A simple and versatile method to synthesize N-acyl-benzotriazoles

An efficient method for the synthesis of N-acyl-benzotriazoles from a wide variety of protected amino acids, as well as from compounds frequently used in drug discovery such as biotin and N-Fmoc polyethylene glycol, has been developed. The reaction of carboxylic acid derivatives with benzotriazole in the presence of T3P (R) yielded the corresponding N-acyl-benzotriazoles, which were obtained in high purity following a simple work-up procedure, in most cases via precipitation of the desired product in water. (C) 2018 Elsevier Ltd. All rights reserved.