Process for producing simvastatin

Details Process for producing simvastatin Process for producing simvastatin

C - Chemistry, Metallurgy

07

D

C07D 319/06 (2006.01) C07D 309/30 (2006.01)

Patent

CA 2320163

A convenient, efficient and industrially favorable process for producing simvastatin which is useful as an HMG-coA reductase inhibitor. This process comprises deacylating lovastatin by treating with an inorganic base and a secondary or tertiary alcohol to thereby form diol lactone, and then selectively protecting, acylating, deblocking and lactonizing the diol lactone by using a ketal or acetal protective group to thereby give simvastatin.

L'invention concerne un procédé pratique, efficace et intéressant sur le plan industriel, qui permet de produire de la simvastatine, utile comme inhibiteur de l'HMG-CoA réductase. Selon le procédé, on désacyle la lovastatine en la traitant avec une base organique et un alcool secondaire ou tertiaire, de façon à former une diol-lactone; puis on protège, acyle, débloque et lactonise sélectivement ladite diol-lactone avec un groupe protecteur cétal ou acétal, de façon à obtenir la simvastatine.

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