Atroposelective Construction of Axially Chiral 2-Aryl-Pyrroloquinolones

A two-step protocol including an enantioselective organocatalyzed synthesis of pyrroloquinolines followed by an oxidation reaction allowed the formation of axially chiral 2-aryl-pyrroloquinolones. Thorough optimization of the experimental conditions for the second step allowed the oxygenation reaction to take place and ensured, in most cases, a central-to-axial chirality conversion with complete retention of the enantiomeric excess.