A ruthenium(Ⅱ)‐catalyzed C‐H acylmethylation of Trp‐containing peptides with α‐chloro ketones has been reported. This reaction features good C‐2 selectivity and chemoselectivity，making it suitable for the late‐stage modification of Trp‐containing peptides. Low‐cost metal ruthenium as a catalyst enables the reaction to be conducted on a gram scale. This report also discusses the synthetic applications and presents a method to remove the pyridine directing group. In addition, a plausible mechanism of the C(2)‐H acylmethylation reaction is proposed in this article.

中文翻译：

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钌 （II） 催化的吡啶定向色氨酸 C-H 酰基甲基化与 α-氯酮


据报道，含钌 （II.） 催化的含 Trp 的肽与 α-氯酮的 C-H 酰甲基化。该反应具有良好的 C-2 选择性和化学选择性，使其适用于含 Trp 的肽的后期修饰。低成本金属钌作为催化剂，使反应能够在克级上进行。本报告还讨论了合成应用，并提出了一种去除吡啶定向基团的方法。此外，本文还提出了 C（2）-H 酰基甲基化反应的合理机制。