Synthesis of P-Chiral Tertiary Phosphine Oxides by Copper-Catalyzed Dynamic Kinetic Asymmetric C-P Cross-Coupling

P-Stereogenic phosphorus compounds are of importance in various areas. Some strategies have been developed for the enantioselective formation of C-P bonds, among which transition-metal -catalyzed asymmetric C-P cross-coupling of secondary phosphine oxides (SPOs)-bench-stable, odorless, and nontoxic-is more appealing. Due to the elusive racemization of SPOs, reactions with them usually proceed in a kinetic resolution fashion, thus being less practical. Highlighted here is a copper-catalyzed, highly enantioselective dynamic kinetic intermolecular C-P coupling of SPOs and aryl iodides. The successful development of this reaction relies on two key factors: the facile racemization of SPOs under the reaction conditions and the high enantioselectivity of the carefully tuned copper catalysts. P-Stereogenic tertiary phosphine oxide (TPO) products were obtained in high yields and with good enantioselectivities and were further converted into structurally diverse P-chiral scaffolds that are highly valuable as ligands and catalysts in asymmetric synthesis.