Citation: Ye Huang, Wen-Hua Feng. N,O-Bis(trimethylsilyl)acetamide/N-hydroxysuccinimide ester (BSA/NHS) as coupling agents for dipeptide synthesis[J]. Chinese Chemical Letters, ;2016, 27(03): 357-360. doi: 10.1016/j.cclet.2015.11.012 shu

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

Ye Huang ,
Wen-Hua Feng ^,

1.
Department of New Drug Research and Development, Institute of Materia Medica & Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing 100050, China

Corresponding author: Wen-Hua Feng,
Received Date: 29 September 2015
Available Online: 26 October 2015
Fund Project:

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.
- Dipeptide synthesis,
- Solution-phase,
- N,O-Bis(trimethylsilyl)acetamide,
- N-Hydroxysuccinimide ester,
- Water washing
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