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专利权人:
LES LABORATOIRES SERVIER
发明人:
MARIA ISABEL GARCIA ARANDA,JOSÉ LORENZO GONZALEZ,FRÉDÉRIC SANCHEZ,MARÍA DEL PILAR CARRANZA
申请号:
MX2013012858
公开号:
MX2013012858A
申请日:
2013.11.04
申请国别(地区):
MX
年份:
2014
代理人:
摘要:
Process (P1) for synthesizing (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile (I), comprises subjecting 4-bromo-1,2-dimethoxybenzene (II) to a coupling reaction with acrylonitrile in the presence of a palladium catalyst, a ligand, a base and a phase transfer agent in an organic solvent to yield (I). Process (P1) for synthesizing (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile of formula (I), comprises subjecting 4-bromo-1,2-dimethoxybenzene of formula (II) to a coupling reaction with acrylonitrile in the presence of a palladium catalyst, a ligand, a base and a phase transfer agent in an organic solvent to yield (I). An independent claim is also included for a process (P2) for synthesizing ivabradine, or its salts and hydrates, comprising: converting (II) into (I) according to the process (P1); subsequently converting (I) into 3-(3,4-dimethoxyphenyl)propanenitrile (III) by a reduction reaction; converting (III) into 3-(2-bromo-4,5-dimethoxyphenyl)propanenitrile (IV) by a bromination reaction; and subsequently converting (IV) into ivabradine, which may be converted into its addition salts with an acid (comprising hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, acetic acid, trifluoroacetic acid, lactic acid, pyruvic acid, malonic acid, succinic acid, glutaric acid, fumaric acid, tartaric acid, maleic acid, citric acid, ascorbic acid, oxalic acid, methanesulfonic acid, benzenesulfonic acid or camphoric acid), and into its hydrates. [Image].Procedimiento de síntesis del compuesto de fórmula (1): (ver Fórmula) Aplicación en la síntesis de la ivabradina, de sus sales de adición a un ácido farmacéuticamente aceptable y de sus hidratos.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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