Process for the preparation of pyrido[2,1-a]isoquinoline...

Details Process for the preparation of pyrido[2,1-a]isoquinoline... Process for the preparation of pyrido[2,1-a]isoquinoline...

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01)

Patent

CA 2662413

This invention relates to a process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the Formula (I), wherein R1, R2, R3 and R4 are defined in the specification, comprising the optical resolution of an enamine of the Formula (II), wherein R1 is lower alkyl, in the presence of an optical active resolving agent to form an (S)-enamine salt of the Formula (III), wherein RCO2- is the conjugate base of the resolving agent.

Cette invention concerne une méthode de préparation de dérivés de pyrido[2,1-a]isoquinoline de formule (I), dans laquelle R1, R2, R3 et R4 sont tels que définis dans la description. Ces dérivés comprennent la résolution optique d'une énamine de formule (II) dans laquelle R1 est alkyle inférieur, en présence d'un agent de résolution optiquement actif, pour former un sel de (S)-énamine de formule (III) dans laquelle RCO2- est la base conjuguée de l'agent de résolution.

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