Abstract

Abstract 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.

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