Process for the preparation of 3-aryl-3-aminoalkyl-2,...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/88 (2006.01) C07D 401/04 (2006.01) C07D 409/04 (2006.01) C07D 413/04 (2006.01)

Patent

CA 2036968

ABSTRACT Disclosed is a process for the preparation of 3-aryl-3- aminoalkyl-2,6-dioxohexahydropridines and particularly the compound 3-[3-(dimethylamino)propyl]-3-(3-methoxyphenyl)-4 4-dimethyl-2,6-piperidinedione, monohydrochloride, which is useful as an antidepressant. The process of the present invention comprises the condensation of a sterically hindered nitrile with a sterically hindered .alpha., .beta.-unsaturated diester to produce a nitrile diester. These compounds can then undergo acid catalyzed cyclization and decarboalkoxylation in a one step process to provide the desired 3-ary-3-aminoalkyl-2,6-dioxohexahydropyridine.

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