A novel method synthesizes a tyr to trp linkage in noncanonical cyclic peptides, enabling new biaryl incorporation.
In this study, a facile synthesis method for a highly strained Tyr C6‐to‐Trp C5′ linkage was developed. This method enables the convergent introduction of arbitrary biaryls to peptide linkers through electrochemically assisted Ni‐catalyzed cross‐electrophile coupling, followed by regioselective Larock macrocyclization. Additionally, using this approach, the total synthesis of the ribosomally synthesized and post‐translationally modified peptide (RiPP) molecule micitide 982 was accomplished. Furthermore, this synthetic strategy allows for the incorporation of various biaryls.
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Ogawa et al. (2025) studied this question.
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