Journal
TETRAHEDRON LETTERS
Volume 58, Issue 30, Pages 2877-2880Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2017.05.050
Keywords
Iodine-catalyzed; Formylation; Indole; 3-Formylindole; Hexamethylenetetramine
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Funding
- National High Technology Research and Development Program of China [2007AA02Z301]
- Natural Science Foundation of Jiangsu Province [BK20141257]
- Natural Science Foundation of Yancheng Teachers University [09YCKL021, 14YCKL001]
- Fundamental Research Funds for the Central University [WY111307]
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An efficient iodine-catalyzed chemoselective 3-formylation of free (N-H) and N-substituted indoles was achieved by using hexamethylenetetramine (HMTA) in the presence of activated carbon under air atmosphere. This new method could provide 3-formylindoles in moderate to excellent yields with fairly short reaction times. Moreover, this catalytic formylation of indoles procedure can be applied to gram-scale synthesis. (C) 2017 Elsevier Ltd. All rights reserved.
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