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

Abstract

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(sp³)–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.