Tetrahedron: Asymmetry

An efficient synthesis of (R)-(−)-baclofen

P Resende, WP Almeida, F Coelho

Index: Resende, Patricia; Almeida, Wanda P.; Coelho, Fernando Tetrahedron Asymmetry, 1999 , vol. 10, # 11 p. 2113 - 2118

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Citation Number: 41

Abstract

In this report we describe an efficient synthesis of (R)-(−)-baclofen, a selective GABAB agonist used as an antispastic agent. Our strategy is based on an enantioselective deprotonation of a cyclobutanone easily obtained by [2+ 2] cycloaddition of 4-chlorostyrene and dichloroketene.

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