Pd-catalyzed cascade coupling reaction of cyclopropanols with N-allenyl-2-iodoanilines to construct 3-substituted indole derivatives

Abstract

We report herein a concise and useful method for the construction of 3-substituted indole derivatives via a palladium-catalyzed ring-opening coupling reaction of cyclopropanols with N-allenyl-2-iodoanilines. Various indoles bearing different functional groups have been synthesized in moderate to good yields. Furthermore, a gram-scale experiment and diverse transformation of the products showed a great potential utility of this method.