Construction of Lactones via Ligand-Enabled Ni-Catalyzed Alkene Hydroxylarylation/Lactonization

Here, we report the preparation of lactones via Ni-catalyzed alkene hydroxylarylation and sequential intramolecular lactonization with O2 as a green oxidant and oxygen source. The bulky 1,3-diketone ligand is crucial by enabling Ni-catalyzed hydroxylarylation of alkenes, providing numerous phthalide and furanone derivatives with high efficiency under mild conditions. The synthetic value of this methodology was further demonstrated by the efficient synthesis of typhaphthalide and a monoamine oxidase B inhibitor.