Highly enantioselective synthesis of alpha-stereogenic esters through catalytic asymmetric michael addition of 4-oxo-4-arylbutenoates

Chemistry. 2010 Sep 3;16(33):10130-6. doi: 10.1002/chem.201001129.

Abstract

Highly enantioselective Michael addition of 1,3-dicarbonyl compounds and nitromethane to 4-oxo-4-arylbutenoates catalyzed by N,N'-dioxide-Sc(OTf)(3) complexes has been developed. Using 0.5-2 mol % catalyst loading, various alpha-stereogenic esters were obtained regioselectively with excellent yields (up to 97 %) and enantioselectivities (up to >99 % ee). Moreover, the reaction performed well under nearly solvent-free conditions. The products with functional groups are ready for further transformation, which showed the potential value of the catalytic approach. According to the experimental results and previous reports, a plausible working model has been proposed to explain the origin of the activation and the asymmetric induction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry*
  • Butyrates / chemistry*
  • Catalysis
  • Esters / chemical synthesis*
  • Mesylates / chemistry
  • Molecular Conformation
  • Molecular Structure
  • Scandium / chemistry
  • Stereoisomerism

Substances

  • Alkenes
  • Butyrates
  • Esters
  • Mesylates
  • scandium triflate
  • Scandium