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US 2010/0063283 A1Published application
Process for stereoselective synthesis of lamivudine
AssigneeShanghai Desano Pharmaceutical Holding Co., Ltd.
InventorsJinliang LI, Feng LV
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Abstract
A process for stereoselective synthesis of lamivudine, comprising (a) glycosylation of compounds of formula (I) and cytosine or protected cytosine, separating the resulting products by crystallization to afford intermediates of formula (II); (b) removing the protecting groups of intermediates of formula (II) to obtain lamivudine.
Claims15
A process for stereoselective synthesis of Lamivudine, comprising the following steps:
- (a) performing a glycosylation reaction between the compound of formula (I) and cytosine or protected cytosine, and separating the reaction product by recrystallization to obtain the intermediate of formula (II);
- and
- (b) deprotecting the intermediate of formula (II) to obtain Lamivudine,
- wherein the reaction scheme is as follows:
- wherein R1 is a hydroxyl protecting group containing a chiral center, L is a leaving group;
- and R2 is a hydrogen or an amino protecting group.
3 more elements
Dependencies are inferred from the claim text.