高效的微波辅助氮-硫酰基化和硫酯交换制备硫酯化修饰..
通过高效的微波辅助氮-硫酰基化和硫酯交换制备硫酯化修饰的糖肽
Efficient
Microwave-Assisted Tandem N- to S-Acyl Transfer and Thioester Exchange
for the Preparation of a Glycosylated Peptide Thioester
Abstract: A peptide carrying a mercaptomethylatedproline derivative at the C-terminus was prepared by solid-phase peptide synthesis(SPPS) and converted to the thioester of 3-mercaptopropionic acid(MPA) by aqueous MPA under microwave irradiation conditions. This post-SPPS thioesterification reaction was successfully applied to the synthesis of a glycopeptidethioester composed of 25 amino acid (AA) residues, which was then used for the preparation of a 61-AA glycopeptide by the thioester condensation method.
通过高效的微波辅助加热进行串联反应，先进行氮-硫酰基化的转移后进行硫酯交换，从而制备硫酯化修饰的糖肽。
通过固相合成技术（SPPS）合成一条在碳端含有巯甲基脯氨酸的多肽，并且在微波辐射下用3-巯基丙酸（MPA）水溶液进行硫酯交换。在25个氨基酸长的硫酯化糖肽的合成中，成功的应用了该硫酯交换反应，然后用硫酯的缩合方法合成了一条61个氨基酸长的糖肽。
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