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A facile and rapid synthesis of N-benzyl-2-substituted piperazines
Authors:Mouhamad Jida  Mohamad Soueidan  Nicolas Willand  Francine Agbossou-Niedercorn  Lydie Pelinski  Guillaume Laconde  Rebecca Deprez-Poulain  Benoit Deprez
Affiliation:a INSERM U761 Biostructures and Drug Discovery, Lille F-59000, France
b Faculté de Pharmacie, Université Lille Nord de France, Lille F-59000, France
c Institut Pasteur de Lille, IFR 142, Lille F-59021, France
d PRIM, Lille F-59000, France
e UMR CNRS 8181 Unité de Catalyse et de Chimie du Solide, Université Lille, Cité Scientifique Villeneuve d′Ascq F-59655, France
Abstract:A facile and rapid synthetic approach of N-benzyl-2-substituted piperazine building-blocks via an Ugi strategy is described. This strategy is high yielding (80-92% overall yield), step-efficient and fast using microwave heating and tert-butylisocyanide as a convertible isocyanide. This method is useful for the obtention of key intermediates in medicinal chemistry.
Keywords:Multicomponent reaction   UGI   Piperazines   Microwave
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