Abstract
AbstractSynthesis of previously unknown 5‐alkynyl‐L‐histidines and 2,5‐dialkynyl‐L‐histidines is reported. Fully protected 5‐iodo‐ and 2,5‐diiodo‐L‐histidines obtained upon electrophilic iodination underwent cross‐coupling alkynylation reaction with terminal alkynes in the presence of palladium‐copper co‐catalytic system to afford ring‐modified histidines in 62–85 % yield. The method is also successfully utilized to late‐stage alkynylate a 5‐iodohistidine residue containing peptide.
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