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

Seo Hee Jung, Dan Bi Sung, Cho Hee Park, Won Suk Kim

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

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.

Original languageEnglish
Pages (from-to)7717-7724
Number of pages8
JournalJournal of Organic Chemistry
Volume81
Issue number17
DOIs
StatePublished - 2 Sep 2016

Bibliographical note

Funding Information:
This research was supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF) (NRF-015R1A1A1A05001334) and the New & Renewable Energy of the Korea Institute of Energy Technology Evaluation and Planning (KETEP) grant (No.20133030000210)

Publisher Copyright:
© 2016 American Chemical Society.

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