Enantioselective synthesis of chiral γ-aryl α-keto ester by copper-catalyzed 1,4-conjugate addition using D 2-symmetric biphenyl phosphoramidite ligand

Abstract: Cu-catalyzed enantioselective 1,4-conjugate addition of β,γ-unsaturated α-keto ester compound was carried out to afford chiral γ-substituted γ-aryl α-keto ester, which could be conveniently converted to the potential skeleton of new Pril drugs. Up to 81% ee and 99% yield were afforded for the 1,4-conjugate addition using D 2-symmetric biphenyl phosphoramidite ligand. [Copyright &y& Elsevier]