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Rapid and Efficient Microwave-Assisted Amination of Electron-Rich Aryl Halides without a Transition-Metal Catalyst

Lei Shi, Min Wang, Chun-An Fan, Fu-Min Zhang and Yong-Qiang Tu*

*Department of Chemistry & State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, P. R. China, Email:

L. Shi, M. Wang, C.-A. Fan, F.-M. Zhang, Y.-Q. Tu, Org. Lett., 2003, 5, 3515-3517.

DOI: 10.1021/ol0353868


An efficient, transition metal catalyst-free amination of aryl halides under microwave irradiation is a particularly powerful method for the coupling of electron-rich aryl halides with various amines. Meta-substituted anilines have been prepared from ortho- or para-substituted phenylhalides. A mechanism via a benzyne intermediate has been proposed.

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Key Words

Microwave Synthesis, Arylamines

ID: J54-Y2003-570