Organic and Medicinal Chemistry Division, CSIR-Indian Institute of Chemical Biology , 4 Raja S. C. Mullick Road, Jadavpur, Kolkata-700032, West Bengal, India.
J Org Chem. 2016 May 20;81(10):4295-303. doi: 10.1021/acs.joc.6b00659. Epub 2016 May 11.
Despite significant progress, copper-catalyzed/mediated C-H amination reactions with electron-rich anilines remain an unsolved problem due to catalyst deactivation and deleterious side reactions. Herein, we report a copper(II)-mediated C(sp(2))-H amination of benzamides with electronically neutral or electron-rich anilines. A dramatic influence of silver(I) and tetrabutylammonium bromide was observed on the reaction outcome. The present protocol also demonstrates the synthesis of a number of nonsteroidal anti-inflammatory drugs.
尽管取得了显著进展，但由于催化剂失活和有害副反应的存在，铜催化/介导的富电子苯胺 C-H 胺化反应仍然是一个未解决的问题。在此，我们报道了铜(II)介导的苯甲酰胺与电子中性或富电子苯胺的 C(sp(2))-H 胺化反应。银(I)和四丁基溴化铵对反应结果有显著影响。本方案还展示了一些非甾体抗炎药的合成。
