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Efficient loading of sulfonamide safety-catch linkers by Fmoc amino acid fluorides
Raffaele Ingenito1, Dijana Dreznjak, Stefan Guffler
1Jerini AG, Rudower Chaussee 29, 12489 Berlin, Germany. ingenito@jerini.com
Organic Letters
|April 2, 2002
Abstract:
[reaction: see text] 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.