Double C−H Activation: The Palladium-Catalyzed Direct C-Arylation of Xanthines with Arenes

Abstract

The novel Pd-catalyzed C(sp(2))-H/C(sp(2))-H cross-coupling of unactivated xanthines with unactivated arenes utilizing a combination of Ag(I) and O(2) as oxidants exclusively yields C-8 arylated xanthines in a single synthetic operation.