Novel method for synthesis of ivabradine and additive salts...

Details Novel method for synthesis of ivabradine and additive salts... Novel method for synthesis of ivabradine and additive salts...

C - Chemistry, Metallurgy

07

C

C07C 47/47 (2006.01) C07D 223/16 (2006.01)

Patent

CA 2688815

The present invention related to a process for the synthesis of ivabradine of formula (VI) in racemic or optically active form (see formula VI) in which A represents H2C-HC or HC=CH, wherein the formula compound (VII) is subjected, in racemic or optically active for, (see formula VII) to a reductive amination reaction with the compound of formula (VIII) (see formula VIII) in the presence of a reducing agent in a organic solvent or a mixture of organic solvents. Where A is H2C-CH2, the product of the reductive amination of the compound of formula (VII) (S) configuration of the compound of formula (VIII) is ivabradine. The invention also extends to the formula compound (VII).

La présente invention concerne un procédé de synthèse du composé de formule (VI), sous forme racémique ou optiquement active : (voir formule VI) dans laquelle A représente H2C-CH2 ou HC=CH, caractérisé en ce que l'on soumet le composé de formule (VII), sous forme racémique ou optiquement active : (voir formule VII) à une réaction d'amination réductrice par le composé de formule (VIII): (voir formule VIII) en présence d'un agent de réduction, dans un solvant organique ou un mélange de solvants organiques. Dans le cas où A représente H2C-CH2, le produit de l'amination réductrice du composé de formule (VII) de configuration (S) par le composé de formule (VIII) est l'ivabradine. L'invention s'étend également au composé de formule (VII).

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