Chiral Phosphoric Acid‐Catalyzed Asymmetric Aza‐Friedel–Crafts Reaction of Indoles with Cyclic <i>N</i>‐Acylketimines: Enantioselective Synthesis of Trifluoromethyldihydroquinazolines

Abstract

Abstract An enantioselective aza‐Friedel–Crafts (F‐C) reaction of indoles with cyclic N ‐acylketimines has been developed. By using chiral phosphoric acid catalysts, a wide range of enantioenriched trifluoromethyldihydroquinazolines was obtained in excellent yields (up to 98%) with good to high enantioselectivities (up to 99% ee ). magnified image