Bioorganic & medicinal chemistry

Progress in arylpiperazine synthesis by the catalytic amination reaction

Y Torisawa, T Nishi, J Minamikawa

Index: Torisawa, Yasuhiro; Nishi, Takao; Minamikawa, Jun-Ichi Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 12 p. 4023 - 4027

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Citation Number: 11

Abstract

Careful base and solvent optimization for catalytic amination is described. A Pd-catalyzed amination between some arylbromide and unprotected piperazine (1equiv) was efficiently carried out with Pd/BINAP catalyst in a toluene–DBU solvent system, which is useful for the one-pot preparation of unsymmetrical piperazine through amination and in-situ N-protection. Reaction with N-BOC-piperazine was also successful in toluene–DBU or more polar NMP ...