Copper-Catalyzed Chemo-, Regio-, and Stereoselective Multicomponent 1,2,3-Trifunctionalization of Internal Alkynes

Herein, we report the first diaryliodonium salts promoted multicomponent 1,2,3-trifunctionalization of alkynes, where both the acetylenic bond and the adjacent nonactivated propargylic C(sp³)-H bond were functionalized synergistically to generate α-arylated enones with high chemo-, regio-, and stereoselectivity. A broad spectrum of diaryliodonium salts and internal alkynes could be utilized in this protocol, and a diverse collection of highly substituted and stereochemically defined linear and cyclic complex structures could be elaborated from the enone products.