Radical Aminomethylation of Imines

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• 作者：Shintaro Fujii ; Takehito Konishi ; Yusuke Matsumoto ; Yousuke Yamaoka ; Kiyosei Takasu ; Ken-ichi Yamada
• 刊名：Journal of Organic Chemistry
• 出版年：2014
• 出版时间：September 5, 2014
• 年：2014
• 卷：79
• 期：17
• 页码：8128-8133
• 全文大小：318K
• ISSN：1520-6904

文摘

Taking advantage of the high level of performance of N-alkoxycarbonyl-imines, we achieved the first example of addition of the aminomethyl radical to imine. The reaction efficiency depended on the structure of the radical precursor, whether it is an iodide or a xanthate, and an electron-withdrawing group on the nitrogen atom of the radical. This reaction allows direct introduction of an N-substituted aminomethyl group onto imine to provide 1,2-diamine as well as the short-step synthesis of ICI-199,441.