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Short Paper | Special issue | Vol 88, No. 2, 2014, pp.1511-1517
Published online, 28th August, 2013
DOI: 10.3987/COM-13-S(S)51
■ Synthesis of 1,4-Disubstituted-1,2,3-trizazoles via Click Reaction in Micro Flow Reactor

Ming Lei,* Ruijun Hu, Yanguang Wang, and Hong Zhang

*Department of Chemistry, Zhejiang University , 38 Zheda Road, Hangzhou, 310027, China

Abstract

A Cu (I)-catalyzed three-component click reaction of alkyl bromide, terminal alkyne and sodium azide was developed in micro flow reactor. Sodium ascorbate was added as additive to prevent the oxidative coupling of desired product with terminal alkyne. Under optimized condition, various 1,4-disubstituted-1,2,3-triazoles were obtained in 85-95% yield with exclusive 1,4-regioisomeric selectivity. The present smooth procedure greatly accelerated the reaction due to the excellent mixing and mass transfer in micro flow system.