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Communication | Regular issue | Vol 36, No. 7, 1993, pp.1463-1469
Published online, 1st January, 1970
DOI: 10.3987/COM-93-6357
Pd(0)-Catalysed Synthesis of Buspirone and Gepirone

David L. Kuo

*Research and Development Department, Lonza Ltd., Walliser Werke, CH-3930 Visp, Switzerland

Abstract

A novel synthetic approach to buspirone and its anologue (gepirone) is described, in which 3 subunits, namely 2-(1-piperazinyl)pyrimidine, a bifunctional allylderivative, and an imide were efficiently assembled via a Pd(0)-catalysed amination-imidation sequence followed by a hydrogenation.