Abstract
1<i>H</i>-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 <i>N</i> <sup>1</sup>-substituted 1<i>H</i>-indazoles in high to excellent yields with exclusive <i>N</i> <sup>1</sup>-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 <i>N</i> <sup>1</sup>-substituted 1<i>H</i>-indazoles.
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