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Copper mediated C–H amination with oximes: en route to primary anilines†
Chemical Science ( IF 8.4 ) Pub Date : 2018-05-14 00:00:00 , DOI: 10.1039/c8sc01256c
Lin-Lin Xu 1, 2, 3, 4, 5 , Xing Wang 4, 6, 7, 8, 9 , Biao Ma 4, 6, 7, 8, 9 , Ming-Xing Yin 4, 6, 7, 8, 9 , Hai-Xia Lin 1, 2, 3, 4, 5 , Hui-Xiong Dai 4, 6, 7, 8, 9 , Jin-Quan Yu 1, 10, 11, 12
Affiliation  

Here we report an efficient Cu(I)-mediated C–H amination reaction with oximes as amino donors to introduce NH2 groups directly. Various strongly coordinating heterocycles including quinoline, pyrimidine, pyrazine, pyrazole and triazole were tolerated well. The potential utility was further demonstrated in a late-stage modification of telmisartan (an antagonist for the angiotensin II receptor).

中文翻译:

肟介导的铜介导的C–H胺化反应:向初级苯胺的过程中

在这里,我们报告了一种以肟为氨基供体的Cu(I)介导的CH氨基化反应,可直接引入NH 2基团。包括喹啉,嘧啶,吡嗪,吡唑和三唑在内的各种强配位杂环均具有良好的耐受性。在替米沙坦(血管紧张素II受体的拮抗剂)的后期修饰中进一步证明了这种潜在的效用。
更新日期:2018-05-14
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