Enantioselective PCCP Brønsted Acid Catalyzed Aminalization of Aldehydes

Here we present an enantioselective aminalization of aldehydes catalyzed by Bronsted acids based on pentacarboxycyclopentadienes (PCCPs). The cyclization reaction using readily available anthranilamides as building blocks provides access to valuable 2,3-dihydroquinazolinones containing one stereogenic carbon center with good enantioselectivity (ee up to 80%) and excellent yields (up to 97%).