Jingya Yang, Yun-Hong Bao, Hongyan Zhou
Feb 4, 2016
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Influential Citations
16
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Journal
Synthesis
Abstract
Abstract 1H-Indazoles are important heterocycles as they are a substantial part in many drugs. Here, a DBU-catalyzed aza-Michael reaction of indazole with enones is described. A variety of aromatic and aliphatic enones are well tolerated and afford the corresponding N 1-substituted 1H-indazoles in high to excellent yields with exclusive N 1-regioselectivity. The use of a metal-free catalyst, good substrate tolerance, mild reaction conditions, and high atom economy make this procedure a direct and facile method for the preparation of N 1-substituted 1H-indazoles.