Hong-Yan Shen, G. Tian, Wenjiang Zhu
Aug 26, 2010
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Journal
Chinese Journal of Chemistry
Abstract
3-(Diethoxyphosphoryloxy)-1, 2, 3-benzotriazin-4(3H)-one (DEPBT) was an organophosphorus coupling reagent developed by our group. It was an effective coupling reagent for the synthesis of protected peptides containing Tyr, Ser and Thr with unprotected hydroxy group on their side chain. The further study of the synthesis of a series of protected dipeptides containing histidine with unprotected imidazole group using DEPBT is reported. During the synthetic procedure, the imidazole group of histidine did not need to be protected. When the carboxyl components were N-protected aromatic amino acids or basic amino adds, the yields were relatively high (63%—81%). However, when the carboxyl components were N-protected acidic amino adds, the yields were relatively low (47%—48%). The results expanded the application of DEPBT on the synthesis of bioactive peptides containing histidine.