Synthesis 2022; 54(20): 4592-4600
DOI: 10.1055/a-1874-4829
paper

Stereoselective Synthesis of β-Thiolated Aryl Amino Acids

Mengjie Zheng
,
Hongli Yin
,
Siyao Wang
,
Ping Wang
We acknowledge the financial support for this work from Shanghai Pilot Program for Basic Research - Shanghai Jiao Tong University (21TQ1400210), the National Natural Science Foundation of China (22107068, 22077080 and 21907064), and Special Projects of the Central Government in Guidance of Local Science and Technology Development (2021Szvup077).


Abstract

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

Supporting Information



Publication History

Received: 15 May 2022

Accepted after revision: 13 June 2022

Accepted Manuscript online:
13 June 2022

Article published online:
20 July 2022

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