Palladium-catalyzed methylene C(sp3)-H arylation of the adamantyl scaffold

The adamantyl group is prevalent as a key pharmacophore element in drugs. We describe herein a palladium-catalyzed C-H functionalization logic for the methylene C(sp(3))-H arylation of the adamantyl scaffold with the assistance of an amide group. The resulting arylated adamantyl amide was smoothly converted to an amine, providing facile access to the memantine analog.