Regioselective and stereospecific amination of iridoids: conversion of aucubin into aminoside antibiotic analogues

J Nat Prod. 2007 Jan;70(1):19-23. doi: 10.1021/np060368v.

Abstract

Treatment of aucubin (1) with tert-butyldimethylsilyl chloride under alkaline conditions permitted regioselective silylation of either the primary hydroxyl groups at C-9 and C-6' or both primary hydroxyl groups and the secondary allylic hydroxyl group at C-6. Acetylation with acetic anhydride, followed by selective removal of the silyl groups and Mitsunobu reaction involving phthalimide as nitrogen donor, gave a stereospecific entry to aminoside antibiotic analogues: 10,6'-diamino-10,6'-dideoxyaucubin (16) and (6R)-6,10,6'-triamino-6,10,6'-trideoxyaucubin (17).

MeSH terms

  • Amination
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Bacteria / drug effects*
  • Glucosides / chemistry*
  • Iridoid Glucosides
  • Iridoids / chemistry*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Stereoisomerism

Substances

  • Anti-Bacterial Agents
  • Glucosides
  • Iridoid Glucosides
  • Iridoids
  • aucubin