Formal Transition-Metal-Catalyzed Phosphole C-H Activation for the Synthesis of Pentasubstituted Phospholes.

Unprecedented formal transition-metal-catalyzed phosphole C-H functionalization is described in this paper. Pentasubstituted phospholes were prepared via the copper-catalyzed reaction of 1,3,4-trisubstituted phosphole with aryl iodides or bromides under distinct conditions. The developed methodology is able to accommodate a wide variety of substituents, including aryl, heteroaryl, and alkenyl.