Regioselective Difluoroalkylation of 2‐Pyridones with Fluoroalkyl Bromides Enabled by a Nickel(II) Catalyst

Abstract Regioselective C−H difluoroalkylation of diverse 2‐pyridones with ethyl bromodifluoroacetates and bromodifluoroacetamides is accomplished by using a (dppf)NiCl 2 catalyst under mild conditions. This efficient protocol could deliver a variety of C‐3 difluoroalkylated pyridones with the tolerance of a range of highly susceptible functionalities, such as −Cl, −Br, −I, −COMe, −CN, −NMe 2 and −NO 2 , including heteroarenes like pyridinyl, furanyl, thiophenyl and carbazolyl moieties. A preliminary mechanistic study suggests the radical pathway for the reaction involving fluoroalkyl radical intermediate.