Abstract
A series of chiral binaphthyl-containing diphenylethylenediamine (binaph-dpen) ligands was designed and synthesized for the copper-catalyzed asymmetric Henry reaction. The <i>N</i>-monobenzyl (<i>S</i>)-binaph-(<i>R</i>,<i>R</i>)-dpen ligand, with a secondary amine portion, promoted the Cu(OAc)<sub>2</sub>-catalyzed Henry reaction with excellent enantioselectivity in an <i>anti</i>-selective manner.
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