Facile Synthesis of β-Phenylethylamine Derivatives Related to Baclofen via Aziridine Ring Opening

Abstract

Nucleophilic ring opening of the protonated salt of 2-(4-chlorophenyl ) aziridine with substituted thiols provides a very simple route to β- phenylethylamine derivatives which are analogues of the GABA_B receptor agonist baclofen and its antagonists phaclofen and saclofen.