Organocatalytic Enantioselective Chloroiminocyclization for the Synthesis of Imidazoline

Imidazoline is an important scaffold in organic synthesis and a pharmacophore in medicinal chemistry. We apply basic imines as nucleophiles for the catalytic asymmetric chloroiminocyclization to furnish tetrasubstituted stereocenter-containing imidazolines in excellent yields and enantioselectivities. The reaction can be conducted in the polar solvent acetonitrile under concentrated reaction conditions.