The Backbone N-(4-Azidobutyl) Linker for the Preparation of Peptide Chimera

Autor: Jaume Adan, Ana I. Fernández-Llamazares, Francesc Mitjans, Jesús García, David Meunier, Fernando Albericio, Jan Spengler
Rok vydání: 2013
Předmět:
Zdroj: Organic Letters. 15:4572-4575
ISSN: 1523-7052
1523-7060
DOI: 10.1021/ol402150m
Popis: 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.
Databáze: OpenAIRE