N,O-Bis(trimethylsilyl)acetamide/N-hydroxysuccinimide ester(BSA/NHS) as coupling agents for dipeptide synthesis  

作　　者：Ye Huang Wen-Hua Feng 

机构地区：[1]Department of New Drug Research and Development,Institute of Materia Medica & Peking Union Medical College,Chinese Academy of Medical Sciences

出　　处：《Chinese Chemical Letters》2016年第3期357-360,共4页中国化学快报（英文版）

基　　金：financially supported by the National Science and Technology Major Project of China(No.521042)

摘　　要：A method using N,O-bis（trimethylsilyl）acetamide/N-hydroxysuccinimide ester（BSA/NHS） as coupling agents for dipeptide synthesis is descried. The coupling reaction between N-hydroxysuccinimide（NHS）esters and amines could be performed under mild conditions with N,O-bis（trimethylsilyl）acetamide（BSA） as coupling reagent and no additional acid/base is required. All byproducts and excessive reactants are water soluble or hydrolysable and easy to eliminate through water-washing at the purification stage.Moreover, all the reactants are inexpensive and widely used in conventional drug production.A method using N,O-bis（trimethylsilyl）acetamide/N-hydroxysuccinimide ester（BSA/NHS） as coupling agents for dipeptide synthesis is descried. The coupling reaction between N-hydroxysuccinimide（NHS）esters and amines could be performed under mild conditions with N,O-bis（trimethylsilyl）acetamide（BSA） as coupling reagent and no additional acid/base is required. All byproducts and excessive reactants are water soluble or hydrolysable and easy to eliminate through water-washing at the purification stage.Moreover, all the reactants are inexpensive and widely used in conventional drug production.

关 键 词：Dipeptide synthesis Solution-phase N O-Bis（trimethylsilyl）acetamide N-Hydroxysuccinimide ester Water washing 

分 类 号：O629.72[理学—有机化学]