一锅法合成吡唑并[3,4-b]喹啉酮类化合物
One-pot synthesis of pyrazolo[3,4-b]quinolinone compounds
刘昭文 1洪朝国 1彭凉谦 1陶佳怡 1王榆榕 1周鹏辉 1曹一帆 1杨凯1
作者信息
- 1. 赣南医科大学药学院,江西 赣州 341000
- 折叠
摘要
目的:探究吡唑并[3,4-b]喹啉酮类化合物{Pyrazolo[3,4-b]quinolinone compounds,PQO}绿色、高效的合成方法.方法:以5-氨基-3-甲基-1-苯基吡唑、1,3-环己二酮类和苯乙二醛类水合物为原料,通过一锅法3组分反应合成PQO.结果:获得PQO的最佳合成工艺为EtOH/H2O(V=1/1)为溶剂,反应温度50℃,反应时间1.5 h,且目标化合物经 1H NMR、13C NMR和HR-MS确证.结论:该方法具有操作简单、产率高、高原子经济性等特点,在新药设计与合成、组合化学和天然产物合成中具有潜在的应用价值.
Abstract
Objective:To explore green and efficient synthesis methods for pyrazolo[3,4-b]quinolinone compounds(PQO).Methods:PQO were obtained by arylglyoxals,1,3-cyclohexanediones,and 5-amino-3-methyl-1-phenylpyrazole as raw materials via a one-pot three-component reaction.Results:The optimal synthetic process for obtaining PQO was EtOH/H2O(V=1/1)as the solvent,the reaction temperature 50℃,and the reaction time 1.5 hours.The target compounds were confirmed by 1H NMR,13C NMR,and HR-MS.Conclusion:The reaction is characterized by simple operation,high yield,and high atom economy,with potential applications in the design and synthesis of new drugs,combinatorial chemistry,and the synthesis of natural products.
关键词
吡唑并[3,4-b]喹啉酮/有机合成/一锅法Key words
Pyrazolo[3,4-b]quinolinone/Organic synthesis/One-pot引用本文复制引用
出版年
2024
国家科技期刊平台
NSTL
万方数据