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Title:
NEW METHOD FOR SYNTHESIZING IVABRADINE AND ADDITION SALT THEREOF WITH PHARMACOLOGICALLY ACCEPTABLE ACID
Document Type and Number:
Japanese Patent JP2010241809
Kind Code:
A
Abstract:

To provide a method for synthesizing a racemic or optically active ivabradine and its addition salt with a pharmacologically acceptable acid, and an intermediate for use in synthesizing ivabradine.

There is provided the method for synthesizing a compound (ivabradine) represented by formula (VII) by allowing a compound represented by formula (VIII) to react with an amine compound in the presence of a salt of a transition metal or of a lanthanoid in a solvent to obtain an intermediate and subsequently converting the resulting intermediate into the compound (ivabradine) represented by formula (VII) by virtue of a hydride donor. In formula (VII), R represents a hydrogen atom or a methyl group.


Inventors:
PEGLION JEAN-LOUIS
DESSINGES AIME
SERKIZ BERNARD
Application Number:
JP2010076768A
Publication Date:
October 28, 2010
Filing Date:
March 30, 2010
Export Citation:
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Assignee:
SERVIER LAB
International Classes:
C07D223/16; C07B53/00; C07B57/00; A61K31/55; A61P9/00; A61P9/04; A61P9/10; C07B61/00
Domestic Patent References:
JP2005298480A2005-10-27
JP2005330263A2005-12-02
JPH05213890A1993-08-24
Attorney, Agent or Firm:
Hajime Tsukuni
Fusayuki Saito