Palladium-Catalyzed C-H Oxidation of Isoquinoline N-Oxides: Selective Alkylation with Dialkyl Sulfoxides and Halogenation with Dihalo sulfoxides

A novel palladium-catalyzed C?H oxidation of isoquinoline N-oxides has been developed for regioselectively synthesizing substituted isoquinolines. The method represents the first example of using dialkyl sulfoxides as the alkyl sources for the construction of 1-alkylated isoquinolines. Moreover, the regioselective halogenation of isoquinoline N-oxides is also successful using dihalo sulfoxides as the halide sources.