Copper-catalyzed oxidative phosphonoheteroarylation of alkenes with phosphonates and N-heteroarenes via P–H/C–H functionalization

Abstract

A copper-catalyzed oxidative intermolecular phosphonoheteroarylation of alkenes with phosphonates and nucleophilic N-heteroarenes (such as indoles and pyrroles) involving P–H/C–H functionalization for the synthesis of highly valuable β-(N-heteroaryl)-alkylphosphonates is disclosed. This method allows the incorporation of two functional groups, a phosphonate and a N-heteroarene, into the alkene in a single reaction step through oxidative formation of the P-centered radicals, addition across the CC bond, single electron oxidation and C–H functionalization cascades.