Title:
NEW METHOD FOR SYNTHESIZING 7,8-DIMETHOXY-1,3-DIHYDRO-2H-3-BENZOAZEPIN-2-ONE, AND APPLICATION OF THE METHOD FOR SYNTHESIZING IVABRADINE AND ITS ADDITION SALT WITH PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
Document Type and Number:
Japanese Patent JP2010006807
Kind Code:
A
Abstract:
To provide an improved method for synthesizing ivabradine by using specific operational conditions.
The method comprises the following process: 3,4-dimethoxyphenylacetic acid is converted to a compound of formula (V) (wherein groups R1 and R2 are each a straight-chain or branched-chain 1-6C alkoxy group, or forms a ring by being bound to each other together with carbon atoms born thereon), which is then put to cyclization reaction in an acidic medium to obtain a compound of formula (I), which is then put to N-alkylation followed by reductive amination to effect conversion to the objective ivabradine.
Inventors:
LERESTIF JEAN-MICHEL
LECOUVE JEAN-PIERRE
BRIGOT DANIEL
LECOUVE JEAN-PIERRE
BRIGOT DANIEL
Application Number:
JP2009145931A
Publication Date:
January 14, 2010
Filing Date:
June 19, 2009
Export Citation:
Assignee:
SERVIER LAB
International Classes:
C07D223/16; A61K31/55; A61P9/06; A61P9/10
Domestic Patent References:
| JP2005298480A | 2005-10-27 | |||
| JPH05213890A | 1993-08-24 | |||
| JPS59152374A | 1984-08-31 | |||
| JP2004521084A | 2004-07-15 | |||
| JP2005298480A | 2005-10-27 |
Foreign References:
| WO2002074746A1 | 2002-09-26 |
Other References:
JPN6012019538; ＲＥＩＦＦＥＮ，Ｍ． ｅｔ ａｌ．: 'Ｓｐｅｃｉｆｉｃ ｂｒａｄｙｃａｒｄｉｃ ａｇｅｎｔｓ． １． Ｃｈｅｍｉｓｔｒｙ， ｐｈａｒｍａｃｏｌｏｇｙ， ａｎｄ ｓｔｒｕｃｔｕｒｅ-ａｃｔｉｖｉｔｙ ｒｅｌａｔｉｏｎｓｈｉｐｓ ｏｆ ｓｕｂ' Ｊ．Ｍｅｄ．Ｃｈｅｍ． Ｖｏｌ．３３， Ｎｏ．５, 1990, ｐ．１４９６-５０４
Attorney, Agent or Firm:
Hajime Tsukuni
Koshiro Tsukuda
Fusayuki Saito
Koshiro Tsukuda
Fusayuki Saito
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