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Org Lett. 2013 Oct 18;15(20):5286-9. doi: 10.1021/ol402515s. Epub 2013 Oct 7.

Ru(II)-catalyzed ortho-C-H amination of arenes and heteroarenes at room temperature.

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  • 1State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 345 Lingling Road, Shanghai 200032, China, and Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.


The Ru(II)-catalyzed ortho-C-H amination directed by a weakly coordinating amide auxiliary with O-benzoyl hydroxylamines at room temperature has been achieved. This reaction is compatible with heterocycles including pyrazole, thiophene, benzothiophene, furan, benzofuran, and indole.

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