Efficient Loading of Sulfonamide Safety-Catch Linkers by Fmoc Amino Acid Fluorides
摘要:
[GRAPHICS]Fmoc-protected amino acid fluorides were found to be excellent reagents for the acylation of sulfonamide safety-catch linkers (SCL) suitable for the subsequent preparation of peptide C-terminal thioesters. High loadings were obtained on different types of resins with low levels of epimerization.
Germanium and Silicon Linking Strategies for Traceless Solid-Phase Synthesis
作者:Matthew J. Plunkett、Jonathan A. Ellman
DOI:10.1021/jo961889y
日期:1997.5.1
application of germanium and silicon linkage strategies for the solid-phasesynthesis of aromatic compounds, as demonstrated for 1,4-benzodiazepinederivatives. The metal-aryl bond that attaches the benzodiazepine to the polymeric support may be cleaved by electrophilic reagents such as H(+) and Br(2) to provide the corresponding substituted derivatives. A number of compounds have been prepared in good overall