通过串联亚硝化/有氧氧化 C-N 键形成高效合成喹喔啉-N-氧化物。

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

机构信息

Faculty of Pharmaceutical Sciences, Mukogawa Women's University, 11-68 Koshien Kyubancho, Nishinomiya 663-8179, Hyogo, Japan.

出版信息

Org Lett. 2011 Dec 2;13(23):6280-3. doi: 10.1021/ol202760c. Epub 2011 Nov 8.

DOI:10.1021/ol202760c

PMID:22066966

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.

摘要

一种从氰乙酰胺构建喹喔啉酮-N-氧化物的有效方法已经被开发出来。这种转化可以使用廉价的试剂和分子氧在温和条件下实现，因此为含有喹喔啉酮的药物如阿他喹莫和奥帕伐林提供了一条实用的途径。