Silver(I)-Catalyzed Regioselective Construction of Highly Substituted α‑Naphthols and Its Application toward Expeditious Synthesis of Lignan Natural Products

A novel route has been developed for regioselective synthesis of highly substituted α-naphthols, binaphthols, and anthracenol through silver­(I) catalyzed C­(sp3)–H/C­(sp)–H, C­(sp2)–H/C­(sp)–H functionalization of β-ketoesters and alkynes, respectively, in a single step using water as a solvent. This protocol exhibited broad substrate scope and paved the way for synthesis of anticancer arylnaphthalene lignan natural products such as diphyllin, taiwanin E, and justicidin A with excellent selectivity.