- NOVEL POLYMORPHS OF SAQUINAVIR
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The present invention provides novel polymorphs of saquinavir, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides a process for purification of saquinavir. The present invention further provides a novel process for preparation of known saquinavir crystalline form I.
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Page/Page column 3
(2012/02/15)
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- A PROCESS FOR THE PREPARATION OF SAQUINAVIR USING NOVEL INTERMEDIATE
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The present invention provides a commercially viable process for preparing saquinavir and pharmaceutically acceptable acid addition salts thereof using novel intermediate. Thus, for example, N?2?-(2-quinolinylcarbonyl)-L-asparagine is reacted with pivaloyl chloride in methylene chloride in presence of triethyl amine to give pivaloyl N?2?-(2-quinolinylcarbonyl)-L-asparaginate, which is then condensed with [3S,4aS,8aS]-2-(3S-amino-2R-hydroxy-4-phenylbutyl)-N-(1,1-dimethylethyl)decahydro-3-isoquinoline carboxamide to give saquinavir, followed by treatment with methanesulfonic acid to give saquinavir mesylate.
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Page/Page column 4-5
(2008/06/13)
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