Enantioselective phosphonation of isoquinolines <i>via</i> chiral phosphoric acid-catalyzed dearomatization

Abstract

An efficient and enantioselective phosphonation protocol for construction of chiral α-aminophosphates and α-aminodiarylphosphine oxides has been developed based on chiral phosphoric acid-catalyzed dearomatization of isoquinolines. A series of chiral 1,2-dihydroisoquinolines with dimethoxy phosphoryl or diphenylphosphono substituents at the C1-position were constructed with good to excellent yields and enantioselectivities under mild reaction conditions.