Ligand- and Substrate-Controlled Chemodivergent Pd-Catalyzed Annulations of Cyclic β-Keto Esters with 3-Aryl-2 H-azirines

Org Lett. 2022 Jan 14;24(1):268-273. doi: 10.1021/acs.orglett.1c03933. Epub 2021 Dec 10.

Abstract

Chemodivergent Pd-catalyzed annulations of cyclic β-keto esters with 3-aryl-2H-azirines have been developed to provide rapid access to eight-membered ring lactams, bicyclic 3,4-dihydro-2H-pyrrole derivatives, and (E)-methyl [2-(2-oxocyclohexylidene)-2-phenylethyl]carbamates with high efficiency. The chemoselectivity can be determined by tuning the mono- or bisphosphine ligands as well as the substrate structure of cyclic β-keto esters.