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Stereoselective Synthesis of β-Thiolated Aryl Amino Acids
Synthesis ( IF 2.2 ) Pub Date : 2022-07-20 , DOI: 10.1055/s-0041-1738655
Ping Wang , Mengjie Zheng , Hongli Yin , Siyao Wang

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.



中文翻译:

β-硫醇化芳基氨基酸的立体选择性合成

多种 β-硫醇化芳基氨基酸很容易通过 1,4-加成从易于获得的噻唑啉前体以中等至优异的产率合成,该前体可以通过半胱氨酸甲酯盐酸盐通过三个步骤制备。随后,硫醇化产物可以在一个步骤内以高产率脱保护,并直接用于后续的固相肽合成。

更新日期:2022-07-21
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