Enantioselective PCCP Brønsted Acid Catalyzed Aminalization of Aldehydes

Abstract

Here we present an enantioselective aminalization of aldehydes catalyzed by Brønsted acids based on pentacarboxycyclopentadienes (PCCPs). Cyclization reaction using readily available anthranilamides as building-blocks provides an access to valuable 2,3-dihydroquinazolinones containing one stereogenic carbon center with high degree of enantioselectivities (ee up to 81 %) and excellent yields (up to 97%).