Dehydrocholyl benzotriazole was synthesized from dehydrocholic acid and benzotriazole with the method of dicyclohexylcarbodiimide coupling reaction and the yield was about 60%,and its structure was characterized by FT-IR and 1H NMR.Dehydrocholyl benzotriazole showed a high reaction activity in the chemical modification of insulin and it confirmed that the synthesis of dehydrocholyl benzotriazole was successful.