Synthesis of Polysubstituted 2‐Naphthols by Palladium‐Catalyzed Intramolecular Arylation/Aromatization Cascade

A palladium‐catalyzed intramolecular α‐arylation and defluorinative aromatization strategy for the synthesis of polysubstituted 2‐naphthols is reported. With ortho‐bromobenzyl‐substituted α‐fluoroketones as the substrates and palladium acetate/triphenylphosphine as the catalyst, this method features good functional group tolerance, readily available catalyst and starting materials, and high yields. The applications of the strategy are demonstrated by the synthesis of useful building blocks, such as naphtha[2,3‐b]furan, naphthol AS‐D, and ligands/catalysts.