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-aryl-3-aminoalkyl-2,6 -dioxohexahydropyridine.
Pharmaceutical composition and medical uses of dioxopiperidine derivatives, especially as immune response potentiators, antiviral and antibacterial agents
申请人:BRITISH TECHNOLOGY GROUP LIMITED
公开号:EP0452765A2
公开(公告)日:1991-10-23
Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I
wherein:
R₁ represents methoxy, ethoxy or hydroxy,
R₂ represents methoxy, ethoxy, hydroxy or hydrogen;
each R₃ independently represents methyl or ethyl;
R₄ represents hydrogen or methyl;
R₅ represents hydrogen or methyl; and
n represents 2 or 3,
and a pharmacologically acceptable acid addition salt thereof potentiate the immunoresponse of a patient and thereby have antibacterial and antiviral activity.