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.