Ir-catalyzed Transfer Hydrogenation and N-alkylation of Alkynyl/alkenyl Arylamines with Carbonyls in Water

Herein, we advance a novel and efficient iridium-catalyzed transfer hydrogenation and N-alkylation of alkynyl/ alkenyl arylamines with carbonyls to facilitate the streamlined synthesis of diverse amines. The reaction could be achieved direct hydrogenation and alkylation of alkynyl/alkenyl arylamines with carbonyls using H2O as reaction media and HCO2H as hydrogen donor, providing a variety of arylamine derivatives in moderate to excellent yields. Control experiments indicated the N-alkylation of alkynyl/alkenyl arylamines contributed to the reduction of alkynes/alkenes. The practicality of this sustainable process was evidenced by large-scale, catalyst recycling experiments and derivatization of biologically active molecules.