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Improved Protocol for Indoline Synthesis via Palladium-Catalyzed Intramolecular C(sp2)-H Amination

Gang He, Chengxi Lu, Yingsheng Zhao, William A. Nack and Gong Chen*

*Department of Chemistry, The Pennsylvania State University, University Park, Pennsylvania 16802, United States, Email:

G. He, C. Lu, Y. Zhao, W. A. Nack, G. Chen, Org. Lett., 2012, 14, 2936-2939.

DOI: 10.1021/ol301352v


An efficient synthesis of indoline compounds from picolinamide (PA)-protected β-arylethylamine substrates via palladium-catalyzed intramolecular amination of ortho-C(sp2)-H bonds features high efficiency, low catalyst loadings, mild operating conditions, and the use of inexpensive reagents.

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Key Words

Indolines, Iodosobenzene Diacetate

ID: J54-Y2012-1860