Preparation of α-chlorinated chiral β-keto phosphine oxides by cinchona alkaloid-catalyzed asymmetric chlorination

A cinchona alkaloid-catalyzed asymmetric chlorination of β-ketophosphine oxides has been established, enabling efficient access to chiral α-chlorinated phosphine oxides with a sterically hindered tertiary carbon stereocenters. This protocol proceeds with high yields, broad substrate compatibility, moderate to excellent enantioselectivity, and employs readily available chlorinating reagents. • Cinchona-alkaloid-catalyzed asymmetric chlorination of β-ketophosphine oxides for the first time • High yields, broad substrate scope • Moderate to good enantioselectivity