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An Efficient Synthesis of Buspirone and its Analogues.

✍ Scribed by Jacek Cybulski; Zdzislaw Chilmonczyk; Wieslaw Szelejewski; Krystyna Wojtasiewicz; Jerzy T. Wróbel

Publisher
John Wiley and Sons
Year
1992
Tongue
English
Weight
231 KB
Volume
325
Category
Article
ISSN
0365-6233

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✦ Synopsis

Benzodiazepines at clinically effective doses often produce side effects like drowsiness, ataxia, or sedation'). Thus, some interest has recently been put to non-diazepine anxiolytic compounds. That resulted in the development of such compounds like buspirone (l), gepirone (2), SM-3997 (3)" or ipsopirone with the possibility of selective activation of the 5-HT1,+ receptor?". This is a new class of anxiolytics with so-called amioselective p m perties"). Several syntheses of the compounds were described4*). In general, all syntheses are based on three fragments: N-derivative of piperazine I, substituted imide or anhydride ii, four-carbon aliphatic chain Ui (Scheme

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