Chiral Phosphoric Acid-Catalyzed Synthesis of Fluorinated 5,6-Dihydroindolo[1,2- c]quinazolines with Quaternary Stereocenters.

A chiral phosphoric acid-catalyzed enantioselective synthesis of fluorinated 5,6-dihydroindolo[1,2- c]quinazolines has been developed by a condensation/amine addition cascade from 2-(1 H-indolyl)anilines and fluorinated ketones, giving the fluorinated aminals with quaternary stereogenic centers with excellent yields and up to 97% ee. A series of the fluorinated aromatic, aliphatic ketones, and ethyl trifluoropyruvate are suitable.