PROCESS FOR THE PREPARATION OF 4-OXYTETRAHYDROPYRAN-2-ONES

A process for the preparation of inhibitors of HMG-CoA reductase, such as simvastatin, from 4-silyloxytetrahydropyran-2-ones with triethylamine trihydrofluoride being used as the desilylation reagent is described. The reaction is performed in organic solvents, a mixture thereof or without solvents....

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Bibliographic Details
Main Authors KRASOVEC, DUSAN, ZUPANCIC, SILVO, ZUPET, PAVEL
Format Patent
LanguageEnglish
French
Published 02.10.2003
Edition7
Subjects
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:A process for the preparation of inhibitors of HMG-CoA reductase, such as simvastatin, from 4-silyloxytetrahydropyran-2-ones with triethylamine trihydrofluoride being used as the desilylation reagent is described. The reaction is performed in organic solvents, a mixture thereof or without solvents. It is characteristic of this reaction that no additional impurities are obtained and that it takes place without the use of additional catalysts and with low excesses of the reagent. L'invention porte sur un procédé de préparation d'inhibiteurs de la réductase HMG-CoA telle que la simvastatine, de 4-silyloxytétrahydropyran-2-ones avec triéthylamine trihydrofluorure utilisé comme réactif de désilylation. La réaction s'effectue dans des solvants organiques, dans un mélange de ceux-ci ou sans solvants. Cette réaction se caractérise en ce qu'il n'y a pas d'ajout d'impuretés et qu'elle s'effectue sans utilisation de catalyseurs additionnels et avec quelques excédents de réactif.
Bibliography:Application Number: WO2003SI00009