Rh(III)-catalyzed chelation-assisted intermolecular carbenoid functionalization of α-imino Csp(3)-H bonds.

A Rh(iii)-catalyzed cross-coupling/cyclization cascade of α-imino Csp(3)-H bonds with donor/acceptor α-acyl diazocarbonyl compounds has been developed. This novel transformation involves ligand-directed Csp(3)-H bond functionalization with carbenoids under the pyridine-chelation assistance, and offered an efficient access to synthetically versatile polysubstituted N-(2-pyridyl)pyrroles with a broad range of functional group tolerance.