Process for the preparation of 4- substituted-1,...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/90 (2006.01) C07D 401/02 (2006.01) C07D 401/04 (2006.01) C07D 405/02 (2006.01) C07D 405/04 (2006.01) C07D 413/02 (2006.01) C07D 413/04 (2006.01) C07D 491/113 (2006.01)

Patent

CA 2077919

TITLE OF THE INVENTION NOVEL PROCESS FOR THE PREPARATION OF 4-SUBSTITUTED- 1,4-DIHYDROPYRIDINES ABSTRACT OF THE DISCLOSURE 4-Substituted-1,4-dihydropyridines are prepared by a cycloaddition reaction in which the cyclization is driven to completion, after thermal reaction, by addition of an acid. Felodipine, a vasodilator, is prepared by a cycloaddition reaction of ethyl 3-aminocrotonate with a suitably substituted dichlorobenzylidine under reaction conditions whereby the product crystallizes out of the reaction solution and may be directly isolated by filtration.

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