Process for preparing certain azapirones

Details Process for preparing certain azapirones Process for preparing certain azapirones

1994-05-05

1996-05-28

Grumbling, Matthew V.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544231, 544295, C07D40312, C07D40314, C07D24104

Patent

active

055213138

ABSTRACT:
An improved process for preparation of certain useful azapirones, e.g. buspirone, gepirone, tandospirone, etc., comprises the reaction of a novel spiroquaternary piperazinium hydroxide with an appropriate imide to form imidate salts which are then converted to the azapirone by heating. This process is suitable for large scale adaptation and has advantages in greater safety and efficiency.

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patent: 4417049 (1983-11-01), Sims
patent: 4423049 (1983-12-01), Temple
patent: 4507303 (1985-03-01), Ishizumi et al.
patent: 4524206 (1985-06-01), New et al.
patent: 4892943 (1990-01-01), Abou-Gharbia
patent: 5227486 (1993-07-01), Merce-Vidal et al.

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