The regioselective carbon-hydrogen bond functionalization reaction in atom- and step-economy holds significant potential for the late-stage elaboration of complex molecules and natural products. In recent years, the hydrogen atom transfer strategy involving radicals has garnered considerable attention from chemists due to its high chemoselectivity and regioselectivity. However, owing to the marginal differences in bond dissociation energies (BDEs) among C(sp³)-H bonds, hydrogen atom transfer reactions mediated by alkyl radicals remain less-developed. We report a copper-catalyzed sulfone-induced regioselective C(sp³)-H bond heteroarylation reaction. This strategy utilizes the α-alkyl radical of sulfone as an intramolecular hydrogen abstraction reagent, enabling the regioselective formation of carbon-nitrogen bonds under copper catalysis.

Key words: radical reaction, hydrogen atom transfer, C-H bond functionalization, heteroarylation