Regioselective Ruthenium-Catalyzed Carbonylative Direct Arylation of Five-Membered and Condensed Heterocycles

摘要

A ruthenium-catalyzed carbonylative C-H bond arylation process for the three-component synthesis of complex aryl–(hetero)aryl ketones in an aqueous solution has been developed. By exploiting the ortho-activating effect of nitrogen-containing directing groups, a regioselective, successive twofold C(sp~2)-C(sp~2) bond formation has been achieved. This straightforward catalytic process provides access to versatile products prevalent in multiple bioactive compounds and supplies a valuable functional group for subsequent transformations.