Nickel-Catalyzed Intramolecular Defluorinative [4+2] Cycloaddition for the Construction of Monofluoroarenes with gemdifluoroalkenes

Abstract

A nickel-catalyzed defluorinative [4+2] cycloaddition has been developed for the direct synthesis of monofluoroarenes. This method employs gem-difluoroalkenes as effective surrogates for scarce 1-fluoroalkyne precursors, thereby circumventing conventional late-stage aromatic fluorination. The reaction enables simultaneous arene ring formation and fluorine incorporation, displays broad functional group tolerance, and provides a modular strategy to access aryl fluorides of interest in pharmaceutical and materials science.