Hantzsch based macrocyclization approach for the synthesis of thiazole containing cyclopeptides

Abstract

An innovative macrocyclization approach via high-yielding solid-phase intramolecular thioalkylation reaction is described. The reaction of S-nucleophiles with newly generated N-terminal 4-chloromethyl thiazoles leads to the desired cyclic products in high purities and good yields. © 2013 Springer Science+Business Media New York.