Pd(ii)-Catalyzed asymmetric intramolecular arylation of unbiased methylene C(sp3)–H bonds using readily accessible 3,3′-F2-BINOL as a chiral ligand

Abstract

Herein, we report a Pd(II)-catalyzed asymmetric intramolecular arylation of unbiased methylene C(sp³)–H bonds using 2-pyridylisopropyl (PIP) as a directing group and readily accessible 3,3′-F₂-BINOL as a chiral ligand. The reaction provided a straightforward and efficient strategy to access various chiral benzo-fused six-membered heterocyclic compounds with excellent yields (up to 99%) and enantioselectivities (up to 97%). The PIP directing group could be removed under mild conditions without the loss of enantiopurity.