Copper-Catalyzed 1,4-Alkylarylation of 1,3-Enynes with Ethers and Aryl Boronic Acids Enabled via C(sp3)-H Functionalization

J Org Chem. 2025 Jan 17. doi: 10.1021/acs.joc.4c02207. Online ahead of print.

Abstract

Herein, we present a copper-catalyzed, three-component intermolecular 1,4-alkylarylation of 1,3-enynes with ethers and aryl boronic acids. This method, driven by α-C(sp3)-H functionalization of the oxygen atom in ethers, regioselectively produces various tetrasubstituted allenes from simple, readily available precursors. Key features include mild reaction conditions and a simple catalytic system.