Benzotriazole Coupling Reagents Design, Synthesis And Activity Studies

Benzotriazolomide analogous coupling reagents show good efficiency in peptide coupling reaction, these reagents can reduce the racemization and cyclization reaction in peptide synthesis efficiently. In addition, benzotriazolomide reagents are reported to be non-poisonous, non-corrosive and quite stable to store.In this paper, classification, characteristics and the application of peptide coupling reagents were entirely described. We studied and improved the synthetic process of the benzotrizolomide analogous coupling reagent HCTU, and got a perfect reaction conditions. The yield was greatly improved too. On the basis of previous study result, modifications were made at the potions of Onium-ammonium/uranium of HCTU, totally 9 targets compounds that never reported in literatures were designed and synthesized. Their activities to catalyze peptide bond formation were confirmed through synthesizing a target tripeptide and the test result showed better activities to the traditional reagents such as HOBt / DCC, HAPyU.