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In conclusions, we described a simple and practical method
for the C3-formylation of free (N–H) and N-substituted indoles
using HMTA as the carbon source. This procedure was
conducted under air using molecular iodine as the catalyst,
avoiding the use of harmful transition-metal catalyst and
peroxide oxidant. 3-Formylindoles with both electron-donating
and electron-withdrawing groups were obtained in moderate to
excellent yields with fairly short reaction times. The protocol
might be useful for the synthesis of indoles bearing acid- or base-
sensitive functional groups. Moreover, this procedure can also be
applied to gram-scale synthesis and represents an exceedingly
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Acknowledgments
We thank the 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) and the Fundamental Research
Funds for the Central University (WY111307) for the generous
financial support.
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Supplementary data
Supplementary data associated with this letter can be found in
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