Liang Yue-jie
2009
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Journal
Journal of Yantai University
Abstract
The preparation of methanesulfonyl N-hydroxysuccinate and its use in the synthesis of oligopeptides in liquid phase has been studied.Methanesulfonyl N-hydroxysuccinate is synthesized from methanesulfonyl chloride and N-hydroxysuccimide,and used to prepare activated esters of N-Boc-Tyr-OH,N-Boc-Ala-OH,N-Boc-Tyr-Pro-OH by SN2 substituted reaction.In this study,methanesulfonyl N-hydroxysuccinate is successfully used in the synthesis of endomorphine-2(EM-2) and alanylglutamine.All the reactions can be operated under mild conditions with less side reaction and in high yield.The results show that methanesulfonyl N-hydroxysuccinate can perfectly meet the performance of oligopeptide synthesis in liquid phase.