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Paper | Regular issue | Vol 71, No. 8, 2007, pp.1755-1763
Published online, 22nd May, 2007
DOI: 10.3987/COM-07-11058
Synthesis of 2-Aryl-2H-indazoles via Copper(I)-Catalyzed Intramolecular Amination Reaction

Rui Liu, Yong-ming Zhu,* Lie-na Qin, Shun-jun Ji, and Hajime Katayama

*College of Pharmacy, Soochow University, Suzhou 215123, China

Abstract

A versatile method for the preparation of 2-aryl-2H-indazoles was developed by copper(I)-catalyzed intramolecular amination reaction under the conditions of [CuI/Cs2CO3(250mol%)/1,4-dioxane/105 °C] starting from N’-aryl -N’-(o-bromobenzyl)acetylhydrazines. The method was applied to a wide scope of substrates and afforded indazole products in high yields.