Resolution of...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 471/04 (2006.01)

Patent

CA 2430305

The invention provides a process for the optical resolution of a racemic mixture, or an otpionally enriched mixture, of trans-7-(hydromethyl)octa-hydro- 2H-pyrido-1,2a)pyrazine, a key intermediate for preparing pharmacologically active 2,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives useful in the treatment of disorders of the dopamine system. The process of the invention involves use of D-(-) or L-(+)naporxen as a resolving agent.

L'invention concerne un procédé de résolution optique d'un mélange racémique, ou un mélange optiquement enrichi, de trans-7-(hydroxyméthyl)octa-hydro-2H-pyrido-1,2a)pyrazine, un intermédiaire clé dans la préparation de dérivés pharcologiquement actifs d'octahydro-1H-pyrido[1,2-a]pyrazine 2,7-substituée utiles dans le traitement de torubles du système de la dopamine. Le procédé de l'invention implique l'utilisation de naproxène D-(-) ou L-(+) comme agent de résolution.

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