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: guc11psu.edu
G. He, C. Lu, Y. Zhao, W. A. Nack, G. Chen, Org. Lett., 2012, 14, 2936-2939.
DOI: 10.1021/ol301352v (free Supporting Information)
An efficient synthesis of indolines 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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