Synthesis of hydrazinopeptides using solid-phase N-electrophilic amination: extension to the Fmoc/tert-butyl strategy and chemistry of the N-N bond in strong acid media

J Pept Res. 1999 Oct;54(4):270-8. doi: 10.1034/j.1399-3011.1999.00105.x.

Abstract

The synthesis of hydrazinopeptides using solid-phase N-electrophilic amination was extended to the Fmoc/tert-butyl strategy. Both Boc/benzyl and Fmoc/tert-butyl strategies led to the isolation of by-products arising from the partial instability of the N-N bond during the final cleavage and deprotection step. Two paths of decomposition have been shown: the cleavage of the N-N bond leading to the regeneration of the amine and a Hofmann-type elimination yielding original dianisyl adducts. Our data suggest that the Fmoc/tert-butyl strategy is better suited for the synthesis of hydrazinopeptides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acids
  • Amination
  • Amino Acid Sequence
  • Fluorenes / chemistry
  • Hydrazines / chemistry*
  • Mass Spectrometry
  • Molecular Sequence Data
  • Peptide Biosynthesis*

Substances

  • Acids
  • Fluorenes
  • Hydrazines