Peptide and protein modifications, especially late-stage derivatization, are invaluable for the synthesis of new pharmaceuticals. Currently, cysteine-mediated peptide modification is mainly limited to bioconjugation and disulfide formation. Therefore, exploration of new cysteine mediated peptide modifications is of great interest. Herein, we present a practical strategy for the three-step, one-pot desulfurative functionalization of cysteine containing peptides. The use of a pyridinium salt enables diverse and selective functionalization with an array of nucleophiles such as amino acid side chains, pharmaceuticals and macrocyclizations. This method allows for easy and diverse late-stage modification of peptides enabling the discovery and synthesis of new pharmaceuticals.

中文翻译：

---

使用吡啶盐对含半胱氨酸的肽进行一锅法化学选择性脱硫功能化

肽和蛋白质修饰，尤其是后期衍生化，对于新药的合成非常宝贵。目前，半胱氨酸介导的肽修饰主要限于生物偶联和二硫键形成。因此，探索新的半胱氨酸介导的肽修饰具有极大的意义。在此，我们提出了一种实用的策略，用于含半胱氨酸肽的三步一锅脱硫功能化。使用吡啶盐可实现一系列亲核试剂（如氨基酸侧链、药物和大环化）的多样化和选择性官能化。该方法允许对肽进行简单多样的后期修饰，从而能够发现和合成新药。