期刊
GREEN CHEMISTRY
卷 21, 期 3, 页码 478-482出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8gc03570a
关键词
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资金
- National Natural Science Foundation of China [21702235, 81841001, 81641002]
- Fundamental Research Funds for the Central Public Welfare Research Institutes [ZZ10-024, ZXKT17053]
- Major National Science and Technology Program of China [2017ZX09101002-001-001]
An environmentally benign decarboxylative cyclization in water has been developed to synthesize 4-quinolones from readily available isatoic anhydrides and 1,3-dicarbonyl compounds. Isatins are also compatible for the reaction to generate 4-quinolones in the presence of TBHP in DMSO. This protocol provides excellent yields under mild conditions for a broad scope of 4-quinolones, and has good functional group tolerance. Only un-harmful carbon dioxide and water are released in this procedure. Moreover, the newly synthesized products have also been selected for anti-malarial examination against the chloroquine drug-sensitive Plasmodium falciparum 3D7 strain. 3u is found to display excellent anti-malarial activity with an IC50 value of 33 nM.
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