Process for manufacturing Simvastatin and novel intermediates thereof

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United States of America Patent

PATENT NO 6603022
SERIAL NO

10348714

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Abstract

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The present invention provides a novel process for the synthesis of Simvastatin of formula II. ##STR1## The process comprises converting Lovastatin to the corresponding amide intermediate using a secondary amine. The C-8 2-methylbutyrate side chain of the amide intermediate is subsequently methylated by reaction with a suitable base, followed by treatment with a methylating agent. The 2,2-dimethylbutyrate intermediate is further transformed to the final product, Simvastatin, by hydrolysis, followed by lactonization. In another aspect, the present invention provides intermediates of formula IIb and IIc useful for the preparation of Simvastatin: ##STR2## wherein R.sub.1 and R.sub.2 are as defined herein.

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Patent Owner(s)

Patent OwnerAddress
BIOCON INDIA LIMITEDHEBBAGODI BANGALORE 561 229

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Acharya, Poornaprajna Karnataka, IN 5 12
Mathew, Joy Karnataka, IN 11 49
Sambasivam, Ganesh Bangalore, IN 13 31
Sridharan, Madhavan Karnataka, IN 14 53

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