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Issue 24, 2014
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Metal-free (Boc)2O-mediated C4-selective direct indolation of pyridines using TEMPO

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Abstract

Direct metal-free C-4-selective indolation of pyridines is achieved for the first time using TEMPO and (Boc)2O. A variety of substituents on both indoles and pyridines are tolerated to give 3-(pyridin-4-yl)-1H-indole derivatives in moderate to excellent yields. This finding provides a novel approach for developing metal-free C–H functionalization of pyridines.

Graphical abstract: Metal-free (Boc)2O-mediated C4-selective direct indolation of pyridines using TEMPO

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Publication details

The article was received on 16 Feb 2014, accepted on 21 Apr 2014 and first published on 22 Apr 2014


Article type: Paper
DOI: 10.1039/C4OB00356J
Author version available: Download Author version (PDF)
Citation: Org. Biomol. Chem., 2014,12, 4252-4259
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    Metal-free (Boc)2O-mediated C4-selective direct indolation of pyridines using TEMPO

    W. Qin, J. Zhu, Y. Kong, Y. Bao, Z. Chen and L. Liu, Org. Biomol. Chem., 2014, 12, 4252
    DOI: 10.1039/C4OB00356J

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