铱催化苯胺与磺酰叠氮的直接C-H酰胺化反应：简便合成1,2-二氨基苯
Iridium-catalyzed direct C-H amidation of anilines with sulfonyl azides: easy access to 1,2-diaminobenzenes.
作者信息
Wang Lianhui, Yang Zi, Yang Mengqi, Zhang Rongyi, Kuai Changsheng, Cui Xiuling
机构信息
Engineering Research Center of Molecular Medicine, Ministry of Education, Key Laboratory of Xiamen Marine and Gene Drugs, Institute of Molecular Medicine and School of Biomedical Sciences, Huaqiao University, Xiamen, 361021, Fujian, China.
出版信息
Org Biomol Chem. 2017 Oct 11;15(39):8302-8307. doi: 10.1039/c7ob01899a.
An Ir(iii)-catalyzed regioselective C-H amidation of anilines with sulfonyl azides is described. The developed protocol has good compatibility with diverse functional groups, efficiently providing the monoamidated products with good to excellent yields under mild reaction conditions. Furthermore, the 2-pyrimidyl and sulfonyl moieties in the amidated products can readily be removed, offering the synthetically useful 1,2-diaminobenzene scaffold.
描述了一种铱（III）催化的苯胺与磺酰叠氮的区域选择性C-H酰胺化反应。所开发的方法与多种官能团具有良好的兼容性，在温和的反应条件下能高效地提供单酰胺化产物，产率良好至优异。此外，酰胺化产物中的2-嘧啶基和磺酰基部分可容易地去除，从而提供具有合成用途的1,2-二氨基苯骨架。
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