Ein verbessertes Verfahren zur Herstellung von Statinen

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
LanguageGerman
Published 07.04.2005
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Abstract 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.
AbstractList 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.
Author THAPER, RAJEST KUMAR
KHANNA, JAG MOHAN
KUMAR, YATENDRA
KUMAR, S.M. DILEEP
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HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Title Ein verbessertes Verfahren zur Herstellung von Statinen
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