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Issue 3, 2019
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Eco-friendly decarboxylative cyclization in water: practical access to the anti-malarial 4-quinolones

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Abstract

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.

Graphical abstract: Eco-friendly decarboxylative cyclization in water: practical access to the anti-malarial 4-quinolones

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Article information


Submitted
15 Nov 2018
Accepted
08 Jan 2019
First published
09 Jan 2019

Green Chem., 2019,21, 478-482
Article type
Communication

Eco-friendly decarboxylative cyclization in water: practical access to the anti-malarial 4-quinolones

Y. Ma, Y. Zhu, D. Zhang, Y. Meng, T. Tang, K. Wang, J. Ma, J. Wang and P. Sun, Green Chem., 2019, 21, 478
DOI: 10.1039/C8GC03570A

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