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A mild inter- and intramolecular amination of aryl halides with a combination of CuI and CsOAc |
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| Authors: | Tetsuji Kubo Ken Yamada Hidetoshi Tokuyama Tohru Fukuyama |
| Affiliation: | a Graduate School of Pharmaceutical Sciences, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan b Graduate School of Pharmaceutical Sciences, Tohoku University, 6-3 Aramaki, Aoba-ku, Sendai 980-8578, Japan |
| Abstract: | A unique combination of CuI and CsOAc was found to catalyze aryl amination under mild conditions. The reaction takes place at room temperature or at 90 °C with broad functional group compatibility. The intramolecular reaction was able to form five-, six-, and seven-membered rings with various protecting groups on the nitrogen atom. The scope of the intermolecular amination, as well as its applications to unsymmetrical N,N′-dialkylated phenylenediamines, was investigated. |
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