LAUSR

An unprecedented base‐metal‐catalyzed oxidative cross‐coupling between 2‐naphthols and phenols or arylamines has been described in this report. Acetic acid and 2,2,6,6‐tetramethylpiperidine‐1‐oxyl (TEMPO) are the crucial oxidative system that promotes the transformation under aerobic conditions with the assistance of base‐metal salts. While ferrous sulfate was the optimal catalyst in the oxidative coupling of 2‐naphthols and phenols to produce 4‐aryloxynaphthalene‐1,2‐diones, cuprous iodide catalyst is utilized to synthesize (arylimino)naphthalen‐1(4H)‐ones from 2‐naphthols and arylamines. Employing this protocol, molecule skeletons similar to tanshinones, 2‐(2‐carboxyvinyl)benzoic acid and neo‐tanshinlactone can be accessed thus highlighting its potential use in organic synthesis and drug discovery.