Highly efficient synthesis of quinoxalinone-N-oxide via tandem nitrosation/aerobic oxidative C-N bond formation

  • Org Lett. 2011 Dec 2;13(23):6280-3. doi: 10.1021/ol202760c.
Yusuke Kobayashi  1 ,  Mami Kuroda ,  Natsuki Toba ,  Mari Okada ,  Rie Tanaka ,  Tetsutaro Kimachi
Affiliations
  • 1. Faculty of Pharmaceutical Sciences, Mukogawa Women's University, 11-68 Koshien Kyubancho, Nishinomiya 663-8179, Hyogo, Japan. [email protected]
PMID: 22066966 DOI: 10.1021/ol202760c
Abstract

An efficient method for constructing quinoxalinone-N-oxides from cyanoacetanilides has been developed. This transformation can be achieved using inexpensive reagents and molecular oxygen under mild conditions, thus offering a practical pathway to quinoxalinone-containing pharmaceuticals such as ataquimast and opaviraline.

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