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通過高效的微波輔助氮-硫;土蝓ソ粨Q制備硫酯化修飾的糖肽

瀏覽次數(shù):5555 發(fā)布日期:2015-2-3  來源:本站 僅供參考,謝絕轉(zhuǎn)載,否則責任自負
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.
 
通過高效的微波輔助加熱進行串聯(lián)反應(yīng),先進行氮-硫酰基化的轉(zhuǎn)移后進行硫酯交換,從而制備硫酯化修飾的糖肽。
 
通過固相合成技術(shù)(SPPS)合成一條在碳端含有巰甲基脯氨酸的多肽,并且在微波輻射下用3-巰基丙酸(MPA)水溶液進行硫酯交換。在25個氨基酸長的硫酯化糖肽的合成中,成功的應(yīng)用了該硫酯交換反應(yīng),然后用硫酯的縮合方法合成了一條61個氨基酸長的糖肽。
 
原文出處:
Efficient Microwave-Assisted Tandem N- to S-Acyl Transfer and Thioester Exchange for the Preparation of a Glycosylated Peptide Thioester
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