Tetrahedron

Novel synthesis of 1, 4, 5-trisubstituted 1, 2, 3-triazoles via a one-pot three-component reaction of boronic acids, azide, and active methylene ketones

J Zhang, G Jin, S Xiao, J Wu, S Cao

Index: Zhang, Jian; Jin, Guanyi; Xiao, Senhan; Wu, Jingjing; Cao, Song Tetrahedron, 2013 , vol. 69, # 10 p. 2352 - 2356

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Citation Number: 15

Abstract

A series of 1-aryl-5-trifluoromethyl (or difluoromethyl)–1, 4, 5-trisubstituted 1, 2, 3-triazoles were synthesized in high yield by a novel one-pot three-component reaction of arylboronic acids, sodium azide, and active methylene ketones, such as ethyl 4, 4-difluoroacetoacetate or ethyl 4, 4, 4-trifluoroacetoacetate in the presence of Cu (OAc) 2 and piperidine using a DMSO/H2O (10/1) mixture as solvent.