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Paper | Regular issue | Vol 78, No. 3, 2009, pp.645-655
Published online, 20th October, 2008
DOI: 10.3987/COM-08-11546
Copper(I)-Catalyzed Direct Arylation of 1,4-Disubstituted 1,2,3-Triazoles with Aryl Iodides

Shin-ichi Fukuzawa,* Eiji Shimizu, and Kenichi Ogata

*Faculty of Science and Engineering, Chuo University, , Japan

Abstract

Treatment of 1,4-disubstituted 1,2,3-triazoles with aryl iodides in the presence of a catalytic amount of copper chloride and lithium tert-butoxide (stoichiometric) in DMF at 140 °C leads to arylation at the 5-position. Various combinations of substituted aryl iodides and 1,4-disubstituted 1,2,3-triazoles bearing functional groups were found to be compatible.