Large-scale process for azapirone synthesis

Details Large-scale process for azapirone synthesis Large-scale process for azapirone synthesis

C - Chemistry, Metallurgy

07

D

C07D 401/14 (2006.01) C07D 401/12 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2146593

Abstract An improved, large-scale process for preparation of certain useful azapirones, e.g., buspirone, gepirone, tandospirone, etc., comprises the anhydrous reaction of a spiroquaternary piperazinium salt with an appropriate preferred imide anion to form the azapirone with heating. This process is designed for large scale production and provides advantages in greater safety, efficiency, and environmental impact in addition to yielding a larger, cleaner amount of azapirone product under mild reaction conditions requiring only about a third of the previous reaction time.

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