Regioselective and Direct Azidation of Anilines via Cu(II)-Catalyzed C-H Functionalization in Water
Regioselective and Direct Azidation of Anilines via Cu(II)-Catalyzed C-H Functionalization in Water
复制标题
水中 Cu(II) 催化的 C-H 官能化对苯胺进行区域选择性和直接叠氮化
DOI：
10.1021/acs.joc.7b01594
复制
发表时间：
2017-10-20
影响因子：
3.6
通讯作者：
Zhu, Qing
中科院分区：
文献类型：
--
作者：
Fang, Hongli;Dou, Yandong;Zhu, Qing
本文报道了在水介质中铜(II)催化的芳香胺C-H官能化中心选择性氮化反应的第一个例子。在我们的策略中，使用了一种温和的试剂。以过氧化氢为氧化剂，叠氮钠为叠氮试剂。该方法也可用于芳香胺类药物的后期功能化。此外，我们还发现利用该催化体系可以有效地进行芳香胺邻位的溴化或碘化反应。
We report herein the first example of Cu(II)-catalyzed site selective azidation of aromatic amines via C-H functionalization in aqueous media. In our strategy, a mild reagent was utilized. H2O2 served as the oxidant, and sodium azide was used as the azidation reagent. This method could also be applied to late-stage functionalization of drugs that possess an aromatic amine moiety. In addition, we found that bromination or iodination on the ortho-position of aromatic amines could occur efficiently using this catalytic system.