| 摘要 |
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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