Peptide Modifications to Increase Metabolic Stability and Activity

Volume 1081 of the series Methods in Molecular Biology pp 1-11


Hantzsch Based Macrocyclization Approach for the Synthesis of Thiazole Containing Cyclopeptides

  • Adel NefziAffiliated withTorrey Pines Institute for Molecular Studies

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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.

Key words

Cyclic peptides Thioalkylation Solid-phase synthesis Parallel synthesis 4-Chloromethyl thiazoles