Palladium-Catalyzed Three-Component Dearomative Carbofluoroallylation of Polycyclic Indoles with gem -Difluorocyclopropanes and Ketones

Abstract We herein report a robust palladium-catalyzed, three-component dearomative carbofluoroallylation of polycyclic indoles using gem-difluorocyclopropanes and ketones. This method enables the diversity-oriented synthesis (DOS) of complex ketone-indolines featuring a linear 2-fluoroallylic motif. With its broad substrate scope and high functional group tolerance, the protocol is highly effective for the late-stage functionalization of natural product derivatives. Moreover, the cross-coupling adducts can be readily elaborated into a variety of distinct fluoroallylic scaffolds, demonstrating the significant synthetic utility of this approach.