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Palladium-catalyzed intramolecular aerobic C-H amination of enamines for the synthesis of 2-trifluoromethylindoles
Tetrahedron ( IF 2.1 ) Pub Date : 2017-12-29 , DOI: 10.1016/j.tet.2017.12.047
Feng Wei , Xiao-Qin Shen , Jing-Jing Chu , Bo-Lun Hu , Xing-Guo Zhang

A new palladium-catalyzed C-H amination of aryl enamines for the synthesis of trifluoromethylated indoles is established. The attractive features of this transformation are the use of atom-economical O2 as the oxidant and easily prepared enamines as substrates. A variety of pharmaceutically important 2-trifluoromethyl indoles can be targeted in moderate to good yields with good functional compatibility.



中文翻译:

钯催化的烯胺的分子内需氧CH胺化反应合成2-三氟甲基吲哚

建立了一种新的钯催化的芳基烯胺的CH胺化反应,用于合成三氟甲基化的吲哚。该转变的吸引人的特征是使用原子经济的O 2作为氧化剂,并容易制备烯胺作为底物。各种药学上重要的2-三氟甲基吲哚都可以以中等至良好的收率和良好的功能相容性进行靶向。

更新日期:2017-12-29
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