Selective Synthesis of Isoquinolines by Rhodium(III)-Catalyzed C–H/N–H Functionalization with α‑Substituted Ketones

A rhodium­(III)-catalyzed C–H/N–H bond functionalization for the synthesis of 1-aminoisoquinolines from aryl amidines and α-MsO/TsO/Cl ketones was achieved under mild reaction conditions. Thus, this approach provides a practical method for the site-selective synthesis of various synthetically valuable isoquinolines with wide functional group tolerance.