Pd(ii)-Catalyzed [3 + 2] spiroannulation of α-aryl-β-naphthols with alkynes via a C–H activation/dearomatization approach

Abstract

Readily available α-aryl-β-naphthols undergo a [3 + 2] spiroannulation with internal alkynes upon treatment with a Pd(II) catalyst and an oxidant. This transformation involves sequential C–H activation, alkyne migratory insertion, and naphthol dearomatization, affording highly appealing spirocyclic molecules in high yields with good functional group tolerance. Preliminary results with chiral phosphoramidite ligands indicate that enantioselective variants are feasible for this process.