Asymmetric Michael addition of malonates to enones catalyzed by a primary β-amino acid and its lithium salt

J Org Chem. 2011 Oct 21;76(20):8513-7. doi: 10.1021/jo201429w. Epub 2011 Sep 16.

Abstract

Highly enantioselective Michael addition of malonates to enones was achieved using a mixed catalyst consisting of a primary β-amino acid, O-TBDPS (S)-β-homoserine, and its lithium salt. Various cyclic and acyclic enones were converted into 1,5-ketoesters in high yields (up to 92%) with high enantioselectivity (up to 97% ee) under mild reaction conditions. Details of synthesis of the catalyst, optimization of the reaction conditions for the Michael addition reaction, and a plausible reaction mechanism are described.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Products / chemical synthesis*
  • Catalysis
  • Chemistry, Pharmaceutical / methods*
  • Homoserine / chemistry
  • Ketones / chemistry*
  • Lithium / chemistry
  • Magnetic Resonance Spectroscopy
  • Malonates / chemistry*
  • Molecular Structure
  • Organosilicon Compounds / chemistry
  • Salts / chemistry
  • Stereoisomerism

Substances

  • Biological Products
  • Ketones
  • Malonates
  • Organosilicon Compounds
  • Salts
  • t-butyldimethylsilyl compounds
  • Homoserine
  • Lithium