Transition‐metal‐catalyzed C−H activation has shown potential in the functionalization of peptides with expanded structural diversity. Herein, the development of late‐stage peptide macrocyclization methods by palladium‐catalyzed site‐selective C(sp²)−H olefination of tryptophan residues at the C2 and C4 positions is reported. This strategy utilizes the peptide backbone as endogenous directing groups and provides access to peptide macrocycles with unique Trp–alkene crosslinks.

中文翻译：

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钯催化色氨酸的位点选择性CH Oleflation后期肽大环化。

过渡金属催化的CH活化在具有扩大的结构多样性的肽的功能化中显示出潜力。本文报道了通过钯催化的C2和C4位色氨酸残基的位点选择性C（sp ²）-H烯化钯催化后期肽大环化方法的发展。该策略利用肽骨架作为内源性指导基团，并提供具有独特的Trp-烯烃交联键的肽大环化合物。