4.8 Article

Rapid and efficient microwave-assisted amination of electron-rich aryl halides without a transition-metal catalyst

Journal

ORGANIC LETTERS
Volume 5, Issue 19, Pages 3515-3517

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol0353868

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[GRAPHICS] A rapid and direct amination of aryl halides has been developed in good to high yields under microwave irradiation without a transition-metal catalyst. This reaction is a particularly powerful method for the coupling of electron-rich aryl halides with various amines. In some cases, the excellent regioselectivity could be observed, which facilitated the preparation of meta-substituted anilines from ortho- or para-substituted phenylhalides. In addition, a mechanism via the interesting benzyne intermediate has been proposed.

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