Ring contraction of oleandrose on the macrolide antibiotic oleandomycin with [(Methoxycarbonyl)sulfamoyl]triethylammonium hydroxide inner salt

J Med Chem. 1982 Jul;25(7):881-4. doi: 10.1021/jm00349a025.

Abstract

Ring contraction of the neutral oleandrose sugar in the 14-membered-ring macrolide antibiotic oleandomycin (2) has been accomplished using [(methoxycarbonyl)sulfamoyl]triethylammonium hydroxide inner salt (1). The product of this interesting rearrangement, after methanolic hydrolysis of the 2'-acetate, is the 11-acetyl-3-O-(3"-methoxy-4"-vinylfuranosyl)oleandomycin (12). The in vitro activity of furanoside 12 is only moderately less than that of 11-acetyloleandomycin (13).

MeSH terms

  • Bacteria / drug effects
  • Bacterial Proteins / biosynthesis
  • Chemical Phenomena
  • Chemistry
  • Deoxy Sugars*
  • Hexoses*
  • Oleandomycin / analogs & derivatives*
  • Oleandomycin / chemical synthesis
  • Oleandomycin / pharmacology
  • Quaternary Ammonium Compounds*

Substances

  • Bacterial Proteins
  • Deoxy Sugars
  • Hexoses
  • Quaternary Ammonium Compounds
  • oleandrose
  • ((methoxycarbonyl)sulfamoyl)triethylammonium
  • Oleandomycin