Process for the production of ezetimibe and intermediates used in this process
US8178665B2 · kind B2 · utility
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Key dates
| Filing date | Dec 18, 2006 |
| Grant date | May 15, 2012 |
| Priority date | — |
| Expiry date | Sep 23, 2028 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F7/1892
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A process for the production of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) where the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, R1, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silyl, e.g., tert-butyl-dimethyl-silyl, tert-butyl-diphenyl-silyl group.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.