Process for producing simvastatin

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 309/30 (2006.01) C07F 5/02 (2006.01) C07F 5/04 (2006.01)

Patent

CA 2185961

A process for manufacturing Simvastatin is provided comprising reacting lovastatin with an organic boronic acid to produce a derivative of lovastatin with a hemiboronate group attached to the C-4 carbon of the pyranyl group, methylating the 2-methylbutyryloxy group on the lovastatin derivative to form a 2,2-dimethylbutyryloxy group on the lovastatin derivative and thereafter removing the hemiboranate group to produce simvastatin.

Méthode pour préparer la Simvastatine, consistant à faire réagir la lovastatine avec un acide borique organique pour former un dérivé de la lovastatine, avec un groupe hémiboronate fixé au carbone C-4 du groupe pyranyle, à méthyler le groupe 2-méthylbutyryloxy sur le dérivé de la lovastatine pour former un groupe 2,2-diméthylbutyryloxy sur le dérivé de la lovastatine, puis à éliminer le groupe hémiboranate pour former la simvastatine.

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