期刊
ORGANIC CHEMISTRY FRONTIERS
卷 5, 期 21, 页码 3133-3137出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8qo00932e
关键词
-
资金
- Department of Science and Technology (DST) INSPIRE faculty award [DST/INSPIRE/04/2016/000414]
Rhodium(iii) catalyzed C-H alkylation at the C2-position of indole with -trifluoromethyl-,-unsaturated ketones is described. The reactions proceed efficiently with low catalyst loading and a broad range of substrates with excellent functional group compatibility. The scale-up reaction was successfully achieved with 0.5 mol% of the Rh catalyst without significant decrease in the yield. This protocol provides direct access to pharmaceutically important indole derivatives containing a stereogenic carbon center bearing a CF3 functionality at the C2-position.
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