Decarboxylative Aminomethylation of Ferulic Acids via Visible‐Light‐Promoted Flavin Photocatalysis and its Application in the Synthesis of Anti‐Inflammatory Lead Compounds

Herein, we report a protocol for the direct visible‐light‐promoted decarboxylative aminomethylation of ferulic acid with N‐aryl tetrahydroisoquinolines under air atmosphere. The current protocol uses naturally available ferulic acid as coupling partner, the inexpensive organic photocatalyst riboflavin tetraacetate (RFTA) as photocatalyst and molecular oxygen as oxidant, which is suitable for late‐stage functionalization of complex nitrogen‐containing molecules. This methodology further demonstrated its utility by the protecting‐group‐free semi‐synthesis of natural alkaloids maclekarpine E and by assessing the anti‐inflammatory activity of its analogues.