4-(3-carboxy-2-oxopropyl)-azetidino-2-ones and process for their preparation

Claim 2

A compound having the structural formula: wherein R 1 ' is hydrogen or a readily removable protecting group; and wherein R 6 and R 7 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, f luoro , R 1 , -OH, -OR 1 , -NR 1 R 2 , -NH 2 , -NHR 1 , -SO2NR 1 R 2 , -CO 2 H, -CO 2 R 1 , -SH , -CN, and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms ; R and R are not both hydrogen at the same time; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not

Claim 3

A compound according to Claim 1 wherein R 1 , is hydrogen or a triorganosilyl group.

Claim 4

A compound according to Claim 2 wherein R is hydrogen or a trialkylsilyl group wherein each alkyl moiety has from 1-6 carbon atoms.

Claim 5

A compound according to Claims 1, 2 or 3 wherein R 6 and R 7 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl and alkynyl having from 1-10 carbon atoms, cycloalkyl, cycloalkylalkyl and alkylcycloalkyl, having 3-6 carbonatoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic protion has 1-6 carbon atoms; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -OR 1 , -NR 1 R 2 , -NH 2 , -NHR 1 , -SO 2 NR 1 R 2 . -CO 2 H, -CO 2 R 1 , -SH , -CN, and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R and R 2 are independently selected from: hydrogen, alkyl, alkenyl and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties, phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms.

Claim 6

A compound according to Claims 1, 2, 3 or 4 wherein R 7 is hydrogen or methyl.

Claim 7

A compound according to Claim 5 wherein R is selected from the group consisting of: substituted and unsubstituted: alkyl, alkenyl and cycloalkylalkyl wherein the substituent or substituents are selected from hydroxyl, alkoxyl having from 1-6 carbon atoms, phenoxy, amino, and carboxy.

Claim 8

A compound according to Claims 5 or 6 wherein R 6 is selected from the group consisting of alkyl, cycloalkylalkyl, alkyl substituted by one or more hydroxyl groups, or cycloalkylalkyl substituted by one or more hydroxyl groups.

Claim 9

A compound according to Claims 5, 6 or 7 wherein R 7 is hydrogen.

Claim 10

A process for preparing a compound according to Claims 1, 2, 3, 4, 5, 6, 7 or 8 comprising treating: in the presence of a base with an alkylating or acylating agent calculated to establish R and R .

Claim 11

1Q A compound having the structural formula: wherein R b and R 7 are independently selected from the group consisting of hydrogen, substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -OR 1 , -NR 1 R 2 , -NH 2 , -NHR 1 , -SO 2 NR 1 R 2 , -CO 2 H, -CO 2 R 1 , -SH , -CN and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms; R 6 and R are not both hydrogen at the same time; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not

Claim 12

1Q A compound having the structural formula: wherein R b and R 7 are independently selected from the group consisting of hydrogen, substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -OR 1 , -NR 1 R 2 , -NH 2 , -NHR 1 , -SO 2 NR 1 R 2 , -CO 2 H, -CO 2 R 1 , -SH , -CN and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms; R 6 and R are not both hydrogen at the same time; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not

Claim 13

11 . A compound according to Claim 10 wherein R 1 ' is hydrogen or a triorganosilyl group.

Claim 14

A compound according to Claim 11 wherein R is hydrogen or a trialkylsilyl group wherein each alkyl moiety has from 1-6 carbon atoms.

Claim 15

A compound according to Claims 10, 11 or 12 wherein R 6 and R 7 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl and alkynyl having from 1-10 carbon atoms, cycloalkyl, cycloalkylalkyl and alkylcycloalkyl, having 3-6 carbonatoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic protion has 1-6 carbon atoms; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -OR 1 , -NR 1 R 2 , -NH 2 . -NHR 1 , -SO 2 NR 1 R 2 , -CO 2 H, -CO 2 R 1 , -SH , -CN and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms.

Claim 16

A compound according to Claims 10, 11, 12 or 13 wherein R 7 is hydrogen or methyl.

Claim 17

A compound according to Claim 14 wherein R 6 is selected from the group consisting of: substituted and unsubstituted: alkyl, alkenyl and cycloalkylalkyl wherein the substituent or substituents are selected from hydroxyl, alkoxyl having from 1-6 carbon atoms, phenoxy, amino and carboxy.

Claim 18

A compound according to Claims 14 or 15 wherein R 6 is selected from the group consisting of alkyl, cycloalkylalkyl, alkyl substituted by one or more hydroxyl groups, or cycloalkylalkyl substituted by one or more hydroxyl groups.

Claim 19

A compound according to Claims 14, 15 or 16 wherein R 7 is hydrogen.

Claim 20

A process for preparing a compound according to Claims 10, 11, 12, 13, 14, 15, 16 or 17 comprising oxidizing: to form:

Claim 21

1 9 . A compound selected from the group consisting of: wherein R 1 and R 2 ' are hydrogen or a readily removable protecting group; and wherein R 6 and R 7 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -NR 1 R 2 -OR 1 , -NH. -NHR 1 -SO 2 NR 1 R 2 , -CO 2 H, -CO 2 R 1 -SH , -CN and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms; R 6 and R 7 are not both hydrogen at the same time; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not

Claim 22

1 9 . A compound selected from the group consisting of: wherein R 1 and R 2 ' are hydrogen or a readily removable protecting group; and wherein R 6 and R 7 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -NR 1 R 2 -OR 1 , -NH. -NHR 1 -SO 2 NR 1 R 2 , -CO 2 H, -CO 2 R 1 -SH , -CN and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms; R 6 and R 7 are not both hydrogen at the same time; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not

Claim 23

A compound according to Claim 19 wherein R 1 is hydrogen or a triorganosilyl group.

Claim 24

A compound according to Claim 20 wherein R 1 ' is hydrogen or a trialkylsilyl group wherein each alkyl moiety has from 1-6 carbon atoms.

Claim 25

A compound according to Claims 17, 18, or 19 wherein R 6 and R are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl and alkynyl having from 1-10 carbon atoms, cycloalkyl, cycloalkylalkyl and alkylcycloalkyl, having 3-6 carbonatoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic protion has 1-6 carbon atoms; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -OR 1 , -NR 1 R 2 , -NH 2 , -NHR 1 , -SO 2 NR 1 R 2 , -CO 2 H, -CO 2 R 1 , -SH , -CN and -N 3 wherein, relative to the above listed substituents on R 6 , R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties, phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms.

Claim 26

A compound according to Claims 19, 20, 21 or 22 wherein R 7 is hydrogen or methyl.

Claim 27

A compound according to Claim 21 wherein R 6 is selected from the group consisting of: substituted and unsubstituted: alkyl, alkenyl and cycloalkylalkyl wherein the substituent or substituents are selected from hydroxyl, alkoxyl having from 1-6 carbon atoms, phenoxy, amino, and carboxy.

Claim 28

A compound according to Claims 23 or 24 wherein R 6 is selected from the group consisting of alkyl, cycloalkylalkyl, alkyl substituted by one or more hydroxyl groups, or cycloalkylalkyl substituted by one or more hydroxyl groups.

Claim 29

A compound according to Claims 23, 24 or 25 wherein R 7 is hydrogen.

Claim 30

A process for preparing a compound according to Claims 19, 20, 21, 22, 23, 24, 25 or 26 comprising treating: with 1,1'-carbonylimidazole followed by reacting with (R 2 'O 2 CCH 2 CO 2 ) 2 Mg to yield:

Claim 31

A process for preparing a compound according to Claims 19, 20, 21, 22, 23, 24, 25 or 26 comprising diazotizing: to form:

Claim 32

A process for preparing a compound having the structure: comprising cyclizing: wherein R 2 ' is a readily removable protecting group or a pharmaceutically acceptable ester moiety; and wherein R 6 and R 7 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -NR 1 R 2 , -OR 1 , -NH 2 , -NHR 1 . -SO 2 NR 1 R 2 , -CO 2 H, -CO 2 R 1 -SH , -CN, and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms; R 6 and R 7 are not both hydrogen at the same time; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not

Claim 33

A process for preparing a compound having the structure: comprising cyclizing: wherein R 2 ' is a readily removable protecting group or a pharmaceutically acceptable ester moiety; and wherein R 6 and R 7 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -NR 1 R 2 , -OR 1 , -NH 2 , -NHR 1 . -SO 2 NR 1 R 2 , -CO 2 H, -CO 2 R 1 -SH , -CN, and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms; R 6 and R 7 are not both hydrogen at the same time; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not

Claim 34

A process for preparing: and the pharmaceutically acceptable salt, ester and amide derivatives thereof comprising cyclizing: to form: followed by activating and reacting with HSR 8 , wherein R 2 ' is hydrogen, a readily removable protecting group or a pharmaceutically acceptable ester moiety; and wherein R 6 , R 7 and R 8 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -OR 1 . -NR 1 R 2 , -NH 2 , -NHR 1 , -SO 2 NR 1 R 2 , -CO 2 H -CO 2 R 1 , -SH , -CN, and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not when SR is SCH 2 CH 2 NH 2 .

Claim 35

A process for preparing: and the pharmaceutically acceptable salt, ester and amide derivatives thereof comprising cyclizing: to form: followed by activating and reacting with HSR 8 , wherein R 2 ' is hydrogen, a readily removable protecting group or a pharmaceutically acceptable ester moiety; and wherein R 6 , R 7 and R 8 are independently selected from the group consisting of: hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; wherein the substituent or substituents relative to the above-named radicals are selected from the group consisting of: chloro, bromo, fluoro, -OH, -OR 1 . -NR 1 R 2 , -NH 2 , -NHR 1 , -SO 2 NR 1 R 2 , -CO 2 H -CO 2 R 1 , -SH , -CN, and -N 3 wherein, relative to the above listed substituents on R 6 , and R 7 , the groups R 1 and R 2 are independently selected from: hydrogen, alkyl, alkenyl, and alkynyl, having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl, having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl; and wherein the hetero atom or atoms in the above-named heterocyclic moieties are selected from the group consisting of 1-4 oxygen, nitrogen or sulphur atoms and wherein the alkyl moieties associated with said heterocyclic moieties have 1-6 carbon atoms; when R 6 /R 7 is hydrogen, then R 7 /R 6 is not when SR is SCH 2 CH 2 NH 2 .

Claim 36

The process of Claim 30 wherein -SR 8 is selected from the group consisting of:

Claim 37

The process of Claim 30 wherein R 7 is hydrogen or methyl and R 6 is selected from the group consisting of CH 3 CH 2 HO CH 2 HO 2 CCH 2

Claim 38

The process of Claim 32 wherein R 7 is hydrogen.

Claim 39

A process according to Claims 32 or 33 wherein -SR 8 is selected from the group consisting of

Claim 40

A process according to Claim 31 wherein R 7 is hydrogen or methyl.

Claim 41

A process according to Claim 35 wherein R 6 is selected from the group consisting of: substituted and unsubstituted: alkyl, alkenyl and cycloalkylalkyl wherein the substituent or substituents are selected from hydroxyl, alkoxyl having from 1-6 carbon atoms, phenoxy, amino, and carboxy.

Claim 42

A process according to Claims 35 or 36 wherein R 6 is selected from the group consisting of alkyl, cycloalkylalkyl, alkyl substituted by one or more hydroxyl groups, or cycloalkylalkyl substituted by one or more hydroxyl groups.

Claim 43

A process according to Claims 35, 36 or 37 wherein R 7 is hydrogen.

Claim 44

A compound selected from the group consisting of: wherein R 1 ' and R 2 ' are independently selected from the group consisting of hydrogen and a readily removable protecting group; R 7 is hydrogen and R 6 is selected from the group consisting of CH 3 CH 2 HO CH 2 HO 2 CCH 2

Claim 45

A compound selected from the group consisting of: wherein R 1 ' and R 2 ' are independently selected from the group consisting of hydrogen and a readily removable protecting group; R 7 is hydrogen and R 6 is selected from the group consisting of CH 3 CH 2 HO CH 2 HO 2 CCH 2