Title:
IMPROVED PROCESS FOR NUCLEOSIDES
Document Type and Number:
WIPO Patent Application WO/2011/083484
Kind Code:
A3
Abstract:
The present invention relates to improved process for the preparation of lamivudine or emtricitabine. Thus, (1'R,2'S,5'R)-menthyl- 5(R,S)-acetoxy-[1,3]-oxathiolane-2(R)-carboxylate is reacted with N-propinoyl cytosine in hexamethyl disilazane and then added trityl perchlorate to obtain a solid containing (1'R,2'S,5'R)-menthyl-5S-(N-4''-propionylcytosin-1''-yl)-[1,3]-oxathiolane -2R-carboxylate. The solid obtained above is reacted with methane sulfonic acid to obtain (2R,5S)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)- [1,3]-oxathiolane-2-carboxylic acid, 2S-isopropyl-5R-methyl-1R-cyclohexyl ester. The above compound is reduced with sodium borohydride to obtain lamivudine.
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Inventors:
PARTHASARADHI REDDY BANDI (IN)
RATHNAKAR REDDY KURA (IN)
MURALIDHARA REDDY DASARI (IN)
RAJI REDDY RAPOLU (IN)
VAMSI KRISHNA BANDI (IN)
RATHNAKAR REDDY KURA (IN)
MURALIDHARA REDDY DASARI (IN)
RAJI REDDY RAPOLU (IN)
VAMSI KRISHNA BANDI (IN)
Application Number:
PCT/IN2010/000014
Publication Date:
December 27, 2012
Filing Date:
January 08, 2010
Export Citation:
Assignee:
HETERO RESEARCH FOUNDATION (IN)
PARTHASARADHI REDDY BANDI (IN)
RATHNAKAR REDDY KURA (IN)
MURALIDHARA REDDY DASARI (IN)
RAJI REDDY RAPOLU (IN)
VAMSI KRISHNA BANDI (IN)
PARTHASARADHI REDDY BANDI (IN)
RATHNAKAR REDDY KURA (IN)
MURALIDHARA REDDY DASARI (IN)
RAJI REDDY RAPOLU (IN)
VAMSI KRISHNA BANDI (IN)
International Classes:
C07D411/04; C07H19/06
Domestic Patent References:
| WO2009069011A1 | 2009-06-04 |
Foreign References:
| EP0515156A1 | 1992-11-25 |
Other References:
See also references of EP 2521729A4
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