Asymmetric synthesis of both enantiomers of anti-4,4,4-trifluorothreonine and 2-amino-4,4,4-trifluorobutanoic acid

J Org Chem. 2003 Sep 19;68(19):7544-7. doi: 10.1021/jo0344384.

Abstract

A short and efficient enantioselective synthesis of both enantiomers of anti-4,4,4-trifluorothreonine and 2-amino-4,4,4-trifluorobutanoic acid was successfully developed. Trifluoromethylation of benzyl-protected bromoalkene 4 provided key intermediate trifluoromethylated trans-disubstituted alkene 2 in good yield. The sequence then involved Sharpless asymmetric dihydroxylation, nucleophilic opening of cyclic sulfate with NaN(3), palladium-catalyzed selective hydrogenation, and oxidation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids / chemical synthesis*
  • Amino Acids / chemistry
  • Butyrates / chemical synthesis*
  • Chemistry, Pharmaceutical
  • Fluorine*
  • Hydrocarbons, Fluorinated
  • Stereoisomerism
  • Threonine / analogs & derivatives
  • Threonine / chemical synthesis*

Substances

  • 2-amino-4,4,4-trifluorobutanoic acid
  • Amino Acids
  • Butyrates
  • Hydrocarbons, Fluorinated
  • anti-4,4,4-trifluorothreonine
  • Fluorine
  • Threonine