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J Org Chem. 2016 Sep 2;81(17):7717-24. doi: 10.1021/acs.joc.6b01415. Epub 2016 Aug 9.

Copper-Catalyzed N-Arylation of 2-Pyridones Employing Diaryliodonium Salts at Room Temperature.

Author information

1
Department of Chemistry and Nano Science, Ewha Womans University , Seoul 120-750, South Korea.

Abstract

A new and mild synthetic approach for the N-arylation of 2-pyridones with diaryliodonium salts has been developed. Most reactions proceed readily at room temperature in the presence of 10 mol % of copper chloride. As a result, a wide range of N-arylpyridine-2-ones were synthesized in yields of 23% to 99%. With this method, an antifibrotic drug, Pirfenidone, was successfully synthesized in 99% yield within 30 min at room temperature.

PMID:
27484240
DOI:
10.1021/acs.joc.6b01415
[Indexed for MEDLINE]

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