We present a highly selective protocol for the ortho benzylation of N-aryl amides. This method offers mild conditions, excellent site specificity, and scalability, enabling the synthesis of diarylmethane amides and dibenzoazepines. The protocol allows for one-pot diagonal dibenzylation of dianilides, creating valuable precursors for pharmaceutically active compounds and addressing limitations in current direct C–H activation methodologies.

中文翻译：

---

正芳基酰胺的位点选择性硼定向邻位苄基化反应：获得结构多样化的二苯并氮卓类药物


我们提出了一种用于 N-芳基酰胺邻位苄基化的高选择性方案。该方法条件温和，位点特异性好，可扩展性强，能够合成二芳基甲烷酰胺和二苯并氮杂吡啶。该方案允许二苯胺类的一锅对角线二苄基化，为药物活性化合物创造有价值的前体，并解决当前直接 C-H 活化方法的局限性。