Spectinomycin modification. II. Spectinomycin C-3'-modification via diazoketone intermediates

J Antibiot (Tokyo). 1985 Feb;38(2):197-207. doi: 10.7164/antibiotics.38.197.

Abstract

The C-3'-carbonyl group of N-protected spectinomycin is efficiently converted into a diazo group via base treatment of the corresponding tosylhydrazone. The diazo group imparts a new synthetically useful reactivity pattern on the sugar ring of the molecule. The synthesis of C-3'-deoxo-, monohalo- and dihalospectinomycins via the intermediacy of these diazo compounds is described. The reduced bioactivity of these analogs as compared to the parent and the C-3'-dihydro and aminospectinomycins established the need for hydrogen bonding groups in this region of the molecule for good activity, further refining the structure activity relationships in the spectinomycin series.

MeSH terms

  • Chemical Phenomena
  • Chemistry
  • Diazomethane / analogs & derivatives*
  • Hydrogen Bonding
  • Spectinomycin*
  • Structure-Activity Relationship

Substances

  • diazomethyl ketones
  • Diazomethane
  • Spectinomycin