Application of chiral bi- and tetra-dentate bispidine-derived ligands in the copper(II)-catalyzed asymmetric Henry reaction

The application of a number of chiral bispidine-based ligands in the copper-catalyzed enantioselective Henry reaction is here reported. The results showed good conversion rates and low to moderate enantiomeric ratios, depending on the substituents on the bispidine core. The enantioselectivities of selected ligands were rationalized on the basis of single-crystal X-ray analyses, NMR studies and computational tools.