Copper-Catalyzed N-Arylation of Pyranoquinolinones with Boronic Acids at Room Temperature without Ligand

Pyranoquinolinones synthesized from citral were used for Cu-catalyzed N-arylation with a wide range of arylboric acids. The reaction proceeded well broad substrate scope, providing direct way to access highly functional pyranoquinolinone core structure derivatives in yields up 80%. Compared citral, the compounds we obtained have much better inhibitory effect on HeLa cervical cancer cells, and compound 3p has an IC50 value 4.6 μM, lower than cisplatin’s 5.9 μM.