位点选择性硼导向的α-芳基酰胺的苄基化反应：构建结构多样的二苯并氮杂卓类化合物
Site Selective Boron Directed Benzylation of -Aryl Amides: Access to Structurally Diversified Dibenzoazepines.
作者信息
Shinde Ganesh H, Castlind Hugo, Ghotekar Ganesh S, Amombo Noa Francoise M, Öhrström Lars, Sundén Henrik
机构信息
Department of Chemistry and Molecular Biology, University of Gothenburg, SE-41296 Gothenburg, Sweden.
Department of Chemistry and Chemical Engineering, Chalmers University of Technology, SE-41296 Gothenburg, Sweden.
出版信息
Org Lett. 2025 Jan 10;27(1):207-211. doi: 10.1021/acs.orglett.4c04196. Epub 2024 Dec 17.
We present a highly selective protocol for the benzylation of -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.
我们提出了一种用于芳基酰胺苄基化的高选择性方案。该方法条件温和、位点特异性优异且具有可扩展性，能够合成二芳基甲烷酰胺和二苯并氮杂卓。该方案允许二酰胺的一锅对角二苄基化反应，为药物活性化合物创造了有价值的前体，并解决了当前直接C-H活化方法中的局限性。
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