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Macrocyclization via an efficient high-yielding solid-phase intramolecular thioalkylation reaction is described. The reaction of S-nucleophiles with newly generated N-terminal 4-chloromethyl thiazoles led to the desired macrocyclization products 5 in high purities and good overall yields.

Two-Step Hantzsch Based Macrocyclization Approach for the Synthesis of Thiazole-Containing Cyclopeptides