3-Aroylindoles via Copper-CatalyzedCyclization of <i>N</i>-(2-Iodoaryl)enaminones

Abstract

3-Aroylindoles have been prepared via copper-catalyzed cyclization of N-(2-iodoaryl)enaminones, readily available from 2-iodoanilines and α,β-ynones. The reaction tolerates a variety of useful functionalities including ether, keto, cyano, bromo, and chloro substituents. This indole synthesis can also be carried out from 2-iodoanilines and α,β-ynones through a sequential process that omits the isolation of enaminone intermediates. © Georg Thieme Verlag Stuttgart.