Synergistic Photoredox and Copper Catalysis for 1,2-Alkylamination of Alkynes.

Herein, we report a novel three-component protocol for the radical 1,2-alkylamination of alkynes enabled by the synergistic combination of photoredox and copper catalysis. By employing redox-active N-hydroxyphthalimide (NHPI) esters as alkyl radical precursors, the first photocatalytic method capable of directly converting readily available commercial alkynes, simple amides, and NHPI esters into alkylated enamides was established. The developed protocol exhibits broad functional group compatibility, enabling the late-stage functionalization of complex molecular architectures.