Palladium‐Catalyzed Asymmetric [3+2] Cyclization for the Synthesis of Chiral 2,3‐dihydrofuran Regulated by the Side‐Arm Effect of diSaBOX Ligands

ABSTRACT We have developed a synthetic method for the asymmetric [3+2] cyclization to synthesize chiral 2,3‐dihydrofurans using a novel diSaBOX ligand. The Hammett equation and kinetic experiments were employed to reveal the influence of different substituents on the side arm of the diSaBOX ligand on the enantioselectivity and reaction rate of the reaction. This method exhibits good functional group tolerance and can modify a variety of biologically active molecules. The reaction mechanism of this palladium‐catalyzed [3+2] cyclization was further clarified through nonlinear experiments and intermolecular competition experiments.