Palladium-catalyzed regioselective hydrofunctionalization of methylenecyclopropanes (MCPs) with azaaryl alcohols as latent C(sp3)-nucleophiles

Abstract

Herein, we report a palladium-catalyzed regioselective hydrofunctionalization of methylenecyclopropanes (MCPs). The reaction uses azaaryl alcohols as methyl azaarene surrogates and proceeds smoothly with a wide variety of mono- and di-substituted MCPs. A range of terminal alkene fragments were introduced to the α-carbon of azaarenes successfully. The reaction is characterized by good yields, high regioselectivity, and broad substrate scope.