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US 2010/0249409 A2Published application
Process for stereoselective synthesis of lamivudine
AssigneeShanghai Desano Pharmaceutical Holding Co., Ltd.
InventorsJinliang LI, Feng LV
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Abstract
The present invention discloses 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.
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.