Copper-catalyzed 4-HO-TEMPOH mediated phosphorylation of alkenes

Org Biomol Chem. 2023 Jun 28;21(25):5171-5175. doi: 10.1039/d3ob00607g.

Abstract

An efficient, practical and regioselective synthesis of (E)-alkenylphosphine oxides has been developed starting from alkenes under copper catalysis and 4-HO-TEMPOH oxidation. Preliminary mechanistic studies clearly reveal that a phosphinoyl radical is involved in this process. Moreover, this method features mild reaction conditions, good functional group tolerance, and excellent regioselectivity and also promises to be efficient for the late-stage functionalization of drug molecular skeletons. The reaction will create an opportunity for the synthesis of complex phosphorus containing bioactive molecules.