Palladium(0)-Catalyzed Regioselective Three-Component Cross-Coupling via C–H Activation: Synthesis of Eight-Membered Azacycles

A Pd(0)-catalyzed three-component cross-coupling reaction involving <i>o</i>-bromobenzylamines, aryl iodides, and alkynes was developed through C-H activation. This reaction exhibits excellent regioselectivity, selectively forming a C(vinyl)-C(aryl) bond. The process yields eight-membered azacycles as the products, providing straightforward access to such compounds using simple substrates.