendens, Panicum dichotomiflorum, Xanthium strumarium, Abutilon theophrasti, Amaranthus lividus, Polygonum longisetum and Zea mays were spot-wisely sown, and tubers of Cyperus esculentus were further planted. Then, the soil was covered thereon in a thickness of about 1.5 cm. When the various weeds and crops grew to the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed on the foliages so that the active ingredient is applied in a predetermined concentration.
The herbicidal solution was prepared by diluting the wettable powder, the emulsifiable concentrate, the liquid formulation or the flowable as described in the above Formulation Examples with water and applied onto the entire surface of the foliages of the weeds and the crop plants by a small spray. Two weeks after the application of the herbicide solution, the herbicidal effects against each weed were determined on the basis of the standard ratings described in Test Example 1, and the phytotoxicity against each crop plant was determined on the basis of the standard ratings in Test Example 1. The results are shown in Table 7. The Compound Nos. in Table 7 correspond to the Compound Nos. in Table 3.
In Tables 6 and 7, the following abbreviations are used:
Dose: Dose of active ingredient (g/are)
EC: Echinochloa crus-galli (barnyardgrass)
SE: Setaria viridis (green foxtail)
EL: Eleusine indica (goosegrass)
DI: Digitaria adscendens (large crabgrass)
PA: Panicum dichotomiflorum (fall panicum)
AB: Abutilon theophrasti (velvet leaf)
AM: Amaranthus lividus (livid amaranth)
PO: Polygonum longisetum (persicaria blumei gross)
XA: Xanthium strumarium (cocklebur)
CY: Cyperus esculentus (yellow nutsedge)
ZE: Zea mays (corn)
TABLE 6__________________________________________________________________________CompoundNo. Dose EC SE EL DI PA AB AM PO CY ZE__________________________________________________________________________ 0.5 5 5 5 5 5 5 5 5 5 01 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 02 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 03 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 04 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 06 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 07 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 08 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 09 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 010 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 011 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 012 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 013 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 014 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 015 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 016 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 017 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 018 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 019 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 020 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 021 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 022 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 023 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 024 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 025 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 026 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 027 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 028 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 029 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 030 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 034 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 035 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 036 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 037 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 039 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 040 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 041 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 042 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 043 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 044 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 045 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 046 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 047 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 048 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 049 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 050 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0Reference 4 3 1 3 3 1 4 5 5 0 0Compound 8 4 2 4 4 2 5 5 5 0 0A 16 5 3 5 5 3 5 5 5 1 1Reference 4 5 5 5 5 5 1 1 1 2 0Compound 8 5 5 5 5 5 2 2 2 3 0B 16 5 5 5 5 5 3 3 3 4__________________________________________________________________________
TABLE 7__________________________________________________________________________CompoundNo. Dose EC SE EL DI PA AB AM PO XA CY ZE__________________________________________________________________________ 0.5 5 5 5 5 5 5 5 5 5 5 01 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 02 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 03 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 04 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 06 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 07 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 08 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 09 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 010 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 011 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 012 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 013 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 014 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 015 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 016 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 017 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 018 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 019 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 020 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 021 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 022 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 023 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 024 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 025 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 026 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 027 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 028 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 029 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 030 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 034 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 035 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 036 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 037 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 039 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 040 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 041 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 042 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 043 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 044 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 045 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 046 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 047 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 048 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 049 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 0.5 5 5 5 5 5 5 5 5 5 5 050 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0Reference 4 3 1 2 3 0 3 5 5 4 0 0Compound 8 4 2 3 4 1 5 5 5 5 0 1A 16 5 3 4 5 2 5 5 5 5 1 2Reference 4 4 3 3 4 3 0 2 2 0 1 0Compound 8 4 4 4 4 4 1 3 3 1 2 1B 16 5 5 5 5 5 2 4 4 2 3 2__________________________________________________________________________
In Tables 6 and 7, the Comparative Compounds are as follows:
Comparative Compound A: Atrazine ##STR49##
Comparative Compound B: Alachlor ##STR50##

Number	Date	Country
62-61937	Mar 1987	JPX
62-179797	Jul 1987	JPX
62-247601	Sep 1987	JPX

Number	Name	Date
4063925	Konotsune et al.	Dec 1977
4230481	Nishiyama et al.	Oct 1980
4316040	Plath et al.	Feb 1982
4406688	Konno et al.	Sep 1983
4460597	Yanai et al.	Jul 1984
4643757	Baba et al.	Feb 1987

Herbicidal pyrazole derivatives

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