Efficient asymmetric synthesis of the vasopeptidase inhibitor BMS-189921

Org Lett. 2003 Aug 21;5(17):3155-8. doi: 10.1021/ol0352308.

Abstract

[reaction: see text] An efficient asymmetric synthesis of the vasopeptidase inhibitor BMS-189921 was accomplished. Two short enantioselective syntheses of the common key intermediate (S)-alpha-aminoazepinone 6b were developed. Olefin 3 was converted to 6b via asymmetric hydrogenation. Alternatively, enyne 12 was converted to racemic alpha-aminoazepinone 15b, which was transformed to 6b by a practical dynamic resolution.

MeSH terms

  • Azepines / chemical synthesis*
  • Azepines / chemistry*
  • Azepines / pharmacology
  • Endothelium, Vascular / enzymology*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Hydrogenation
  • Neprilysin / antagonists & inhibitors*
  • Stereoisomerism

Substances

  • Azepines
  • Enzyme Inhibitors
  • Neprilysin
  • gemopatrilat