Process for production of optically active amine derivatives

Details Process for production of optically active amine derivatives Process for production of optically active amine derivatives

C - Chemistry, Metallurgy

07

D

C07D 307/77 (2006.01) A61K 31/343 (2006.01) A61P 25/20 (2006.01)

Patent

CA 2579121

An industrial process for producing high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2- (1, 6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8- ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100~C and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro -2H-indeno [5,4-b]furan-8- yl)ethylamine to propionylation, and then crystallizing the reaction mixture.

La présente invention concerne un procédé industriel de fabrication de dérivés d~amines optiquement actifs de haute pureté à haut rendement tout en inhibant la formation de sous-produits, lequel procédé consiste à soumettre la (E)-2-(1,6,7,8-tétrahydro-2H-indéno[5,4-b]furan-8-ylidène)éthylamine à une réduction asymétrique, à réduire de manière catalytique le produit obtenu à une température de réaction de 40 à 100 °C et à un pH de 3 à 9, à soumettre la (S)-2-(1,6,7,8-tétrahydro-2H-indéno[5,4-b]furan-8-yl)éthylamine obtenue à une propionylation et ensuite à cristalliser le mélange réactionnel.

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