Copper-catalyzed aerobic double functionalization of benzylic C(sp)-H bonds for the synthesis of 3-hydroxyisoindolinones.

A copper-catalyzed aerobic 3-hydroxyisoindolinone synthesis was developed via the benzylic double C(sp)-H functionalization of 2-alkylbenzamides. In this reaction, molecular oxygen was used as both an oxidant for C(sp)-H functionalization and an oxygen source. Our method can be extended to diverse benzylic C(sp)-H bonds and shows excellent functional group tolerance.