2. Academic Validation
  3. The backbone N-(4-azidobutyl) linker for the preparation of peptide chimera

The backbone N-(4-azidobutyl) linker for the preparation of peptide chimera

  • Org Lett. 2013 Sep 6;15(17):4572-5. doi: 10.1021/ol402150m.
Ana I Fernández-Llamazares 1,  Jesús García,  Jaume Adan,  David Meunier,  Francesc Mitjans,  Jan Spengler,  Fernando Albericio
Affiliations

Affiliation

  • 1 Institute for Research in Biomedicine (IRB), PCB, 08028-Barcelona, Spain.
PMID: 24006938 DOI: 10.1021/ol402150m
Abstract

A robust synthetic strategy for the introduction of the N-(4-azidobutyl) linker into Peptides using standard SPPS techniques is described. Based on the example of Cilengitide it is shown that the N-(4-azidobutyl) group exerts similar conformational restraints as a backbone N-Me group and allows conjugation of a desired molecule either via Click Chemistry or-after azide reduction-via acylation or reductive alkylation.

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