Rh(III)-Catalyzed Synthesis of Multisubstituted Isoquinolines from Benzylamines and Diazo Compounds

Multisubstituted isoquinolines have been prepared by Rh(III)-catalyzed cyclization of benzylamines with diazo compounds via aryl C-H bond activation using molecular oxygen from air as an oxidant. This method features mild reaction conditions, simple catalytic system, tolerance of a broad range of substrates, high efficiency and regioselectivity.