Stereoselective Synthesis of β-Thiolated Aryl Amino Acids

Abstract

A variety of β-thiolated aryl amino acids were readily synthesized with moderate to excellent yields from a readily-accessible thiazoline precursor via 1,4-addition, which can be prepared from cysteine methyl ester hydrochloride in just three steps. The thiolated products can be subsequently deprotected within one single step with high yield and used directly for subsequent solid-phase peptide synthesis.