One-step synthesis of 2-arylindoles from indolines Pd-catalyzed oxidative dehydrogenation and C2-selective arylation.

We report an efficient synthetic approach to 2-arylindoles from indolines a one-step process involving Pd-catalyzed oxidative dehydrogenation and a sequential C2-regioselective Heck-type reaction. The mild reaction conditions, which utilize O as the sole oxidant, show a broad substrate scope and good functional group compatibility.