Method for the preparation of clopidogrel and its analogues of methyl-tetrahydrothieno[3,2-C]pyridine acetate
US7932391B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Sep 7, 2006 |
| Grant date | Apr 26, 2011 |
| Priority date | — |
| Expiry date | Nov 26, 2027 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/582
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention disclosed a preparation method of Clopidogrel (X=2−Cl) and its analogues of methyl tetrahydrothienopyridine acetate (I) by using halogen phenyl acetonitrile (VIII) as starting material and tetrahydrothienopyridine acetonitrile (IV), tetrahydrothienopyridine acetate (V) as key intermediates, and further using kinetic resolution to prepare the optical active Clopidogrel and compounds of methyl tetrahydrothenopridine acetate of formula (XII). The Clopidogrel of present invention is a novel high effective and safety drug for inhibition of platelet aggregation. This invention applied systematic technique of racemization of unwanted optical active enantiomer, recover recycle and reuse of resolution agent etc., with greater economic advantages and suitable for commercial scale industrial production.Wherein: X represents atoms of hydrogen, fluorine, chlorine, bromine or iodine, M represents an alkali metal ion.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.