Asymmetric synthesis of alpha,alpha-difluoro-beta-amino acid derivatives from enantiomerically pure N-tert-butylsulfinimines

J Org Chem. 2002 Nov 15;67(23):8276-9. doi: 10.1021/jo0259313.

Abstract

Addition of the Reformatsky reagent derived from ethyl bromodifluoroacetate to alkyl- and aryl-substituted N-tert-butylsulfinimines furnishes beta-tert-butylsulfinamyl-beta-substituted alpha,alpha-difluoroproponiates in diastereomeric ratios ranging from 80:20 to 95:5. The diastereomers are easily separated and the enantiomerically pure, protected beta-amino esters are readily transformed to the corresponding acid, amide, and amine derivatives as useful synthons for medicinal chemistry targets.

MeSH terms

  • Amino Acids / chemical synthesis*
  • Fluorine
  • Imines
  • Stereoisomerism
  • Sulfonamides / chemistry

Substances

  • Amino Acids
  • Imines
  • Sulfonamides
  • tert-butylsulfonamide
  • Fluorine