A simple and versatile method to synthesize N-acylbenzotriazoles

Guillaume Laconde (1) , Muriel Amblard (1) , Jean Martinez (1)

1 IBMM - Institut des Biomolécules Max Mousseron [Pôle Chimie Balard]

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_ 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.

Domaines: Autre [cond-mat.other]

Guillaume Laconde, Muriel Amblard, Jean Martinez. A simple and versatile method to synthesize N-acylbenzotriazoles. Tetrahedron Letters, 2019, 60 (4), pp.341-343. ⟨10.1016/j.tetlet.2018.12.046⟩. ⟨hal-03082020⟩