A practical method for preparation of 4-hydroxyquinolinone esters
A practical method for preparation of 4-hydroxyquinolinone esters
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DOI：
10.1021/jo071200x
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发表时间：
2007-08-31
影响因子：
3.6
通讯作者：
Yasuda, Nobuyoshi
中科院分区：
文献类型：
--
作者：
Beutner, Gregory L.;Kuethe, Jeffrey T.;Yasuda, Nobuyoshi
4-羟基喹啉酮酯是许多药剂的常见基元。存在几种制备这些化合物的方法，通常涉及使用氢化钠，这引起了显著的安全问题并限制了它们在大规模合成中的应用。本文介绍了一种实用、安全和通用的方法，即采用二异丙基乙胺和叔丁醇钠的组合。这允许以良好的产率合成4-羟基喹啉酮酯和酰胺。
4-hydroxyquinolinone esters are a common motif for many medicinal agents. Several methods exist for preparation of these compounds, generally involving the use of sodium hydride, which raises significant safety issues and limits their application to large-scale synthesis. In this note a practical, safe, and general method that employs a combination of diisopropylethylamine and sodium tert-butoxide is described. This allows for the synthesis of 4-hydroxyquinolinone esters and amides in good yields.