Rhodium-catalyzed regioselective direct C–H arylation of indoles with aryl boronic acids

A highly efficient Rh(III)-catalyzed direct C–H arylation of indoles with aryl boronic acids under mild conditions has been developed. The methodology features wide substrate scope and excellent functional group compatibility (34 examples, up to 99% yield). The arylated products can also be conveniently transformed into biologically active polycyclic indole derivatives.