Chiral Phosphoric Acid-Catalyzed Enantioselective Three-Component Povarov Reaction Using Cyclic Enethioureas as Dienophiles: Stereocontrolled Access to Enantioenriched Hexahydropyrroloquinolines

International audience; Three become one: Phosphoric acid-catalyzed enantioselective three-component Povarov reactions of aldehydes, anilines, and endocyclic enethioureas have been developed. This process afforded hexahydropyrroloquinolines in high yields with excellent diastereo- and enantioselectivities. The presence of the thiourea functionality is crucial for the enantioselectivity of the reaction.