Copper-Catalyzed Enantioselective Synthesis of β-Boron β-Amino Esters

In this report, the enantioselective, copper-catalyzed borylation of beta-amidoacrylates is disclosed. A broad variety of biologically important alpha-aminoboronates has been prepared with consistently high levels of enantiocontrol using an inexpensive copper catalyst and a commercially available chiral ligand. The method can be applied to the synthesis of novel boron-containing dipeptides and hemiboronates.