Modular Access to Aryl Quinolinyl Ketones via Visible Light‐Induced Palladium‐Catalyzed Aldehyde C‐H Bond Arylation of Quinoline‐8‐Carbaldehydes with Arylboronic Acid

This article describes the development of a room‐temperature visible light‐induced palladium‐catalyzed directed aldehyde C‐H bond arylation to access aryl quinolinyl ketones. In this pathway, the Pd catalyst plays a dual role by harvesting light as a photocatalyst and catalyzing the chemical transformation via C‐H bond activation. This process is general to synthesize a range of aryl quinolinyl ketones and tolerates many common functional groups. Our methodology was successfully applied to synthesize highly potent tubulin polymerization inhibitors.