Access to Chiral Cyclic β‐Enaminones via Enantioselective Imine Condensation

Abstract

Abstract We report herein an unprecedented catalytic enantioselective synthesis of cyclic β‐enaminones from simple meso‐1,3‐diketones via chiral phosphoric acid‐catalyzed desymmetrization through imine condensation. This transformation provides efficient access to a broad array of cyclic β‐enaminones and acridinones bearing a remote β‐stereogenic center, delivering products in excellent yields and enantioselectivities under mild conditions with a straightforward protocol. Furthermore, the resulting β‐enaminones can undergo one‐step derivatizations to furnish diverse enantioenriched carbo‐ and heterocycles, highlighting their high potential for applications in medicinal chemistry.