NCS-Mediated Direct C(sp3)-H Oxygenation of 2-Methylindoles Using Water as the Oxygen Source
Fan Zhang1, Yuling Luo2, Xiaoyi Liu1
1School of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, China.
Abstract:
In continuation of our research interest in the green oxidation of indoles, we further explore the direct oxidation of 2-methylindoles to 2-formyl indoles promoted by NCS and associated with H2O as the oxygen source. This methodology was demonstrated to be a robust protocol consisting of chlorination, SN2', and oxidation processes, and presents a reasonably broad substrate scope and excellent functional group tolerance, thus enabling the preparation of high added-value versatile building blocks susceptible to further functionalization.
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