Pyrazole derivatives and herbicides containing them

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.
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 develp 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.
The present invention provides a pyrazole derivative having the formula: ##STR3## wherein
A is a C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.4 alkenyl group or a C.sub.2 -C.sub.4 alkynyl group;
B is a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group, a halogen atom, a C.sub.1 -C.sub.3 haloalkyl group, a C.sub.1 -C.sub.3 alkoxy group, a C.sub.1 -C.sub.3 alkylthio group, a C.sub.2 -C.sub.4 alkoxyalkyl group, a C.sub.2 -C.sub.4 alkylthioaalkyl group or a C.sub.2 -C.sub.4 alkoxycarbonyl group;
X is a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a halogen atom, a nitro group, a cyano group, a C.sub.1 -C.sub.6 haloalkyl group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a C.sub.2 -C.sub.6 alkylcarbonyl group, a C.sub.2 -C.sub.6 alkoxycarbonyl group, an aminocarbonyl group substituted independently by hydrogen or by a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 haloalkoxy group, a C.sub.1 -C.sub.6 alkylthio group or a C.sub.2 -C.sub.6 alkylthioalkyl group;
Y is --OR.sup.1 (Wherein R.sup.1 is a C.sub.3 -C.sub.8 cycloalkyl group, a C.sub.4 -C.sub.8 cycloalkylalkyl group, a C.sub.3 -C.sub.6 alkenyl group, a C.sub.2 -C.sub.6 alkynyl group, a C.sub.1 -C.sub.6 haloalkyl group, a C.sub.3 C.sub.8 halocycloalkylalkyl group, a C.sub.3 -C.sub.6 haloalkenyl group, a C.sub.2 -C.sub.6 haloalkynyl group, a C.sub.2 -C.sub.6 nitroalkyl group or a phenyl group which may be substituted by a C.sub.1-C.sub.3 alkyl group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy group), --O--L--O--R.sup.1 (Wherein L is a C.sub.1 -C.sub.6 alkylene group which may be substituted by a C.sub.1 -C.sub.3 alkyl group, and R.sub.1 is as defined above), --O--L--OH (wherein L is as defined above), --O--L--O--L--O--R.sup.2 (wherein L is as defined above, and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a phenyl group which may be substituted by a C.sub.1 -C.sub.3 alkyl group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy group), --O--L--R.sup.3 (wherein L is as defined above, and R.sup.3 is a phenyl group which may be substituted by a C.sub.1 -C.sub.3 alkyl group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy group), --O--M (wherein M is a 3- to 6-membered alicyclic group containing not more than two sulfur or oxygen atoms and formed by a linkage of from 1 to 4 carbon atoms), --O--L--M (wherein L and M are as defined above), --O--L--NR.sup.4 R.sup.5 (wherein L is as defined above and each of R.sup.4 and R.sup.5 which may be the same or different is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, or R.sup.4 and R.sup.5 form a ring together with the adjacent nitrogen atom), --O--L-COOR.sup.4 (wherein L and R.sup.4 are as defined above), --O--CH.dbd.CH--COOR.sup.4 (wherein R.sup.4 is as defined above), --O--L--CN (wherein L is as defined above), --O--L--C(O)--R.sup.2 (wherein L and R.sup.2 are as defined above), --O--L--S(O).sub.n --R.sup.4 (wherein L and R.sup.4 are as defined above, and n is an integer of from 0 to 2), --O--COOR.sup.4 (wherein R.sup.4 are as defined above), --O--CONR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 are as defined above), --OP(O)(OR.sup.4).sub.2 (wherein R.sup.4 is as defined above), --S(O).sub.n R.sup.1 (wherein R.sup.1 and n are as defined above), or --S(O).sub.n --L--O--R.sup.1 (wherein L, R.sup.1 and n are as defined above);
Z is a halogen atom, a nitro group, a C.sub.1 -C.sub.3 alkoxy group, a trifluoromethyl group, a trifluoromethoxy group, a cyano group or --S(O).sub.n R.sup.6 (wherein n is as defined above, and R.sup.6 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 haloalkyl group);
V is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.4 alkoxy group;
W is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a C.sub.2 -C.sub.5 alkoxycarbonyl group, a C.sub.1 -C.sub.3 haloalkoxy group, a nitro group, a cyano group or --S(O).sub.n --R.sup.6 (wherein n and R.sup.6 are as defined above); and
Q is a hydrogen atom, a C.sub.1 --C.sub.6 alkyl group which may be substituted by a halogen atom, a C.sub.1 -C.sub.6 alkenyl group which may be substituted by a halogen atom, a C.sub.1 -C.sub.6 alkynyl group which may be substituted by a halogen atom, a cyanomethyl group, --C(O)--R.sup.7 (wherein R.sup.7 is a phenyl group which may be substituted by the same or different substituents selected from the group consisting of a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkenyl group, a C.sub.1 -C.sub.6 alkynyl group, a C.sub.1 -C.sub.6 haloalkyl group, a C.sub.1 -C.sub.6 haloalkenyl group, a C.sub.1 -C.sub.6 haloalkynyl group, a halogen atom, a nitro group and a trifluoromethyl group, a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, or a hydroxyl group), --S(O).sub.2 R.sup.7 (wherein R.sup.7 is as defined above), --P(O)(OR.sup.7).sub.2 (wherein R.sup.7 is as defined above), --L--C(O)--R.sup.7 (wherein L and R.sup.7 are as defined above), --L--C(O)--N(R.sup.8)(R.sup.9) (wherein L is as defined above, and each of R.sup.8 and R.sup.9 which may be the same or different is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group), --L--R.sup.10 (wherein L is as defined above, and R.sup.10 is a phenyl group which may be substituted by the sam or different substituents selected from the group consisting of a halogen atom, a nitro group and a trifluoromethyl group, a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, or a hydroxyl group), --L--N(R.sup.8)(R.sup.9) (wherein L, R.sup.8 and R.sup.9 are as defined above), --L--OR.sup.11 (wherein L is as defined above, and R.sup.11 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, or a C.sub.1 -C.sub.6 alkenyl group), --L--OC(O)R.sup.12 (wherein L is as defined above, and R.sup.12 is a C.sub.1 -C.sub.6 alkyl group or a C.sub.1 C.sub.6 alkoxy group), --L--S(O).sub.n R.sup.11 (wherein L, n and R.sup.11 are as defined above), --L--SC(O)R.sup.8 (wherein L and R.sup.8 are as defined above), ##STR4## (wherein each of L1 and L2 which may be the same or different is a methylene group, an oxygen atom or a sulfur atom, R.sup.12 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, and m is 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.
Furthermore, the present invention provides a substituted benzene derivative of the formula: ##STR5## wherein G is a carboxyl group, a halocarbonyl group or a cyanocarbonyl group, and X, Y, Z, V and W are as defined above.
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 inveniton, 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, t-Bu
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-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, CHMiOEt, 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: ##STR6## OCHMeCH.dbd.CH.sub.2, OCMe.sub.2 CH.dbd.CH.sub.2, OCH.sub.2 CMe.dbd.CH.sub.2, OCH.sub.2 CH.dbd.CHMe, OCH.sub.2 CH.dbd.CMe.sub.2, OCH.sub.2 C.tbd.CH, OCHMeC.tbd.CH, OCHMe.sub.2 C.tbd.CH, OCH.sub.2 .tbd.CMe, OCH.sub.2 CH.sub.2 F, OCH.sub.2 CHF.sub.2, OCH.sub.2 CF.sub.3, OCH.sub.2 CH.sub.2 Cl, OCHMeCH.sub.2 Cl, OCH.sub.2 CCl.sub.3, OCH.sub.2 CH.sub.2 CH.sub.2 Cl, OCH.sub.2 CH.sub.2 Br, ##STR7## OCH.sub.2 CCl.dbd.CH.sub.2, OCH.sub.2 CH.sub.2 CH.dbd.CH.sub.2, OCH.sub.2 CCl.dbd.CHCl, OCH.sub.2 CH.sub.2 NO.sub.2, OPh,OPh-Me-2 OPh-Cl-4, OPh-NO.sub.2 -4, OPH.sub.2 CH.sub.2 OMe, OCH.sub.2 CH.sub.2 OEt, OCH.sub.2 CH.sub.2 OPr-n, OCH.sub.2 CH.sub.2 OPr-i, OCH.sub.2 CH.sub.2 OBu-n, OCH.sub.2 CH.sub.2 OBu-i, OCH.sub.2 CH.sub.2 Bu-s, OCH.sub.2 CH.sub.2 OBu-t, OCHMeCH.sub.2 OMe, OCH.sub.2 CH.sub.2 OPh, OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe, OCH.sub.2 CH.sub.2 OH, OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe, OCH.sub.2 Ph, OCHMePh, OCH.sub.2 Ph-4-Me, OCH.sub.2 Ph-4-Cl, OCH.sub.2 CH.sub.2 Ph, ##STR8## OCH.sub.2 CH.sub.2 NH.sub.2, OCH.sub.2 CH.sub.2 NHMe, OCH.sub.2 CH.sub.2 NMe.sub.2, OCH.sub.2 CH.sub.2 NEt.sub.2, OCH.sub.2 COOMe, OCH.sub.2 COOEt, OCH.sub.2 COOPr-n, OCH.sub.2 COOPr-i, OCH.sub.2 COOBu-t, OCHMeCOOMe, OCHMeCOOEt OCHMeCOOPr-n, OCHMeCOOPr-i, OCHMeCOOBu-t OCH.sub.2 CH.sub.2 CN, OCH.sub.2 CN, OCHMeCN, OCH.sub.2 SMe, OCH.sub.2 C(O)Ph, OCH.sub.2 C(O)Me, OCH.sub.2 CH.sub.2 SMe, OCH.sub.2 CH.sub.2 SOMe, OCH.sub.2 CH.sub.2 SO.sub.2 Me, OCH.sub.2 CH.sub.2 SEt, OCH.sub.2 CH.sub.2 SO.sub.2 Et, OCOOMe, OCOOEt, OCOOPr-i, OCONH.sub.2, OCONHMe, OCONMe.sub.2, OP(O)(OMe).sub.2, OP(O)(OEt).sub.2, ##STR9## SCH.sub.2 CH.dbd.CH.sub.2, SCH.sub.2 C.tbd.CH, SCH.sub.2 CF.sub.3, SCH.sub.2 CH.sub.2 Cl, SCH.sub.2 CCl.sub.3, ##STR10## SPh, SCH.sub.2 CH.sub.2 OMe, SCH.sub.2 CH.sub.2 OEt, SCH.sub.2 CH.sub.2 OPr-i, SCH.sub.2 CH.sub.2 OPh, ##STR11## S(O)CH.sub.2 .dbd.CH.sub.2, S(O)CH.sub.2 CH.tbd.CH,S(O)CH.sub.2 CF.sub.3, S(O)CH.sub.2 CH.sub.2 Cl, ##STR12## S(O)Ph, S(O)CH.sub.2 CH.sub.2 OMe, S(O)CH.sub.2 CH.sub.2 OEt, S(O)CH.sub.2 CH.sub.2 OPr-i, S(O)CH.sub.2 CH.sub.2 OPh, ##STR13## SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2, SO.sub.2 CH.sub.2 C.tbd.CH, SO.sub.2 CH.sub.2 CF.sub.3, SO.sub.2 CH.sub.2 CH.sub.2 Cl, SO.sub.2 CH.sub.2 ##STR14## SO.sub.2 Ph, SO.sub.2 CH.sub.2 CH.sub.2 OMe, SO.sub.2 CH.sub.2 CH.sub.2 OEt, SO.sub.2 CH.sub.2 CH.sub.2 OPr-i, 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, ##STR15## 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, CHMeNM.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.2, CONHEt, CONEt.sub.2, CONPr-n.sub.2, CON(CH.sub.2 CH.dbd.CH.sub.2).sub.2, CONMePh, ##STR16## 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 from 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 invention 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 incorporation 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), Amarathus lividus (livid amaranth), Polvgonum 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 Sorphum bicolor. The herbicidal activities against gramineous weeds and Cyperus esculentus are remarkablly high and extremely unique. Heretofore, during the cultivation of Zea mays or Sorghum bicolor, it has been common to employ atranzine or cyanazine as a triazine-type herbicide, or alachlor or metolachlor as an acid anilide type herbicide. However, atranzine 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, Sorqhum 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-qalli (barnyardgrass), and it also includes a compound having selectivity for a useful plant such as Goxxypium spp (cotton), Beta vulgaris (sugar beat) or Clycine 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 research 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 treatment 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. ##STR17##
In the above formulas, A, B, V, W, X, Y, Z and Q are as defined above, E is a halogen atom, a methanesulfonyloxy group or a p-toluenesulfonyloxy group. Further, ##STR18## and may be represented by either formula.
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 a condensation agent and a base to obtain 4-benzoyl-5-hydroxypyrazole. The condensation agent is used in an amount of from 1.0 to 1.5 mols per mol of the benzoic acid and pyrazole. As the condensation agent, N,N'-dicyclohexylcarbodiimide may be mentioned. The solvent may be any aolvent 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 boiling point of the solvent, but is peferably 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, toluene or xylene 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 30 hours.
Reaction scheme (3) shows a reaction wherein a benzene derivative, a 5-hydroxypyrazole derivative and carbon tetrachloride are condensed in the presence of a Lewis acid in an inert solvent or in the absence of a solvent, followed by hydrolysis to obtain a 4-benzoyl-5-hydroxypyrazole derivative. As the Lewis acid, anhydrous aluminum chloride or anhydrous aluminum bromide in an amount of at least the theoretical amount for the reaction is preferred. The solvent may be of any type so long as it is inert to the reaction. However, a chlorine-type solvent such as methylene chloride, dichloroethane or tetrachloroethane is preferred. The temperature for condensation may range from 0.degree. C. to the boiling point of the solvent, but it is preferably from 10.degree. to 80.degree. C. The hydrolysis is conducted in the presence of hydrochloric acid or sulfuric acid. The temperature for the hydrolysis is preferably from room temperature to 100.degree. C. The time for the hydrolysis is usually from 0.1 to 10 hours.
Reaction scheme (4) shows a reaction wherein a benzoyl cyanide derivative and a 5-hydroxypyrazole derivative are reacted in the presence of a Lewis acid and a base in an inert solvent or in the absence of a solvent to obtain a 4-benzoyl-5-hydroxypyrazole. As the Lewis acid, zinc chloride, aluminum chloride or aluminum bromide may be used. As the base, pyridine or triethylamine may be mentioned. The Lewis acid and the base are used usually in an amount of from 1 to 10 mol times. As the solvent, methylene chloride, dichloroethane or tetrachloroethane may be mentioned. The reaction temperature is usually from 0.degree. to 80.degree. C., preferably from 10.degree. to 50.degree. C. The reaction time is from 0.5 to 20 hours.
Reaction scheme (5) shows a reaction wherein 4-benzoyl-5-hydroxyyrazole 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 triethylaine, 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 (6) shows a reaction wherein 4-benzoyl-5-hydroxypyrazole is converted to a 5 halogeno compound by a halogenating agent, or to a methanesulfonate compound or a p-toluenesulfonate compound by methane sulfonyl chloride or p-toluenesulfonyl chloride, followed by condensation with a suitable alcohol or acid.
As the halogenating 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.
As 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 substituted benzene derivatives used as the starting materials for the compounds of the present invention have novel structures, and they may readily be prepared by a proper 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. ##STR19##
In the above formulas, X and Y are as defined above, and Hal is a halogen atom.

Now, the preparation of the substituted benzene derivatives and pyrazole derivatives will be described in detail with reference to Examples. However, it should be understood that the present invention is by no means restricted by such specific Examples.
EXAMPLE 1
Preparation of 4-(2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoyl)-1-ethyl-5-hydroxypyrazole
(1) (2-methoxy)ethyl 2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoate
1.2 g of 2-chloro-3-hydroxy-4-methanesulfonylbenzoic acid, 1.4 g of potassium carbonate and 2.1 g of 2bromoethyl methyl ether were put into 20 ml of N,N-dimethylformamide and reacted under heating at a temperture of from 60.degree. to 70.degree. C. for from 6 to 7 hours. Then, the solvent was distilled off, and after an addition of water, the reaction mixture was extracted with chloroform. The extract was dried over anhydrous sodium sulfate, and the solvent was distilled off to obtain 1.9 g of a crude product of the above identified compound.
(2) 2 -chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoic acid
1.9 g of the crude product of (2-methoxy)ethyl 2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoate was dissolved in 50 ml of ethanol, and 20 ml of an aqueous solution containing 1 g of sodium hydroxide was added thereto. The mixture was stirred at room temperature for 30 minutes. Then, ethanol was distilled off, and water was added to the residue. The mixture was washed with chloroform, then acidified with concentrated hydrochloric acid and extracted with chloroform. The extract was dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain 1.4 g of a crude product of the above identified compound. To the crude product, n-hexane was added, and the mixture was left to stand, whereby the desired product was gradually crystallized. Melting point: 89.degree.-92.degree. C.
(3) 4-(2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoyl)-1-ethyl-5-hydroxypyrazole
1.2 g of the crude product of 2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoic acid, 0.3 g of potassium carbonate, 0.45 g of 1-ethyl-5-hydroxypyrazole and 0.77 g of N,N'-dicyclohexyl carbodiimide were put into 40 ml of t-amyl alcohol, and the mixture was stirred under heating at a temperature of from 80.degree. to 90.degree. C. for from 4 to 5 hours. The solvent was distilled off, and a dilute potassium carbonate aqueous solution was added to the residue. 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. Then, the solvent was distilled off to obtain a crude product of the above identified compound. The crude product was recrystallized from ethanol to obtain 0.3 g of the desired product. Melting point: 159.degree.-160.degree. C.
EXAMPLE 2
Preparation of 4-(3-benzyloxy-2-chloro-4-methanesulfonylbenzoyl)-1-ethyl-5-hydroxypyrazole (1}Benzyl 3-benzyloxy-2-chloro-4-methanesulfonylbenzoate
1.5 g of 2-chloro-3-hydroxy-4-methanesulfonylbenzoic acid, 1.7 g of potassium carbonate and 5.1 g of benzyl bromide were put into 50 ml of dimethylformamide, and the mixture was stirred at room temperature overnight and then heated at a temperature of from 60.degree. to 70.degree. C. for 3 hours. The solvent was distilled off, and water was added to the residue. The mixture was extracted with chloroform. The extract was dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain a crude product of the above identified compound. The crude product was recrystallized from ethanol to obtain 2.5 g of the desired product.
(2) 3-benzyloxy-2-chloro-4-methanesulfonylbenzoic acid
2.5 g of benzyl 3-benzyloxy-2-chloro-4-methanesulfonylbenzoate was put into 50 ml of ethanol, and 25 ml of an aqueous solution containing 1 g of sodium hydrochloride was added thereto. The mixture was stirred at room temperature for 30 minutes. Then, ethanol was distilled off, and water was added to the residue. The mixture was washed with chloroform. The aqueous layer was acidified with concentrated hydrochloric acid and then extracted with chloroform. The extract was dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain a crude product of the above identified compound. The crude product was washed with ethanol-isopropyl ether to obtain 1.0 g of the desired product.
(3)-4-(3-benzyloxy-2-chloro-4-methanesulfonylbenzol)-ethyl-5-hydroxypyrazol
1.0 g of 3-benzyloxy-2-chloro-4methanesulfonylbenzoic acid, 0.23 g of potassium carbonate, 0.24 g of 1-ethyl-5-hydroxy-pyrazole and 0.59 g of N,N'-dicyclohexylcarbodiimide were put into 20 ml of t-amyl alcohol, and the mixture was stirred under heating at a temperature of from 80.degree. to 90.degree. C. for 4 hours. The solvent was distilled off, and then an aqueous potassium carbonate solution was added to the residue. The mixture was washed with chloroform. The aqueous layer was acidified with concentrated hydrochloric acid and then extracted with chloroform. The extract was dried over anhydrous sodium sulfate. Then, the solvent was distilled off to obtain a crude product of the above identified compound. The crude product was recrystallized from ethanol to obtain 0.3 g of the desired product. Melting point: 162.degree.-165.degree. C.
The physical properties of the benzoic acids and the pyrazole derivatives prepared in accordance with the preceeding Examples will be given in Tables 1 and 2 including those of the preceeding Examples.
TABLE 1______________________________________ ##STR20## MeltingX Y Z point (.degree.C.)______________________________________Cl ##STR21## SO.sub.2 Me 102.about.107Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me 147.about.151Cl ##STR22## SO.sub.2 Me 153.about.157Cl OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me 90.about.94Cl OCH.sub.2 CHCHMe SO.sub.2 Me 113.about.118Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me 89.about.92______________________________________
TABLE 2__________________________________________________________________________ ##STR23##Compound MeltingNo. A B X Y Z Q point (.degree.C.)__________________________________________________________________________ 1 Et H Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H 159.about.160 2 Et H Cl OCH.sub.2 Ph SO.sub.2 Me H 162.about.165 3 Et H Cl ##STR24## SO.sub.2 Me H 156.about.159 4 Et H Cl ##STR25## SO.sub.2 Me H 153.about.157 5 Et H Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H 148.about.150 6 Et H Cl OCH.sub.2 CCH SO.sub.2 Me H 150.7.about.152.4 7 Et H Cl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H 152.3.about.154.9 8 Et H Cl OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H 131.about.134 9 Et H Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H Oily substance10 Et H Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H 206.about.20811 Et H Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H 171.about.17412 Et H Cl ##STR26## SO.sub.2 Me H 191.about.19313 Me Me Cl ##STR27## SO.sub.2 Me H 181.about.183.514 Et H Cl ##STR28## SO.sub.2 Me H 100.about.10115 Et H Cl ##STR29## SO.sub.2 Me H 171.about.17316 Me Me Cl ##STR30## SO.sub.2 Me H 138.about.14217 Me Me Cl ##STR31## SO.sub.2 Me H 100.5.about.10118 Et H Cl ##STR32## SO.sub.2 Me H 154.about.15819 Et H Cl ##STR33## SO.sub.2 Me H 175.about.17920 i-Pr H Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H 180.about.183__________________________________________________________________________
Compounds which can be prepared in the same manner as the preceding Examples will be given in Tables 3 to 8 including those of the preceding Examples. However, the present invention is not restricted to such compounds.
Various symbols used in Tables 3 to 8 have the following meanings. ##STR34##
TABLE 3______________________________________X Y Z Q______________________________________Me Y1 SO.sub.2 Me HMe Y2 SO.sub.2 Me HMe Y3 SO.sub.2 Me HMe Y4 SO.sub.2 Me HMe Y5 SO.sub.2 Me HMe Y6 SO.sub.2 Me HMe Y7 SO.sub.2 Me HMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCHMeCHCH.sub.2 SO.sub.2 Me HMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CHCHMe SO.sub.2 Me HMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CCH SO.sub.2 Me HMe OCHMeC CH SO.sub.2 Me HMe OCMe.sub.2 CCH SO.sub.2 Me HMe OCH.sub.2 CCMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe OCHMeCH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HMe Y8 SO.sub.2 Me HMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CClCHCl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HMe OPh SO.sub.2 Me HMe OPhMe-2 SO.sub.2 Me HMe OPhCl-4 SO.sub.2 Me HMe OPhNO.sub.2 -4 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HMe OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CHMeOMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HMe OCH.sub.2 Ph SO.sub.2 Me HMe OCHMePh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HMe Y9 SO.sub.2 Me HMe Y10 SO.sub.2 Me HMe Y11 SO.sub.2 Me HMe Y12 SO.sub.2 Me HMe Y13 SO.sub.2 Me HMe Y14 SO.sub.2 Me HMe Y15 SO.sub.2 Me HMe Y16 SO.sub.2 Me HMe Y17 SO.sub.2 Me HMe Y18 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NME.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HMe Y19 SO.sub.2 Me HMe OCH.sub.2 COOMe SO.sub.2 Me HMe OCH.sub.2 COOEt SO.sub.2 Me HMe OCH.sub.2 COOPr-i SO.sub.2 Me HMe OCH.sub.2 COOBu-i SO.sub.2 Me HMe OCH.sub.2 COOBu-t SO.sub.2 Me HMe OCH.sub.2 COOY4 SO.sub.2 Me HMe OCHMeCOOMe SO.sub.2 Me HMe OCHMeCOOEt SO.sub.2 Me HMe OCHMeCOOPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HMe OCH.sub.2 SMe SO.sub. 2 Me HMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HMe OCOOMe SO.sub.2 Me HMe OCOOPr-i SO.sub.2 Me HMe OCONH.sub.2 SO.sub.2 Me HMe OCONHMe SO.sub.2 Me HMe OCONMe.sub.2 SO.sub.2 Me HMe OP(O)(OMe).sub.2 SO.sub.2 Me HMe Y20 SO.sub.2 Me HMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SCH.sub.2 CCH SO.sub.2 Me HMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe Y21 SO.sub.2 Me HMe SPh SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe Y22 SO.sub.2 Me HMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CCH SO.sub.2 Me HMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y23 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y24 SO.sub.2 Me HMe Y25 SO.sub.2 Me HMe SO.sub.2 Ph SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub. 2 PhMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub. 2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OEt Cl HMe OCH.sub.2 CH.sub.2 OPr-i Cl HMe OCHMeCH.sub.2 OMe Cl HMe OCH.sub.2 COOMe Cl HMe OCH.sub.2 CH.sub.2 SMe Cl HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HMe SCH.sub.2 CH.sub.2 OMe Cl HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl Y1 SO.sub.2 Me HCl Y2 SO.sub.2 Me HCl Y3 SO.sub.2 Me HCl Y4 SO.sub.2 Me HCl Y5 SO.sub.2 Me HCl Y6 SO.sub.2 Me HCl Y7 SO.sub.2 Me HCl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCHMeCHCH.sub.2 SO.sub.2 Me HCl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CHCHMe SO.sub.2 Me HCl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CCH SO.sub.2 Me HCl OCHMeCCH SO.sub.2 Me HCl OCMe.sub.2 CCH SO.sub.2 Me HCl OCH.sub.2 CCMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCl OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCl OCH.sub.2 CF.sub.3 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl OCHMeCH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCl Y8 SO.sub.2 Me HCl OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CClCHCl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCl OPh SO.sub.2 Me HCl OPhMe-2 SO.sub.2 Me HCl OPhCl-4 SO.sub.2 Me HCl OPhNO.sub.2 -4 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HCl OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CHMeOMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCl OCH.sub.2 Ph SO.sub.2 Me HCl OCHMePh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCl OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCl OCH.sub.2 Ph-3-Me SO.sub.2 Me HCl OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCl Y9 SO.sub.2 Me HCl Y10 SO.sub.2 Me HCl Y11 SO.sub.2 Me HCl Y12 SO.sub.2 Me HCl Y13 SO.sub.2 Me HCl Y14 SO.sub.2 Me HCl Y15 SO.sub.2 Me HCl Y16 SO.sub.2 Me HCl Y17 SO.sub.2 Me HCl Y18 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCl Y19 SO.sub.2 Me HCl OCH.sub.2 COOMe SO.sub.2 Me HCl OCH.sub.2 COOEt SO.sub.2 Me HCl OCH.sub.2 COOPr-i SO.sub.2 Me HCl OCH.sub.2 COOBu-i SO.sub.2 Me HCl OCH.sub.2 COOBu-t SO.sub.2 Me HCl OCH.sub.2 COOY4 SO.sub.2 Me HCl OCHMeCOOMe SO.sub.2 Me HCl OCHMeCOOEt SO.sub.2 Me HCl OCHMeCOOPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCl OCH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCl OCOOMe SO.sub.2 Me HCl OCOOPr-i SO.sub.2 Me HCl OCONH.sub.2 SO.sub.2 Me HCl OCONHMe SO.sub.2 Me HCl OCONMe.sub.2 SO.sub.2 Me HCl OP(O)(OMe).sub.2 SO.sub.2 Me HCl Y20 SO.sub.2 Me HCl SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SCH.sub.2 CCH SO.sub.2 Me HCl SCH.sub.2 CF.sub.3 SO.sub.2 Me HCl SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl Y21 SO.sub.2 Me HCl SPh SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl Y22 SO.sub.2 Me HCl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CCH SO.sub.2 Me HCl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y23 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y24 SO.sub.2 Me HCl Y25 SO.sub.2 Me HCl SO.sub. 2 Ph SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub. 2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OEt Cl HCl OCH.sub.2 CH.sub.2 OPr-i Cl HCl OCHMeCH.sub.2 OMe Cl HCl OCH.sub.2 COOMe Cl HCl OCH.sub.2 CH.sub.2 SMe Cl HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCl SCH.sub.2 CH.sub.2 OMe Cl HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe Y1 SO.sub.2 Me HOMe Y2 SO.sub.2 Me HOMe Y3 SO.sub.2 Me HOMe Y4 SO.sub.2 Me HOMe Y5 SO.sub.2 Me HOMe Y6 SO.sub.2 Me HOMe Y7 SO.sub.2 Me HOMe OCH.sub. 2 CHCH.sub.2 SO.sub.2 Me HOMe OCHMeCHCH.sub.2 SO.sub.2 Me HOMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CHCHMe SO.sub.2 Me HOMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CCH SO.sub.2 Me HOMe OCHMeCCH SO.sub.2 Me HOMe OCMe.sub.2 CCH SO.sub.2 Me HOMe OCH.sub.2 CCMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HOMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe OCHMeCH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HOMe Y8 SO.sub.2 Me HOMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CClCHCl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HOMe OPh SO.sub.2 Me HOMe OPhMe-2 SO.sub.2 Me HOMe OPhCl-4 SO.sub.2 Me HOMe OPhNO.sub.2 -4 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 -Y4 SO.sub.2 Me HOMe OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CHMeOMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HOMe OCH.sub.2 Ph SO.sub.2 Me HOMe OCHMePh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HOMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HOMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HOMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HOMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HOMe Y9 SO.sub.2 Me HOMe Y10 SO.sub.2 Me HOMe Y11 SO.sub.2 Me HOMe Y12 SO.sub.2 Me HOMe Y13 SO.sub.2 Me HOMe Y14 SO.sub.2 Me HOMe Y15 SO.sub.2 Me HOMe Y16 SO.sub.2 Me HOMe Y17 SO.sub.2 Me HOMe Y18 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HOMe Y19 SO.sub.2 Me HOMe OCH.sub.2 COOMe SO.sub.2 Me HOMe OCH.sub.2 COOEt SO.sub.2 Me HOMe OCH.sub.2 COOPr-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-t SO.sub.2 Me HOMe OCH.sub.2 COO-Y4 SO.sub.2 Me HOMe OCHMeCOOMe SO.sub.2 Me HOMe OCHMeCOOEt SO.sub.2 Me HOMe OCHMeCOOPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HOMe OCH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HOMe OCOOMe SO.sub.2 Me HOMe OCOOPr-i SO.sub.2 Me HOMe OCONH.sub.2 SO.sub.2 Me HOMe OCONHMe SO.sub.2 Me HOMe OCONMe.sub.2 SO.sub.2 Me HOMe OP(O)(OMe).sub.2 SO.sub.2 Me HOMe Y20 SO.sub.2 Me HOMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CCH SO.sub.2 Me HOMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe Y21 SO.sub.2 Me HOMe SPh SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe Y22 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CCH SO.sub.2 Me HOMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y23 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub. 2 CCH SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y24 SO.sub.2 Me HOMe Y25 SO.sub.2 Me HOMe SO.sub.2 Ph SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OEt Cl HOMe OCH.sub.2 CH.sub.2 OPr-i Cl HOMe OCHMeCH.sub.2 OMe Cl HOMe OCH.sub.2 COOMe Cl HOMe OCH.sub.2 CH.sub.2 SMe Cl HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HOMe SCH.sub.2 CH.sub.2 OMe Cl HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe Y1 SO.sub.2 Me HCH.sub.2 OMe Y2 SO.sub.2 Me HCH.sub.2 OMe Y3 SO.sub.2 Me HCH.sub.2 OMe Y4 SO.sub.2 Me HCH.sub.2 OMe Y5 SO.sub.2 Me HCH.sub.2 OMe Y6 SO.sub.2 Me HCH.sub.2 OMe Y7 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCHMeCHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCHMeCCH SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 C CH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCH.sub.2 OMe Y8 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCHCl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe OPh SO.sub.2 Me HCH.sub.2 OMe OPhMe-2 SO.sub.2 Me HCH.sub.2 OMe OPhCl-4 SO.sub.2 Me HCH.sub.2 OMe OPhNO.sub.2 -4 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 -Y4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHMeOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCHMePh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y9 SO.sub.2 Me HCH.sub.2 OMe Y10 SO.sub.2 Me HCH.sub.2 OMe Y11 SO.sub.2 Me HCH.sub.2 OMe Y12 SO.sub.2 Me HCH.sub.2 OMe Y13 SO.sub.2 Me HCH.sub.2 OMe Y14 SO.sub.2 Me HCH.sub.2 OMe Y15 SO.sub.2 Me HCH.sub.2 OMe Y16 SO.sub.2 Me HCH.sub.2 OMe Y17 SO.sub.2 Me HCH.sub.2 OMe Y18 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCH.sub. 2 OMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y19 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COO-Y4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOMe SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCH.sub.2 OMe OCOOMe SO.sub.2 Me HCH.sub.2 OMe OCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCONHMe SO.sub.2 Me HCH.sub.2 OMe OCONMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me HCH.sub.2 OMe Y20 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe Y21 SO.sub.2 Me HCH.sub.2 OMe SPh SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe Y22 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub. 2 OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y23 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y24 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub. 2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i Cl HCH.sub.2 OMe OCHMeCH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 COOMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh______________________________________
TABLE 4______________________________________; - ##STR35##X Y Z Q______________________________________Me Y1 SO.sub.2 Me HMe Y2 SO.sub.2 Me HMe Y3 SO.sub.2 Me HMe Y4 SO.sub.2 Me HMe Y5 SO.sub.2 Me HMe Y6 SO.sub.2 Me HMe Y7 SO.sub.2 Me HMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCHMeCHCH.sub.2 SO.sub.2 Me HMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CHCHMe SO.sub.2 Me HMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CCH SO.sub.2 Me HMe OCHMeC CH SO.sub.2 Me HMe OCMe.sub.2 CCH SO.sub.2 Me HMe OCH.sub.2 CCMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe OCHMeCH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HMe Y8 SO.sub.2 Me HMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CClCHCl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HMe OPh SO.sub.2 Me HMe OPhMe-2 SO.sub.2 Me HMe OPhCl-4 SO.sub.2 Me HMe OPhNO.sub.2 -4 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HMe OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CHMeOMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HMe OCH.sub.2 Ph SO.sub.2 Me HMe OCHMePh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HMe Y9 SO.sub.2 Me HMe Y10 SO.sub.2 Me HMe Y11 SO.sub.2 Me HMe Y12 SO.sub.2 Me HMe Y13 SO.sub.2 Me HMe Y14 SO.sub.2 Me HMe Y15 SO.sub.2 Me HMe Y16 SO.sub.2 Me HMe Y17 SO.sub.2 Me HMe Y18 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HMe Y19 SO.sub.2 Me HMe OCH.sub.2 COOMe SO.sub.2 Me HMe OCH.sub.2 COOEt SO.sub.2 Me HMe OCH.sub.2 COOPr-i SO.sub.2 Me HMe OCH.sub.2 COOBu-i SO.sub.2 Me HMe OCH.sub.2 COOBu-t SO.sub.2 Me HMe OCH.sub.2 COOY4 SO.sub.2 Me HMe OCHMeCOOMe SO.sub.2 Me HMe OCHMeCOOEt SO.sub.2 Me HMe OCHMeCOOPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HMe OCH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HMe OCOOMe SO.sub.2 Me HMe OCOOPr-i SO.sub.2 Me HMe OCONH.sub.2 SO.sub.2 Me HMe OCONHMe SO.sub.2 Me HMe OCONMe.sub.2 SO.sub.2 Me HMe OP(O)(OMe).sub.2 SO.sub.2 Me HMe Y20 SO.sub.2 Me HMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SCH.sub.2 CCH SO.sub.2 Me HMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe Y21 SO.sub.2 Me HMe SPh SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe Y22 SO.sub.2 Me HMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CCH SO.sub.2 Me HMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y23 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y24 SO.sub.2 Me HMe Y25 SO.sub.2 Me HMe SO.sub.2 Ph SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub. 2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OEt Cl HMe OCH.sub.2 CH.sub.2 OPr-i Cl HMe OCHMeCH.sub.2 OMe Cl HMe OCH.sub.2 COOMe Cl HMe OCH.sub.2 CH.sub.2 SMe Cl HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HMe SCH.sub.2 CH.sub.2 OMe Cl HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl Y1 SO.sub.2 Me HCl Y2 SO.sub.2 Me HCl Y3 SO.sub.2 Me HCl Y4 SO.sub.2 Me HCl Y5 SO.sub.2 Me HCl Y6 SO.sub.2 Me HCl Y7 SO.sub.2 Me HCl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCHMeCHCH.sub.2 SO.sub.2 Me HCl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CHCHMe SO.sub.2 Me HCl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CCH SO.sub.2 Me HCl OCHMeCCH SO.sub.2 Me HCl OCMe.sub.2 CCH SO.sub.2 Me HCl OCH.sub.2 CCMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCl OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCl OCH.sub.2 CF.sub.3 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl OCHMeCH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCl Y8 SO.sub.2 Me HCl OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CClCHCl SO.sub.2 Me HCl OCH.sub. 2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCl OPh SO.sub.2 Me HCl OPhMe-2 SO.sub.2 Me HCl OPhCl-4 SO.sub.2 Me HCl OPhNO.sub.2 -4 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HCl OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CHMeOMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCl OCH.sub.2 Ph SO.sub.2 Me HCl OCHMePh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCl OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCl OCH.sub.2 Ph-3-Me SO.sub.2 Me HCl OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCl Y9 SO.sub.2 Me HCl Y10 SO.sub.2 Me HCl Y11 SO.sub.2 Me HCl Y12 SO.sub.2 Me HCl Y13 SO.sub.2 Me HCl Y14 SO.sub.2 Me HCl Y15 SO.sub.2 Me HCl Y16 SO.sub.2 Me HCl Y17 SO.sub.2 Me HCl Y18 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCl Y19 SO.sub.2 Me HCl OCH.sub.2 COOMe SO.sub.2 Me HCl OCH.sub.2 COOEt SO.sub.2 Me HCl OCH.sub.2 COOPr-i SO.sub.2 Me HCl OCH.sub.2 COOBu-i SO.sub.2 Me HCl OCH.sub.2 COOBu-t SO.sub.2 Me HCl OCH.sub.2 COOY4 SO.sub.2 Me HCl OCHMeCOOMe SO.sub.2 Me HCl OCHMeCOOEt SO.sub.2 Me HCl OCHMeCOOPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCl OCH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCl OCOOMe SO.sub.2 Me HCl OCOOPr-i SO.sub.2 Me HCl OCONH.sub.2 SO.sub.2 Me HCl OCONHMe SO.sub.2 Me HCl OCONMe.sub.2 SO.sub.2 Me HCl OP(O)(OMe).sub.2 SO.sub.2 Me HCl Y20 SO.sub.2 Me HCl SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SCH.sub.2 C CH SO.sub.2 Me HCl SCH.sub.2 CF.sub.3 SO.sub.2 Me HCl SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl Y21 SO.sub.2 Me HCl SPh SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl Y22 SO.sub.2 Me HCl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CCH SO.sub.2 Me HCl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y23 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y24 SO.sub.2 Me HCl Y25 SO.sub.2 Me HCl SO.sub.2 Ph SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OEt Cl HCl OCH.sub.2 CH.sub.2 OPr-i Cl HCl OCHMeCH.sub.2 OMe Cl HCl OCH.sub.2 COOMe Cl HCl OCH.sub.2 CH.sub.2 SMe Cl HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCl SCH.sub.2 CH.sub.2 OMe Cl HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe Y1 SO.sub.2 Me HOMe Y2 SO.sub.2 Me HOMe Y3 SO.sub.2 Me HOMe Y4 SO.sub.2 Me HOMe Y5 SO.sub.2 Me HOMe Y6 SO.sub.2 Me HOMe Y7 SO.sub.2 Me HOMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCHMeCHCH.sub.2 SO.sub.2 Me HOMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CHCHMe SO.sub.2 Me HOMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CCH SO.sub.2 Me HOMe OCHMeCCH SO.sub.2 Me HOMe OCMe.sub.2 CCH SO.sub.2 Me HOMe OCH.sub.2 CCMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HOMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe OCHMeCH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HOMe Y8 SO.sub.2 Me HOMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CClCHCl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HOMe OPh SO.sub.2 Me HOMe OPhMe-2 SO.sub.2 Me HOMe OPhCl-4 SO.sub.2 Me HOMe OPhNO.sub.2 -4 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HOMe OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CHMeOMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HOMe OCH.sub.2 Ph SO.sub.2 Me HOMe OCHMePh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HOMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HOMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HOMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HOMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HOMe Y9 SO.sub.2 Me HOMe Y10 SO.sub.2 Me HOMe Y11 SO.sub.2 Me HOMe Y12 SO.sub.2 Me HOMe Y13 SO.sub.2 Me HOMe Y14 SO.sub.2 Me HOMe Y15 SO.sub.2 Me HOMe Y16 SO.sub.2 Me HOMe Y17 SO.sub.2 Me HOMe Y18 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub. 2 Me HOMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HOMe Y19 SO.sub.2 Me HOMe OCH.sub.2 COOMe SO.sub.2 Me HOMe OCH.sub.2 COOEt SO.sub.2 Me HOMe OCH.sub.2 COOPr-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-t SO.sub.2 Me HOMe OCH.sub.2 COOY4 SO.sub.2 Me HOMe OCHMeCOOMe SO.sub.2 Me HOMe OCHMeCOOEt SO.sub.2 Me HOMe OCHMeCOOPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HOMe OCH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HOMe OCOOMe SO.sub.2 Me HOMe OCOOPr-i SO.sub.2 Me HOMe OCONH.sub.2 SO.sub.2 Me HOMe OCONHMe SO.sub.2 Me HOMe OCONMe.sub.2 SO.sub.2 Me HOMe OP(O)(OMe).sub.2 SO.sub.2 Me HOMe Y20 SO.sub.2 Me HOMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CCH SO.sub.2 Me HOMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe Y21 SO.sub.2 Me HOMe SPh SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe Y22 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CCH SO.sub.2 Me HOMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y23 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y24 SO.sub.2 Me HOMe Y25 SO.sub.2 Me HOMe SO.sub.2 Ph SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub. 2 PhOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OEt Cl HOMe OCH.sub.2 CH.sub.2 OPr-i Cl HOMe OCHMeCH.sub.2 OMe Cl HOMe OCH.sub.2 COOMe Cl HOMe OCH.sub.2 CH.sub.2 SMe Cl HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HOMe SCH.sub.2 CH.sub.2 OMe Cl HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe SCH.sub. 2 CH.sub.2 OEt Cl CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe Y1 SO.sub.2 Me HCH.sub.2 OMe Y2 SO.sub.2 Me HCH.sub.2 OMe Y3 SO.sub.2 Me HCH.sub.2 OMe Y4 SO.sub.2 Me HCH.sub.2 OMe Y5 SO.sub.2 Me HCH.sub.2 OMe Y6 SO.sub.2 Me HCH.sub.2 OMe Y7 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCHMeCHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCHMeCCH SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCH.sub.2 OMe Y8 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCHCl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe OPh SO.sub.2 Me HCH.sub.2 OMe OPhMe-2 SO.sub.2 Me HCH.sub.2 OMe OPhCl-4 SO.sub.2 Me HCH.sub.2 OMe OPhNO.sub.2 -4 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Y4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHMeOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCHMePh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y9 SO.sub.2 Me HCH.sub.2 OMe Y10 SO.sub.2 Me HCH.sub.2 OMe Y11 SO.sub.2 Me HCH.sub.2 OMe Y12 SO.sub.2 Me HCH.sub.2 OMe Y13 SO.sub.2 Me HCH.sub.2 OMe Y14 SO.sub.2 Me HCH.sub.2 OMe Y15 SO.sub.2 Me HCH.sub.2 OMe Y16 SO.sub.2 Me HCH.sub.2 OMe Y17 SO.sub.2 Me HCH.sub.2 OMe Y18 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y19 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOY4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOMe SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCH.sub.2 OMe OCOOMe SO.sub.2 Me HCH.sub.2 OMe OCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCONHMe SO.sub.2 Me HCH.sub.2 OMe OCONMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me HCH.sub.2 OMe Y20 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe Y21 SO.sub.2 Me HCH.sub.2 OMe SPh SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe Y22 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y23 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y24 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i Cl HCH.sub.2 OMe OCHMeCH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 COOMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh______________________________________
TABLE 5______________________________________ ##STR36##X Y Z Q______________________________________Me Y1 SO.sub.2 Me HMe Y2 SO.sub.2 Me HMe Y3 SO.sub.2 Me HMe Y4 SO.sub.2 Me HMe Y5 SO.sub.2 Me HMe Y6 SO.sub.2 Me HMe Y7 SO.sub.2 Me HMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCHMeCH CH.sub.2 SO.sub.2 Me HMe OCMe.sub.2 CH CH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CMe CH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CHCHMe SO.sub.2 Me HMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CH CH.sub.2 SO.sub.2 Me HMe OCH.sub.2 C CH SO.sub.2 Me HMe OCHMeC CH SO.sub.2 Me HMe OCHMe.sub.2 CCH SO.sub.2 Me HMe OCH.sub.2 CCMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe OCHMeCH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HMe Y8 SO.sub.2 Me HMe OCH.sub.2 CCl CH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CCl CHCl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HMe OPh SO.sub.2 Me HMe OPhMe-2 SO.sub.2 Me HMe OPhCl-4 SO.sub.2 Me HMe OPhNO.sub.2 -4 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HMe OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CHMeOMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HMe OCH.sub.2 Ph SO.sub.2 Me HMe OCHMePh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HMe OCH.sub. 2 Ph-4-OMe SO.sub.2 Me HMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HMe Y9 SO.sub.2 Me HMe Y10 SO.sub.2 Me HMe Y11 SO.sub.2 Me HMe Y12 SO.sub.2 Me HMe Y13 SO.sub.2 Me HMe Y14 SO.sub.2 Me HMe Y15 SO.sub.2 Me HMe Y16 SO.sub.2 Me HMe Y17 SO.sub.2 Me HMe Y18 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HMe Y19 SO.sub.2 Me HMe OCH.sub.2 COOMe SO.sub.2 Me HMe OCH.sub.2 COOEt SO.sub.2 Me HMe OCH.sub.2 COOPr-i SO.sub.2 Me HMe OCH.sub.2 COOBu-i SO.sub.2 Me HMe OCH.sub.2 COOBu-t SO.sub.2 Me HMe OCH.sub.2 COOY4 SO.sub.2 Me HMe OCHMeCOOMe SO.sub.2 Me HMe OCHMeCOOEt SO.sub.2 Me HMe OCHMeCOOPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HMe OCH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HMe OCOOMe SO.sub.2 Me HMe OCOOPr-i SO.sub.2 Me HMe OCONH.sub.2 SO.sub.2 Me HMe OCONHMe SO.sub.2 Me HMe OCONMe.sub.2 SO.sub.2 Me HMe OP(O)(OMe).sub.2 SO.sub.2 Me HMe Y20 SO.sub.2 Me HMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SCH.sub.2 C CH SO.sub.2 Me HMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe Y21 SO.sub.2 Me HMe SPh SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe Y22 SO.sub.2 Me HMe S(O)CH.sub.2 CH CH.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CH CMe.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CCH SO.sub.2 Me HMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y23 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 C CH SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y24 SO.sub.2 Me HMe Y25 SO.sub.2 Me HMe SO.sub.2 Ph SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OEt Cl HMe OCH.sub.2 CH.sub.2 OPr-i Cl HMe OCHMeCH.sub.2 OMe Cl HMe OCH.sub.2 COOMe Cl HMe OCH.sub.2 CH.sub.2 SMe Cl HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HMe SCH.sub.2 CH.sub.2 OMe Cl HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhMe SCH.sub.2 SH.sub.2 OMe Cl CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl Y1 SO.sub.2 Me HCl Y2 SO.sub.2 Me HCl Y3 SO.sub.2 Me HCl Y4 SO.sub.2 Me HCl Y5 SO.sub.2 Me HCl Y6 SO.sub.2 Me HCl Y7 SO.sub.2 Me HCl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCHMeCH CH.sub.2 SO.sub.2 Me HCl OCMe.sub.2 CH CH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CMe CH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CHCHMe SO.sub.2 Me HCl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CH CH.sub.2 SO.sub.2 Me HCl OCH.sub.2 C CH SO.sub.2 Me HCl OCHMeCCH SO.sub.2 Me HCl OCHMe.sub.2 CCH SO.sub.2 Me HCl OCH.sub.2 CCMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCl OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCl OCH.sub.2 CF.sub.3 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl OCHMeCH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCl Y8 SO.sub.2 Me HCl OCH.sub.2 CCl CH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CCl CHCl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCl OPh SO.sub.2 Me HCl OPhMe-2 SO.sub.2 Me HCl OPhCl-4 SO.sub.2 Me HCl OPhNO.sub.2 -4 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HCl OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CHMeOMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCl OCH.sub.2 Ph SO.sub.2 Me HCl OCHMePh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCl OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCl OCH.sub.2 Ph-3-Me SO.sub.2 Me HCl OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCl Y9 SO.sub.2 Me HCl Y10 SO.sub.2 Me HCl Y11 SO.sub.2 Me HCl Y12 SO.sub.2 Me HCl Y13 SO.sub.2 Me HCl Y14 SO.sub.2 Me HCl Y15 SO.sub.2 Me HCl Y16 SO.sub.2 Me HCl Y17 SO.sub.2 Me HCl Y18 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCl Y19 SO.sub.2 Me HCl OCH.sub.2 COOMe SO.sub.2 Me HCl OCH.sub.2 COOEt SO.sub.2 Me HCl OCH.sub.2 COOPr-i SO.sub.2 Me HCl OCH.sub.2 COOBu-i SO.sub.2 Me HCl OCH.sub.2 COOBu-t SO.sub.2 Me HCl OCH.sub.2 COOY4 SO.sub.2 Me HCl OCHMeCOOMe SO.sub.2 Me HCl OCHMeCOOEt SO.sub.2 Me HCl OCHMeCOOPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCl OCH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CO.sub.2 Pr-i SO.sub.2 Me HCl OCOOMe SO.sub.2 Me HCl OCOOPr-i SO.sub.2 Me HCl OCONH.sub.2 SO.sub.2 Me HCl OCONHMe SO.sub.2 Me HCl OCONMe.sub.2 SO.sub.2 Me HCl OP(O)(OMe).sub.2 SO.sub.2 Me HCl Y20 SO.sub.2 Me HCl SCH.sub.2 CHCH.sub.2 SO.sub. 2 Me HCl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SCH.sub.2 C CH SO.sub.2 Me HCl SCH.sub.2 CF.sub.3 SO.sub.2 Me HCl SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl Y21 SO.sub.2 Me HCl SPh SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl Y22 SO.sub.2 Me HCl S(O)CH.sub.2 CH CH.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CH CMe.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CCH SO.sub.2 Me HCl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y23 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 C CH SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y24 SO.sub.2 Me HCl Y25 SO.sub.2 Me HCl SO.sub.2 Ph SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OEt Cl HCl OCH.sub.2 CH.sub.2 OPr-i Cl HCl OCHMeCH.sub.2 OMe Cl HCl OCH.sub.2 COOMe Cl HCl OCH.sub.2 CH.sub.2 SMe Cl HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCl SCH.sub.2 CH.sub.2 OMe Cl HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe Y1 SO.sub.2 Me HOMe Y2 SO.sub.2 Me HOMe Y3 SO.sub.2 Me HOMe Y4 SO.sub.2 Me HOMe Y5 SO.sub.2 Me HOMe Y6 SO.sub.2 Me HOMe Y7 SO.sub.2 Me HOMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCHMeCH CH.sub.2 SO.sub.2 Me HOMe OCMe.sub.2 CH CH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CMe CH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CHCHMe SO.sub.2 Me HOMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CH CH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 C CH SO.sub.2 Me HOMe OCHMeCCH SO.sub.2 Me HOMe OCHMe.sub.2 CCH SO.sub.2 Me HOMe OCH.sub.2 CCMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HOMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe OCHMeCH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HOMe Y8 SO.sub.2 Me HOMe OCH.sub.2 CCl CH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CCl CHCl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HOMe OPh SO.sub.2 Me HOMe OPhMe-2 SO.sub.2 Me HOMe OPhCl-4 SO.sub.2 Me HOMe OPhNO.sub.2 -4 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HOMe OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CHMeOMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HOMe OCH.sub.2 Ph SO.sub.2 Me HOMe OCHMePh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HOMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HOMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HOMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HOMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HOMe Y9 SO.sub.2 Me HOMe Y10 SO.sub.2 Me HOMe Y11 SO.sub.2 Me HOMe Y12 SO.sub.2 Me HOMe Y13 SO.sub.2 Me HOMe Y14 SO.sub.2 Me HOMe Y15 SO.sub.2 Me HOMe Y16 SO.sub.2 Me HOMe Y17 SO.sub.2 Me HOMe Y18 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HOMe Y19 SO.sub.2 Me HOMe OCH.sub.2 COOMe SO.sub.2 Me HOMe OCH.sub.2 COOEt SO.sub.2 Me HOMe OCH.sub.2 COOPr-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-t SO.sub.2 Me HOMe OCH.sub.2 COOY4 SO.sub.2 Me HOMe OCHMeCOOMe SO.sub.2 Me HOMe OCHMeCOOEt SO.sub.2 Me HOMe OCHMeCOOPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HOMe OCH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HOMe OCOOMe SO.sub.2 Me HOMe OCOOPr-i SO.sub.2 Me HOMe OCONH.sub.2 SO.sub.2 Me HOMe OCONHMe SO.sub.2 Me HOMe OCONMe.sub.2 SO.sub.2 Me HOMe OP(O)(OMe).sub.2 SO.sub.2 Me HOMe Y20 SO.sub.2 Me HOMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CCH SO.sub.2 Me HOMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe Y21 SO.sub.2 Me HOMe SPh SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe Y22 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CCH SO.sub.2 Me HOMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y23 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y24 SO.sub.2 Me HOMe Y25 SO.sub.2 Me HOMe SO.sub.2 Ph SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OEt Cl HOMe OCH.sub.2 CH.sub.2 OPr-i Cl HOMe OCHMeCH.sub.2 OMe Cl HOMe OCH.sub.2 COOMe Cl HOMe OCH.sub.2 CH.sub.2 SMe Cl HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HOMe SCH.sub.2 CH.sub.2 OMe Cl HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhOMe SCH.sub.2 SH.sub.2 OMe Cl CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe Y1 SO.sub.2 Me HCH.sub.2 OMe Y2 SO.sub.2 Me HCH.sub.2 OMe Y3 SO.sub.2 Me HCH.sub.2 OMe Y4 SO.sub.2 Me HCH.sub.2 OMe Y5 SO.sub.2 Me HCH.sub.2 OMe Y6 SO.sub.2 Me HCH.sub.2 OMe Y7 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH CH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 CH CH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CMe CH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CH CH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub. 2 C CH SO.sub.2 Me HCH.sub.2 OMe OCHMeCCH SO.sub.2 Me HCH.sub.2 OMe OCHMe.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCH.sub.2 OMe Y8 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCl CH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCl CHCl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe OPh SO.sub.2 Me HCH.sub.2 OMe OPhMe-2 SO.sub.2 Me HCH.sub.2 OMe OPhCl-4 SO.sub.2 Me HCH.sub.2 OMe OPhNO.sub.2 -4 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHMeOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCHMePh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y9 SO.sub.2 Me HCH.sub.2 OMe Y10 SO.sub.2 Me HCH.sub.2 OMe Y11 SO.sub.2 Me HCH.sub.2 OMe Y12 SO.sub.2 Me HCH.sub.2 OMe Y13 SO.sub.2 Me HCH.sub.2 OMe Y14 SO.sub.2 Me HCH.sub.2 OMe Y15 SO.sub.2 Me HCH.sub.2 OMe Y16 SO.sub.2 Me HCH.sub.2 OMe Y17 SO.sub.2 Me HCH.sub.2 OMe Y18 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y19 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOY4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOMe SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CO.sub.2 Pr-i SO.sub.2 Me HCH.sub.2 OMe OCOOMe SO.sub.2 Me HCH.sub.2 OMe OCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCONHMe SO.sub.2 Me HCH.sub.2 OMe OCONMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me HCH.sub.2 OMe Y20 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 C CH SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe Y21 SO.sub.2 Me HCH.sub.2 OMe SPh SO.sub.2 Me HCH.sub.2 OMe SCH.sub. 2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe Y22 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH CH.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH CMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y23 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 C CH SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y24 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub. 2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i Cl HCH.sub.2 OMe OCHMeCH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 COOMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh______________________________________
TABLE 6______________________________________ ##STR37##X Y Z Q______________________________________Me Y1 SO.sub.2 Me HMe Y2 SO.sub.2 Me HMe Y3 SO.sub.2 Me HMe Y4 SO.sub.2 Me HMe Y5 SO.sub.2 Me HMe Y6 SO.sub.2 Me HMe Y7 SO.sub.2 Me HMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCHMeCHCH.sub.2 SO.sub.2 Me HMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CHCHMe SO.sub.2 Me HMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CCH SO.sub.2 Me HMe OCHMeC CH SO.sub.2 Me HMe OCMe.sub.2 CCH SO.sub.2 Me HMe OCH.sub.2 CCMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe OCHMeCH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HMe Y8 SO.sub.2 Me HMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CClCHCl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HMe OPh SO.sub.2 Me HMe OPhMe-2 SO.sub.2 Me HMe OPhCl-4 SO.sub.2 Me HMe OPhNO.sub.2 -4 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub. 2 OEt SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HMe OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CHMeOMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HMe OCH.sub.2 Ph SO.sub.2 Me HMe OCHMePh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HMe Y9 SO.sub.2 Me HMe Y10 SO.sub.2 Me HMe Y11 SO.sub.2 Me HMe Y12 SO.sub.2 Me HMe Y13 SO.sub.2 Me HMe Y14 SO.sub.2 Me HMe Y15 SO.sub.2 Me HMe Y16 SO.sub.2 Me HMe Y17 SO.sub.2 Me HMe Y18 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HMe Y19 SO.sub.2 Me HMe OCH.sub.2 COOMe SO.sub.2 Me HMe OCH.sub.2 COOEt SO.sub.2 Me HMe OCH.sub.2 COOPr-i SO.sub.2 Me HMe OCH.sub.2 COOBu-i SO.sub.2 Me HMe OCH.sub.2 COOBu-t SO.sub.2 Me HMe OCH.sub.2 COOY4 SO.sub.2 Me HMe OCHMeCOOMe SO.sub.2 Me HMe OCHMeCOOEt SO.sub.2 Me HMe OCHMeCOOPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HMe OCH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HMe OCOOMe SO.sub.2 Me HMe OCOOPr-i SO.sub.2 Me HMe OCONH.sub.2 SO.sub.2 Me HMe OCONHMe SO.sub.2 Me HMe OCONMe.sub.2 SO.sub.2 Me HMe OP(O)(OMe).sub.2 SO.sub.2 Me HMe Y20 SO.sub.2 Me HMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SCH.sub.2 CCH SO.sub.2 Me HMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe Y21 SO.sub.2 Me HMe SPh SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe Y22 SO.sub.2 Me HMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CCH SO.sub.2 Me HMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y23 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y24 SO.sub.2 Me HMe Y25 SO.sub.2 Me HMe SO.sub.2 Ph SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OEt Cl HMe OCH.sub.2 CH.sub.2 OPr-i Cl HMe OCHMeCH.sub.2 OMe Cl HMe OCH.sub.2 COOMe Cl HMe OCH.sub.2 CH.sub.2 SMe Cl HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HMe SCH.sub.2 CH.sub.2 OMe Cl HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub. 2 CH.sub.2 SMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl Y1 SO.sub.2 Me HCl Y2 SO.sub.2 Me HCl Y3 SO.sub.2 Me HCl Y4 SO.sub.2 Me HCl Y5 SO.sub.2 Me HCl Y6 SO.sub.2 Me HCl Y7 SO.sub.2 Me HCl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCHMeCHCH.sub.2 SO.sub.2 Me HCl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH CHMe SO.sub.2 Me HCl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CCH SO.sub.2 Me HCl OCHMeCCH SO.sub.2 Me HCl OCMe.sub.2 CCH SO.sub.2 Me HCl OCH.sub.2 CCMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCl OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCl OCH.sub.2 CF.sub.3 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl OCHMeCH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCl Y8 SO.sub.2 Me HCl OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CClCHCl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCl OPh SO.sub.2 Me HCl OPhMe-2 SO.sub.2 Me HCl OPhCl-4 SO.sub.2 Me HCl OPhNO.sub.2 -4 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HCl OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CHMeOMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCl OCH.sub.2 Ph SO.sub.2 Me HCl OCHMePh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCl OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCl OCH.sub.2 Ph-3-Me SO.sub.2 Me HCl OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCl Y9 SO.sub.2 Me HCl Y10 SO.sub.2 Me HCl Y11 SO.sub.2 Me HCl Y12 SO.sub.2 Me HCl Y13 SO.sub.2 Me HCl Y14 SO.sub.2 Me HCl Y15 SO.sub.2 Me HCl Y16 SO.sub.2 Me HCl Y17 SO.sub.2 Me HCl Y18 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCl Y19 SO.sub.2 Me HCl OCH.sub.2 COOMe SO.sub.2 Me HCl OCH.sub.2 COOEt SO.sub.2 Me HCl OCH.sub.2 COOPr-i SO.sub.2 Me HCl OCH.sub.2 COOBu-i SO.sub.2 Me HCl OCH.sub.2 COOBu-t SO.sub.2 Me HCl OCH.sub.2 COOY4 SO.sub.2 Me HCl OCHMeCOOMe SO.sub.2 Me HCl OCHMeCOOEt SO.sub.2 Me HCl OCHMeCOOPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCl OCH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCl OCOOMe SO.sub.2 Me HCl OCOOPr-i SO.sub.2 Me HCl OCONH.sub.2 SO.sub.2 Me HCl OCONHMe SO.sub.2 Me HCl OCONMe.sub.2 SO.sub.2 Me HCl OP(O)(OMe).sub.2 SO.sub.2 Me HCl Y20 SO.sub.2 Me HCl SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SCH.sub.2 C CH SO.sub.2 Me HCl SCH.sub.2 CF.sub.3 SO.sub.2 Me HCl SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl Y21 SO.sub.2 Me HCl SPh SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl Y22 SO.sub.2 Me HCl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CCH SO.sub.2 Me HCl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y23 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y24 SO.sub.2 Me HCl Y25 SO.sub.2 Me HCl SO.sub.2 Ph SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub. 2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OEt Cl HCl OCH.sub.2 CH.sub.2 OPr-i Cl HCl OCHMeCH.sub.2 OMe Cl HCl OCH.sub.2 COOMe Cl HCl OCH.sub.2 CH.sub.2 SMe Cl HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCl SCH.sub.2 CH.sub.2 OMe Cl HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe Y1 SO.sub.2 Me HOMe Y2 SO.sub.2 Me HOMe Y3 SO.sub.2 Me HOMe Y4 SO.sub.2 Me HOMe Y5 SO.sub.2 Me HOMe Y6 SO.sub.2 Me HOMe Y7 SO.sub.2 Me HOMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCHMeCHCH.sub.2 SO.sub.2 Me HOMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CHCHMe SO.sub.2 Me HOMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CCH SO.sub.2 Me HOMe OCHMeCCH SO.sub.2 Me HOMe OCMe.sub.2 CCH SO.sub.2 Me HOMe OCH.sub.2 CCMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HOMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe OCHMeCH.sub. 2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HOMe Y8 SO.sub.2 Me HOMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CClCHCl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HOMe OPh SO.sub.2 Me HOMe OPhMe-2 SO.sub.2 Me HOMe OPhCl-4 SO.sub.2 Me HOMe OPhNO.sub.2 -4 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HOMe OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CHMeOMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HOMe OCH.sub.2 Ph SO.sub.2 Me HOMe OCHMePh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HOMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HOMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HOMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HOMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HOMe Y9 SO.sub.2 Me HOMe Y10 SO.sub.2 Me HOMe Y11 SO.sub.2 Me HOMe Y12 SO.sub.2 Me HOMe Y13 SO.sub.2 Me HOMe Y14 SO.sub.2 Me HOMe Y15 SO.sub.2 Me HOMe Y16 SO.sub.2 Me HOMe Y17 SO.sub.2 Me HOMe Y18 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HOMe Y19 SO.sub.2 Me HOMe OCH.sub.2 COOMe SO.sub.2 Me HOMe OCH.sub.2 COOEt SO.sub.2 Me HOMe OCH.sub.2 COOPr-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-t SO.sub.2 Me HOMe OCH.sub.2 COOY4 SO.sub.2 Me HOMe OCHMeCOOMe SO.sub.2 Me HOMe OCHMeCOOEt SO.sub.2 Me HOMe OCHMeCOOPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HOMe OCH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HOMe OCOOMe SO.sub.2 Me HOMe OCOOPr-i SO.sub.2 Me HOMe OCONH.sub.2 SO.sub. 2 Me HOMe OCONHMe SO.sub.2 Me HOMe OCONMe.sub.2 SO.sub.2 Me HOMe OP(O)(OMe).sub.2 SO.sub.2 Me HOMe Y20 SO.sub.2 Me HOMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CCH SO.sub.2 Me HOMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe Y21 SO.sub.2 Me HOMe SPh SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe Y22 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CCH SO.sub.2 Me HOMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y23 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SO.sub. 2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y24 SO.sub.2 Me HOMe Y25 SO.sub.2 Me HOMe SO.sub.2 Ph SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub. 2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub. 2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OEt Cl HOMe OCH.sub.2 CH.sub.2 OPr-i Cl HOMe OCHMeCH.sub.2 OMe Cl HOMe OCH.sub.2 COOMe Cl HOMe OCH.sub.2 CH.sub.2 SMe Cl HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HOMe SCH.sub.2 CH.sub.2 OMe Cl HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe Y1 SO.sub.2 Me HCH.sub.2 OMe Y2 SO.sub.2 Me HCH.sub.2 OMe Y3 SO.sub.2 Me HCH.sub.2 OMe Y4 SO.sub.2 Me HCH.sub.2 OMe Y5 SO.sub.2 Me HCH.sub.2 OMe Y6 SO.sub.2 Me HCH.sub.2 OMe Y7 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCHMeCHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCHMeCCH SO.sub.2 Me HCH.sub. 2 OMe OCMe.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCH.sub.2 OMe Y8 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCHCl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe OPh SO.sub.2 Me HCH.sub.2 OMe OPhMe-2 SO.sub.2 Me HCH.sub.2 OMe OPhCl-4 SO.sub.2 Me HCH.sub.2 OMe OPhNO.sub.2 -4 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHMeOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCHMePh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y9 SO.sub.2 Me HCH.sub.2 OMe Y10 SO.sub.2 Me HCH.sub.2 OMe Y11 SO.sub.2 Me HCH.sub.2 OMe Y12 SO.sub.2 Me HCH.sub.2 OMe Y13 SO.sub.2 Me HCH.sub.2 OMe Y14 SO.sub.2 Me HCH.sub.2 OMe Y15 SO.sub.2 Me HCH.sub.2 OMe Y16 SO.sub.2 Me HCH.sub.2 OMe Y17 SO.sub.2 Me HCH.sub.2 OMe Y18 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y19 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOY4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOMe SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCH.sub.2 OMe OCOOMe SO.sub.2 Me HCH.sub.2 OMe OCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCONHMe SO.sub.2 Me HCH.sub.2 OMe OCONMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me HCH.sub.2 OMe Y20 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe Y21 SO.sub.2 Me HCH.sub.2 OMe SPh SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe Y22 SO.sub.2 Me HCH.sub. 2 OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y23 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y24 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub. 2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i Cl HCH.sub.2 OMe OCHMeCH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 COOMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh______________________________________
TABLE 7______________________________________ ##STR38##X Y Z Q______________________________________Me Y1 SO.sub.2 Me HMe Y2 SO.sub.2 Me HMe Y3 SO.sub.2 Me HMe Y4 SO.sub.2 Me HMe Y5 SO.sub.2 Me HMe Y6 SO.sub.2 Me HMe Y7 SO.sub.2 Me HMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCHMeCHCH.sub.2 SO.sub.2 Me HMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CHCHMe SO.sub.2 Me HMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CCH SO.sub.2 Me HMe OCHMeC CH SO.sub.2 Me HMe OCMe.sub.2 CCH SO.sub.2 Me HMe OCH.sub.2 CCMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe OCHMeCH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HMe Y8 SO.sub.2 Me HMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CClCHCl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HMe OPh SO.sub.2 Me HMe OPhMe-2 SO.sub.2 Me HMe OPhCl-4 SO.sub.2 Me HMe OPhNO.sub.2 -4 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OEt SO.sub. 2 Me HMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 -Y4 SO.sub.2 Me HMe OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CHMeOMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HMe OCH.sub.2 Ph SO.sub.2 Me HMe OCHMePh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HMe Y9 SO.sub.2 Me HMe Y10 SO.sub.2 Me HMe Y11 SO.sub.2 Me HMe Y12 SO.sub.2 Me HMe Y13 SO.sub.2 Me HMe Y14 SO.sub.2 Me HMe Y15 SO.sub.2 Me HMe Y16 SO.sub.2 Me HMe Y17 SO.sub.2 Me HMe Y18 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HMe Y19 SO.sub.2 Me HMe OCH.sub.2 COOMe SO.sub.2 Me HMe OCH.sub.2 COOEt SO.sub.2 Me HMe OCH.sub.2 COOPr-i SO.sub.2 Me HMe OCH.sub.2 COOBu-i SO.sub.2 Me HMe OCH.sub.2 COOBu-t SO.sub.2 Me HMe OCH.sub.2 COO-Y4 SO.sub.2 Me HMe OCHMeCOOMe SO.sub.2 Me HMe OCHMeCOOEt SO.sub.2 Me HMe OCHMeCOOPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HMe OCH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HMe OCOOMe SO.sub.2 Me HMe OCOOPr-i SO.sub.2 Me HMe OCONHG.sub.2 SO.sub.2 Me HMe OCONHMe SO.sub.2 Me HMe OCONMe.sub.2 SO.sub.2 Me HMe OP(O)(OMe).sub.2 SO.sub.2 Me HMe Y20 SO.sub.2 Me HMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SCH.sub.2 CCH SO.sub.2 Me HMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe Y21 SO.sub.2 Me HMe SPh SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SCH.sub.2 CH.sub. 2 OEt SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe Y22 SO.sub.2 Me HMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CCH SO.sub.2 Me HMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y23 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y24 SO.sub.2 Me HMe Y25 SO.sub.2 Me HMe SO.sub.2 Ph SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OEt Cl HMe OCH.sub.2 CH.sub.2 OPr-i Cl HMe OCHMeCH.sub.2 OMe Cl HMe OCH.sub.2 COOMe Cl HMe OCH.sub.2 CH.sub.2 SMe Cl HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HMe SCH.sub.2 CH.sub.2 OMe Cl HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl Y1 SO.sub.2 Me HCl Y2 SO.sub.2 Me HCl Y3 SO.sub.2 Me HCl Y4 SO.sub.2 Me HCl Y5 SO.sub.2 Me HCl Y6 SO.sub.2 Me HCl Y7 SO.sub.2 Me HCl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCHMeCHCH.sub.2 SO.sub.2 Me HCl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CHCHMe SO.sub.2 Me HCl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CCH SO.sub.2 Me HCl OCHMeCCH SO.sub.2 Me HCl OCMe.sub.2 CCH SO.sub.2 Me HCl OCH.sub.2 CCMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCl OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCl OCH.sub.2 CF.sub.3 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl OCHMeCH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCl Y8 SO.sub.2 Me HCl OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CClCHCl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NO.sub. 2 SO.sub.2 Me HCl OPh SO.sub.2 Me HCl OPh-Me-2 SO.sub.2 Me HCl OPh-Cl-4 SO.sub.2 Me HCl OPh-NO.sub.2 -4 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCl OCH.sub.2 CH.sub.2-Y4 SO.sub.2 Me HCl OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CHMeOMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCl OCH.sub.2 Ph SO.sub.2 Me HCl OCHMePh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCl OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCl OCH.sub.2 Ph-3-Me SO.sub.2 Me HCl OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCl Y9 SO.sub.2 Me HCl Y10 SO.sub.2 Me HCl Y11 SO.sub.2 Me HCl Y12 SO.sub.2 Me HCl Y13 SO.sub.2 Me HCl Y14 SO.sub.2 Me HCl Y15 SO.sub.2 Me HCl Y16 SO.sub.2 Me HCl Y17 SO.sub.2 Me HCl Y18 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCl Y19 SO.sub.2 Me HCl OCH.sub.2 COOMe SO.sub.2 Me HCl OCH.sub.2 COOEt SO.sub.2 Me HCl OCH.sub.2 COOPr-i SO.sub.2 Me HCl OCH.sub.2 COOBu-i SO.sub.2 Me HCl OCH.sub.2 COOBu-t SO.sub.2 Me HCl OCH.sub.2 COO-Y4 SO.sub.2 Me HCl OCHMeCOOMe SO.sub.2 Me HCl OCHMeCOOEt SO.sub.2 Me HCl OCHMeCOOPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCl OCH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCl OCOOMe SO.sub.2 Me HCl OCOOPr-i SO.sub.2 Me HCl OCONH.sub.2 SO.sub.2 Me HCl OCONHMe SO.sub.2 Me HCl OCONMe.sub.2 SO.sub.2 Me HCl OP(O)(OMe).sub.2 SO.sub.2 Me HCl Y20 SO.sub.2 Me HCl SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SCH.sub.2 CCH SO.sub. 2 Me HCl SCH.sub.2 CF.sub.3 SO.sub.2 Me HCl SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl Y21 SO.sub.2 Me HCl SPh SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl Y22 SO.sub.2 Me HCl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CCH SO.sub.2 Me HCl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y23 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y24 SO.sub.2 Me HCl Y25 SO.sub.2 Me HCl SO.sub.2 Ph SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SO.sub.2 CH.sub.2 cH.sub.2 OEt SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.3 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OEt Cl HCl OCH.sub.2 CH.sub.2 OPr-i Cl HCl OCHMeCH.sub.2 OMe Cl HCl OCH.sub.2 COOMe Cl HCl OCH.sub.2 CH.sub. 2 SMe Cl HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCl SCH.sub.2 CH.sub.2 OMe Cl HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe Y1 SO.sub.2 Me HOMe Y2 SO.sub.2 Me HOMe Y3 SO.sub.2 Me HOMe Y4 SO.sub.2 Me HOMe Y5 SO.sub.2 Me HOMe Y6 SO.sub.2 Me HOMe Y7 SO.sub.2 Me HOMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCHMdCHCH.sub.2 SO.sub.2 Me HOMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CHCHMe SO.sub.2 Me HOMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CCH SO.sub.2 Me HOMe OCHMeCCH SO.sub.2 Me HOMe OCMe.sub.2 CCH SO.sub.2 Me HOMe OCH.sub.2 CCMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HOMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe OCHMeCH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub. 2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HOMe Y8 SO.sub.2 Me HOMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CClCHCl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HOMe OPh SO.sub.2 Me HOMe OPhMe-2 SO.sub.2 Me HOMe OPhCl-4 SO.sub.2 Me HOMe OPhNO.sub.2 -4 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 -Y4 SO.sub.2 Me HOMe OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CHMeOMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HOMe OCH.sub.2 Ph SO.sub.2 Me HOMe OCHMePh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HOMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HOMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HOMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HOMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HOMe Y9 SO.sub.2 Me HOMe Y10 SO.sub.2 Me HOMe Y11 SO.sub.2 Me HOMe Y12 SO.sub.2 Me HOMe Y13 SO.sub.2 Me HOMe Y14 SO.sub.2 Me HOMe Y15 SO.sub.2 Me HOMe Y16 SO.sub.2 Me HOMe Y17 SO.sub.2 Me HOMe Y18 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HOMe Y19 SO.sub.2 Me HOMe OCH.sub.2 COOMe SO.sub.2 Me HOMe OCH.sub.2 COOEt SO.sub.2 Me HOMe OCH.sub.2 COOPr-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-t SO.sub.2 Me HOMe OCH.sub.2 COO-Y4 SO.sub.2 Me HOMe OCHMeCOOMe SO.sub.2 Me HOMe OCHMeCOOEt SO.sub.2 Me HOMe OCHMeCOOPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HOMe OCH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HOMe OCOOMe SO.sub.2 Me HOMe OCOOPr-i SO.sub.2 Me HOMe OCONH.sub.2 SO.sub.2 Me HOMe OCONHMe SO.sub.2 Me HOMe OCONMe.sub. 2 SO.sub.2 Me HOMe OP(O)(OMe).sub.2 SO.sub.2 Me HOMe Y20 SO.sub.2 Me HOMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CCH SO.sub.2 Me HOMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe Y21 SO.sub.2 Me HOMe SPh SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe Y22 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CCH SO.sub.2 Me HOMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y23 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y24 SO.sub.2 Me HOMe Y25 SO.sub.2 Me HOMe SO.sub.2 Ph SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub. 2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.1 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub. 2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OEt Cl HOMe OCH.sub.2 CH.sub.2 OPr-i Cl HOMe OCHMeCH.sub.2 OMe Cl HOMe OCH.sub.2 COOMe Cl HOMe OCH.sub.2 CH.sub.2 SMe Cl HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HOMe SCH.sub.2 CH.sub.2 OMe Cl HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe Y1 SO.sub.2 Me HCH.sub.2 OMe Y2 SO.sub.2 Me HCH.sub.2 OMe Y3 SO.sub.2 Me HCH.sub.2 OMe Y4 SO.sub.2 Me HCH.sub.2 OMe Y5 SO.sub.2 Me HCH.sub.2 OMe Y6 SO.sub.2 Me HCH.sub.2 OMe Y7 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCHMeCHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCHMeCCH SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 C CH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCH.sub.2 OMe Y8 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCHCl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe OPh SO.sub.2 Me HCH.sub.2 OMe OPhMe-2 SO.sub.2 Me HCH.sub.2 OMe OPhCl-4 SO.sub.2 Me HCH.sub.2 OMe OPh N.sub.2 -4 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 -Y4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHMeOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCHMePh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y9 SO.sub.2 Me HCH.sub.2 OMe Y10 SO.sub.2 Me HCH.sub.2 OMe Y11 SO.sub.2 Me HCH.sub.2 OMe Y12 SO.sub.2 Me HCH.sub.2 OMe Y13 SO.sub.2 Me HCH.sub.2 OMe Y14 SO.sub.2 Me HCH.sub.2 OMe Y15 SO.sub.2 Me HCH.sub.2 OMe Y16 SO.sub.2 Me HCH.sub.2 OMe Y17 SO.sub.2 Me HCH.sub.2 OMe Y18 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y19 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COO-Y4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOMe SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCH.sub.2 OMe OCOOMe SO.sub.2 Me HCH.sub.2 OMe OCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCONHMe SO.sub.2 Me HCH.sub.2 OMe OCONMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me HCH.sub.2 OMe Y20 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe Y21 SO.sub.2 Me HCH.sub.2 OMe SPh SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe Y22 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH CH.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y23 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y24 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i Cl HCH.sub.2 OMe OCHMeCH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 COOMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh______________________________________
TABLE 8______________________________________ ##STR39##X Y Z Q______________________________________Me Y1 SO.sub.2 Me HMe Y2 SO.sub.2 Me HMe Y3 SO.sub.2 Me HMe Y4 SO.sub.2 Me HMe Y5 SO.sub.2 Me HMe Y6 SO.sub.2 Me HMe Y7 SO.sub.2 Me HMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCHMeCHCH.sub.2 SO.sub.2 Me HMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CHCHMe SO.sub.2 Me HMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CCH SO.sub.2 Me HMe OCHMeC CH SO.sub.2 Me HMe OCMe.sub.2 CCH SO.sub.2 Me HMe OCH.sub.2 CCMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe OCHMeCH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HMe Y8 SO.sub.2 Me HMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CClCHCl SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HMe OPh SO.sub.2 Me HMe OPhMe-2 SO.sub.2 Me HMe OPhCl-4 SO.sub.2 Me HMe OPhNO.sub.2 -4 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Y4 SO.sub.2 Me HMe OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CHMeOMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HMe OCH.sub.2 Ph SO.sub.2 Me HMe OCHMePh SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HMe Y9 SO.sub.2 Me HMe Y10 SO.sub.2 Me HMe Y11 SO.sub.2 Me HMe Y12 SO.sub.2 Me HMe Y13 SO.sub.2 Me HMe Y14 SO.sub.2 Me HMe Y15 SO.sub.2 Me HMe Y16 SO.sub.2 Me HMe Y17 SO.sub.2 Me HMe Y18 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HMe Y19 SO.sub.2 Me HMe OCH.sub.2 COOMe SO.sub.2 Me HMe OCH.sub.2 COOEt SO.sub.2 Me HMe OCH.sub.2 COOPr-i SO.sub.2 Me HMe OCH.sub.2 COOBu-i SO.sub.2 Me HMe OCH.sub.2 COOBu-t SO.sub.2 Me HMe OCH.sub.2 COOY4 SO.sub.2 Me HMe OCHMeCOOMe SO.sub.2 Me HMe OCHMeCOOEt SO.sub.2 Me HMe OCHMeCOOPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HMe OCH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HMe OCOOMe SO.sub.2 Me HMe OCOOPr-i SO.sub.2 Me HMe OCONH.sub.2 SO.sub.2 Me HMe OCONHMe SO.sub.2 Me HMe OCONMe.sub.2 SO.sub.2 Me HMe OP(O)(OMe).sub.2 SO.sub.2 Me HMe Y20 SO.sub.2 Me HMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SCH.sub.2 CCH SO.sub.2 Me HMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HMe Y21 SO.sub.2 Me HMe SPh SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SCH.sub.2 CH.sub. 2 OEt SO.sub.2 Me HMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe Y22 SO.sub.2 Me HMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe S(O)CH.sub.2 CCH SO.sub.2 Me HMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y23 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HMe Y24 SO.sub.2 Me HMe Y25 SO.sub.2 Me HMe SO.sub.2 Ph SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HMe OCH.sub. 2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub. 2 SMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OEt Cl HMe OCH.sub.2 CH.sub.2 OPr-i Cl HMe OCHMeCH.sub.2 OMe Cl HMe OCH.sub.2 COOMe Cl HMe OCH.sub.2 CH.sub.2 SMe Cl HMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HMe SCH.sub.2 CH.sub.2 OMe Cl HMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl Y1 SO.sub.2 Me HCl Y2 SO.sub.2 Me HCl Y3 SO.sub.2 Me HCl Y4 SO.sub.2 Me HCl Y5 SO.sub.2 Me HCl Y6 SO.sub.2 Me HCl Y7 SO.sub.2 Me HCl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCHMeCHCH.sub.2 SO.sub.2 Me HCl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CHCHMe SO.sub.2 Me HCl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CCH SO.sub.2 Me HCl OCHMeCCH SO.sub.2 Me HCl OCMe.sub.2 CCH SO.sub.2 Me HCl OCH.sub.2 CCMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCl OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCl OCH.sub.2 CF.sub.3 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl OCHMeCH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCl Y8 SO.sub.2 Me HCl OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CClCHCl SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCl OPh SO.sub.2 Me HCl OPhMe-2 SO.sub.2 Me HCl OPhCl-4 SO.sub.2 Me HCl OPhNO.sub.2 -4 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HCl OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CHMeOMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCl OCH.sub.2 Ph SO.sub.2 Me HCl OCHMePh SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HCl OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCl OCH.sub.2 Ph-3-Me SO.sub.2 Me HCl OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCl Y9 SO.sub.2 Me HCl Y10 SO.sub.2 Me HCl Y11 SO.sub.2 Me HCl Y12 SO.sub.2 Me HCl Y13 SO.sub.2 Me HCl Y14 SO.sub.2 Me HCl Y15 SO.sub.2 Me HCl Y16 SO.sub.2 Me HCl Y17 SO.sub.2 Me HCl Y18 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCl Y19 SO.sub.2 Me HCl OCH.sub.2 COOMe SO.sub.2 Me HCl OCH.sub.2 COOEt SO.sub.2 Me HCl OCH.sub.2 COOPr-i SO.sub.2 Me HCl OCH.sub.2 COOBu-i SO.sub.2 Me HCl OCH.sub.2 COOBu-t SO.sub.2 Me HCl OCH.sub.2 COO-Y4 SO.sub.2 Me HCl OCHMeCOOMe SO.sub.2 Me HCl OCHMeCOOEt SO.sub.2 Me HCl OCHMeCOOPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCl OCH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCl OCOOMe SO.sub.2 Me HCl OCOOPr-i SO.sub.2 Me HCl OCONH.sub.2 SO.sub.2 Me HCl OCONHMe SO.sub.2 Me HCl OCONMe.sub.2 SO.sub.2 Me HCl OP(O)(OMe).sub.2 SO.sub.2 Me HCl Y20 SO.sub.2 Me HCl SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SCH.sub.2 C CH SO.sub.2 Me HCl SCH.sub.2 CF.sub.3 SO.sub.2 Me HCl SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCl Y21 SO.sub.2 Me HCl SPh SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl Y22 SO.sub.2 Me HCl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y23 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCl Y24 SO.sub.2 Me HCl Y25 SO.sub.2 Me HCl SO.sub.2 Ph SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OEt Cl HCl OCH.sub.2 CH.sub.2 OPr-i Cl HCl OCHMeCH.sub.2 OMe Cl HCl OCH.sub.2 COOMe Cl HCl OCH.sub.2 CH.sub.2 SMe Cl HCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCl SCH.sub.2 CH.sub.2 OMe Cl HCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCl SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe Y1 SO.sub.2 Me HOMe Y2 SO.sub.2 Me HOMe Y3 SO.sub.2 Me HOMe Y4 SO.sub.2 Me HOMe Y5 SO.sub.2 Me HOMe Y6 SO.sub.2 Me HOMe Y7 SO.sub.2 Me HOMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCHMeCHCH.sub.2 SO.sub. 2 Me HOMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CHCHMe SO.sub.2 Me HOMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CCH SO.sub.2 Me HOMe OCHMeCCH SO.sub.2 Me HOMe OCMe.sub.2 CCH SO.sub.2 Me HOMe OCH.sub.2 CCMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HOMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe OCHMeCH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HOMe Y8 SO.sub. 2 Me HOMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CClCHCl SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HOMe OPh SO.sub.2 Me HOMe OPhMe-2 SO.sub.2 Me HOMe OPhCl-4 SO.sub.2 Me HOMe OPhNO.sub.2 -4 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HOMe OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CHMeOMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub. 2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HOMe OCH.sub.2 Ph SO.sub.2 Me HOMe OCHMePh SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me HOMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HOMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HOMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HOMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HOMe Y9 SO.sub.2 Me HOMe Y10 SO.sub.2 Me HOMe Y11 SO.sub.2 Me HOMe Y12 SO.sub.2 Me HOMe Y13 SO.sub.2 Me HOMe Y14 SO.sub.2 Me HOMe Y15 SO.sub.2 Me HOMe Y16 SO.sub.2 Me HOMe Y17 SO.sub.2 Me HOMe Y18 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HOMe Y19 SO.sub.2 Me HOMe OCH.sub.2 COOMe SO.sub.2 Me HOMe OCH.sub.2 COOEt SO.sub.2 Me HOMe OCH.sub.2 COOPr-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-i SO.sub.2 Me HOMe OCH.sub.2 COOBu-t SO.sub.2 Me HOMe OCH.sub.2 COOY4 SO.sub.2 Me HOMe OCHMeCOOMe SO.sub.2 Me HOMe OCHMeCOOEt SO.sub.2 Me HOMe OCHMeCOOPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HOMe OCH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HOMe OCOOMe SO.sub.2 Me HOMe OCOOPr-i SO.sub.2 Me HOMe OCONH.sub.2 SO.sub.2 Me HOMe OCONHMe SO.sub.2 Me HOMe OCONME.sub.2 SO.sub.2 Me HOMe OP(O)(OMe).sub.2 SO.sub.2 Me HOMe Y20 SO.sub.2 Me HOMe SCH.sub. 2 CHCH.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SCH.sub.2 CCH SO.sub.2 Me HOMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HOMe Y21 SO.sub.2 Me HOMe SPh SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe Y22 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe S(O)CH.sub.2 CCH SO.sub.2 Me HOMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y23 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HOMe Y24 SO.sub.2 Me HOMe Y25 SO.sub.2 Me HOMe SO.sub.2 Ph SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhOMe SCH.sub. 2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub. 2 CH.sub.2 OEt Cl HOMe OCH.sub.2 CH.sub.2 OPr-i Cl HOMe OCHMeCH.sub.2 OMe Cl HOMe OCH.sub.2 COOMe Cl HOMe OCH.sub.2 CH.sub.2 SMe Cl HOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HOMe SCH.sub.2 CH.sub.2 OMe Cl HOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhOMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhOMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhOMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhOMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe Y1 SO.sub.2 Me HCH.sub.2 OMe Y2 SO.sub.2 Me HCH.sub.2 OMe Y3 SO.sub.2 Me HCH.sub.2 OMe Y4 SO.sub.2 Me HCH.sub.2 OMe Y5 SO.sub.2 Me HCH.sub.2 OMe Y6 SO.sub.2 Me HCH.sub.2 OMe Y7 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCHMeCHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCHMe.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCHMeCCH SO.sub.2 Me HCH.sub.2 OMe OCMe.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCMe SO.sub. 2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me HCH.sub.2 OMe Y8 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CClCHCl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe OPh SO.sub.2 Me HCH.sub.2 OMe OPhMe-2 SO.sub.2 Me HCH.sub.2 OMe OPhCl-4 SO.sub.2 Me HCH.sub.2 OMe OPhNO.sub.2 -4 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CHMeOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe OCHMePh SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub. 2 Ph SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y9 SO.sub.2 Me HCH.sub.2 OMe Y10 SO.sub.2 Me HCH.sub.2 OMe Y11 SO.sub.2 Me HCH.sub.2 OMe Y12 SO.sub.2 Me HCH.sub.2 OMe Y13 SO.sub.2 Me HCH.sub.2 OMe Y14 SO.sub.2 Me HCH.sub.2 OMe Y15 SO.sub.2 Me HCH.sub.2 OMe Y16 SO.sub.2 Me HCH.sub.2 OMe Y17 SO.sub.2 Me HCH.sub.2 OMe Y18 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me HCH.sub.2 OMe Y19 SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOBu-t SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 COOY4 SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOMe SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me HCH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me HCH.sub.2 OMe OCOOMe SO.sub.2 Me HCH.sub.2 OMe OCOOPr-i SO.sub.2 Me HCH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me HCH.sub.2 OMe OCONHME SO.sub.2 Me HCH.sub.2 OMe OCONMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me HCH.sub.2 OMe Y20 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me HCH.sub.2 OMe Y21 SO.sub.2 Me HCH.sub.2 OMe SPh SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe Y22 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 C CH SO.sub.2 Me HCH.sub.2 OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y23 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me HCH.sub.2 OMe Y24 SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i Cl HCH.sub.2 OMe OCHMeCH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 COOMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl HCH.sub. 2 OMe SCH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl HCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 PhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 PhCH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPhCH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPhCH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPhCH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh______________________________________
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 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 the 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, tridiphane, isoproturon, chlortoluron, triallate, difluphenican, diclofop methyl, diphenzoquat, imazamethabenz methyl, ioxynil, methabenzthazuron, fluroxypil, chlorsulfuron and N-[(4,6-di(difluoromethoxy)pyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulfonamide. 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-5sulfonamide as disclosed in U.S. Pat. No. 4,668,277, or N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-3-dimethylaminocarbonylpyridine-2-sulfonamide as disclosed in Japanese Unexamined Patent Publication No. 223180/1987 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 inveniton 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. 1 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 of asurfactant 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
Emulsifiable concentrate
______________________________________Compound No. 1 of the present invention 1.5 partsXylene 78.5 partsN,N-dimethylformamide 15 partsSorpol 2680 (tradename for a mixture of a 5 partsnonionic surfactant and an anionicsurfactant, manufactured by Toho ChemicalCo., Ltd.)______________________________________
The above ingredients are homogeneously mixed to form an emulsifiable concentrate.
FORMULATION EXAMPLE 3
Flowable
______________________________________Compound No. 1 of the present invention 40 partsAgrizole B-710 (tradename for a nonionic 10 partssurfactant, manufactured by KaoCorporation)Runox 1000C (tradename for an anionic 0.5 partsurfactant, manufactured by Toho ChemicalCo., Ltd.)1% Rodopol water (tradename for a thickner, 20 partsmanufactured by Rhone-Poulenc)Water 29.5 parts______________________________________
The above ingredients are homogeneously mixed to form a flowable.
FORMULATION EXAMPLE 4
Liquid formulation
______________________________________Sodium salt of Compound No 1 of the 30 partspresent inventionNippol (tradename for a nonionic 10 partssurfactant, manufactured by NissanChemical Industries Ltd.)Water 60 parts______________________________________
The above ingredients are homogeneously mixed to obtain a liquid formulation.
FORMULATION EXAMPLE 5
Liquid formulation
______________________________________Potassium salt of Compound No. 1 of the 30 partspresent inventionNippol (tradename for a nonionic 10 partssurfactant, manufactured by NissanChemical Industries Ltd.)Water 60 parts______________________________________
The above ingredients are homogeneously mixed to obtain a liquid formulation.
FORMULATION EXAMPLE 6
Liquid formulation
______________________________________Calcium salt of Compound No. 1 of the 30 partspresent inventionNippol (tradename for a nonionic 10 partssurfactant, manufactured by NissanChemical Industries Ltd.)Water 60 parts______________________________________
The above ingredients are homogeneously mixed to obtain a liquid formulation.
FORMULATION EXAMPLE 7
Liquid formulation
______________________________________Isopropylamine salt of Compound No. 1 of the 10 partspresent inventionSorpol W-150 (tradename for a nonionic 10 partssurfactant, manufactured by Toho ChemicalCo., Ltd.)Water 80 parts______________________________________
The above ingredients are homogeneously mixed to form a liquid formulation.
In their use, the above wettable powder, 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 also 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 of 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 was 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 9. The Compound Nos. correspond to the Compound Nos. in Table 2.
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: ##EQU1## where T: Weight of the weed growth above the soil surface of the treated area
N: Weight of the weed growth above the soil surface of the non-treated area
TEST EXAMPLE 2:
Test 1 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 strumatirum, 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 crop plant grew to the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed on the foliages so that the active ingredient was 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 and Zea mays were determined on the basis of the standard ratings described in Test Example 1. The results are shown in Table 10. The Compound Nos. in Table 10 correspond to the Compound Nos. in Table 2.
TEST EXAMPLE 3
Test 2 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 Veronica persica, Stellaria media, Galium spurium, Matricaria matricarioides, Polygonum persicaria, Lamium purpureum, Solanum nigrum and Triticum aestivum were spot-wisely sown. Then, the soil was covered thereon in a thickness of about 1.5 cm. When the various weeds and crop plant grew to the 2 or 3 leaf atage, a herbicidal solution was uniformly sprayed on the foliages so that the active ingredient was 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 Triticum aestivum by a small spray. Two weeks after the application of the herbicide solution, the herbicidal effects against each weed and Triticum aestivum were determined on the basis of the standard ratings described in Test Example 1 The results are shown in Table 11. The Compound Nos in Table 11 correspond to Compound Nos. in Table 2.
In Tables 9, 10 and 11, 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)
VE: Veronica persia (birdseye speedweell)
ST: Stellaria media (chickweed)
GA: Galium spurium (catchweed)
MA: Matricaria matricarioides (pineappleweed)
PP: Polygonum persicaria (ladysthumb)
LA: Lamium purpureum (red deadnettle)
SO: Solanum nigrum (black nigthshade)
TR: Triticum aestivum (wheat)
TABLE 9__________________________________________________________________________Compound DoseNo. g/are EC SE EL DI PA AB AM PO CY ZE__________________________________________________________________________ 1 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 0 4 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 0 6 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 0 7 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 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 4 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 4 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 4 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 4 5 5 5 5 5 5 5 5 5 0Compara- 4 3 1 3 3 1 4 5 5 0 0tive 8 4 2 4 4 2 5 5 5 0 0Compound 16 5 3 5 5 3 5 5 5 1 1Compara- 4 5 5 5 5 5 1 1 1 2 0tive 8 5 5 5 5 5 2 2 2 3 0Compound 16 5 5 5 5 5 3 3 3 4 1B__________________________________________________________________________
TABLE 10__________________________________________________________________________Compound DoseNo. g/are EC SE EL DI PA AB AM PO XA CY ZE__________________________________________________________________________ 1 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 5 0 4 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 5 0 6 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 5 0 7 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 4 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 4 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 4 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 4 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 4 5 5 5 5 5 5 5 5 5 5 0Compara- 4 3 1 2 3 0 3 5 5 4 0 0tive 8 4 2 3 4 1 5 5 5 5 0 1Compound 16 4 2 3 4 1 5 5 5 5 0 1Compara- 4 4 3 3 4 3 0 2 2 0 1 0tive 8 4 4 4 4 4 1 3 3 1 2 1Compound 16 5 5 5 5 5 2 4 4 2 3 2B__________________________________________________________________________
TABLE 11______________________________________Com-pound DoseNo. g/are VE ST GA MA PP LA SO TR______________________________________ 1 0.5 5 5 5 5 5 5 5 0 1 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 0 7 0.5 5 5 5 5 5 5 5 0 1 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 011 0.5 5 5 5 5 5 5 5 0 1 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 018 0.5 5 5 5 5 5 5 5 0 1 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 0Compar- 1 4 4 3 2 4 2 4 0ative 2 5 5 4 4 5 4 5 1Com-pound C______________________________________
In Tables 9 and 10, the Comparative Compounds are as follows: ##STR40##
In Table 11, the Comparative Compound is as follows:

Number	Date	Country	Kind
63-176758	Jul 1988	JPX
1-26030	Feb 1989	JPX

Number	Name	Date
4083925	Konotsune et al.	Dec 1977
4230481	Nishiyama et al.	Oct 1980
4261729	Konotsune et al.	Apr 1981
4643757	Baba et al.	May 1985
4744815	Baba et al.	May 1988

Number	Date	Country
0203428	Dec 1986	EPX
0282944	Sep 1988	EPX
2277826	Feb 1976	FRX
2513750	Oct 1975	DEX
2122188	Jan 1984	GBX

Pyrazole derivatives and herbicides containing them

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