Synthesis of Thiol-Containing Amino Acids Through Alkylation of Glycinate Ketimine

Abstract

A general synthetic route for the synthesis of thiol-containing amino acids through alkylation of glycinate ketimine followed by hydrolysis was developed in this work. The common problems associated with the instability of ketimines and thioesters were solved by optimization of both synthetic and purification conditions. A series of thiol-containing amino acids were obtained in good yields. This method could be readily extended to the synthesis of other thiol-containing amino acids, which are important intermediates in pharmaceutical research and medical applications.