Palladium-catalyzed direct amination of N-(quinolin-8-yl)-1H-indole-3-carboxamides

Abstract

A palladium-catalyzed C–H bond cleavage and amination of indoles with di-tert-butyldiaziridinone has been developed for the construction of 2-amino indole skeletons. By using di-tert-butyldiaziridinone as the nitrogen source, the reaction worked well to produce a variety of 2-amino indole derivatives in moderate to good yields. Additionally, scale-up reaction and derivatization of 2-amino indoles were realized as well.