An improved process of lactonization in the preparation of statins

An improved process of lactonization in the preparation of statins (e.g., the HMG-CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises treating the open ring hydroxy acid form of the statins with an excess of acetic acid and in th...

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Main Authors THAPER, RAJEST KUMAR, KUMAR, S.M. DILEEP, KUMAR, YATENDRA, KHANNA, JAG MOHAN
Format Patent
LanguageEnglish
French
German
Published 15.12.2004
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:An improved process of lactonization in the preparation of statins (e.g., the HMG-CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises treating the open ring hydroxy acid form of the statins with an excess of acetic acid and in the absence of a strong acid catalyst under mild heating conditions (e.g., ambient to 55 DEG C), and adding an anti-solvent to the reaction mixture, thereby causing the statins in lactone form to crystalize from the reaction mixture. The acetic acid serves as both a solvent and a catalyst for the lactonization reaction.
Bibliography:Application Number: EP19980123252