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Iodine-catalyzed C3-formylation of indoles using hexamethylenetetramine and air |
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| Authors: | Qing-Dong Wang Jin-Ming Yang Dong Fang Jiangmeng Ren Bu-Bing Zeng |
| Institution: | 1. School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China;2. School of Pharmacy, Yancheng Teachers University, Yancheng, Jiangsu 224051, PR China |
| Abstract: | 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. |
| Keywords: | Iodine-catalyzed Formylation Indole 3-Formylindole Hexamethylenetetramine |
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