A ruthenium(II)-catalyzed C−H acylmethylation of Trp-containing peptides with α-chloro ketones is reported here. This reaction features good C-2 selectivity and chemoselectivity, making it suitable for 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

这里报道了含钌 （II） 催化的含 Trp 的肽与 α-氯酮的 C-H 酰基甲基化。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。