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US 7,094,912 B2Granted
Process for the preparation of 4-oxytetrahydropyran-2-ones
AssigneeKRKA, Tovarna Zdravil, D. D.
InventorsSilvo Zupancic, Dusan Krasovec, Pavel Zupet
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Abstract
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.
Claims17
A process for the preparation of 4-oxytetrahydropyran-2-ones of the formula I
- Wherein
- R means a C1-12-alkyl group and
- R1 means H,
- comprising the steps of a) providing a compound of the formula (I), wherein R has the above meaning and R1 means a silyl protection group, b) removing the silyl protection group by triethylamine trihydrofluoride in an organic solvent, a mixture of organic solvents or without an organic solvent, and c) isolating the obtained compound.
1 more element
Dependencies are inferred from the claim text.