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US 7,087,751 B2Granted
Synthesis of temozolomide and analogs
AssigneeSchering Corporation
InventorsShen-Chun Kuo, Janet L. Mas, Donald Hou
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Abstract
This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.
Claims23
A process for the preparation of a compound of the formula:
- wherein R is an alkyl group having from 1 to 6 carbon atoms, which comprises:
- (a) diazotizing a compound of the formula:
- wherein R is as defined above;
- and Pg″ is a divalent protecting group that is readily removable by hydrolysis or hydrogenolysis;
- or two monovalent protecting groups Pg that are readily removable by hydrolysis or hydrogenolysis;
- or a bulky monovalent protecting group Pg that is readily removable by hydrolysis or hydrogenolysis together with a hydrogen atom;
- and thereafter
- (b) hydrolyzing the resulting compound of the formula:
5 more elements
A process for the preparation of a compound of formula I
- where R is a methyl group I which comprises;
- (a) diazotizing a compound of the formula:
- in solution in acetic acid with an inorganic nitrate in presence of LiCl, wherein;
- Pg″ is a monovalent protecting group together with a hydrogen atom wherein the monovalent protecting group is a 1,1-dimethylethyl group:
- and thereafter
- (b) hydrolyzing the resulting compound of the formula:
3 more elements
Dependencies are inferred from the claim text.