摘要/Abstract

报道了温和条件下, 过硫酸铵促进喹喔啉-2(1H)-酮与CF₃SO₂Na三氟甲基化制备3-三氟甲基喹喔啉-2(1H)-酮类的反应, 开发了一种绿色、高效制备3-三氟甲基喹喔啉-2(1H)-酮衍生物的方法. 该方法对不同取代的喹喔啉-2(1H)-酮衍生物具有较好的适用性, 均以较高的产率得到相应的目标产物. 与已有方法相比, 本方法具有底物适用范围广、产率高、实验操作简便等优点, 为3-三氟甲基喹喔啉-2(1H)-酮的制备提供了有效的路径.
关键词: 过硫酸铵, 三氟甲基化, 喹喔啉-2(1H)-酮衍生物, 三氟甲基亚磺酸钠
A green and efficient method for the synthesis of 3-trifluoromethylquinoxalin-2(1H)-ones via direct trifluoromethylation of quinoxalin-2(1H)-ones with CF₃SO₂Na promoted by ammonium persulfate ((NH₄)₂S₂O₈) under mild conditions has been developed. This process is scalable and tolerates a wide spectrum of quinoxalin-2(1H)-one derivatives to deliver corresponding products in good to excellent yields. Comparing to the previous methods, this strategy has the advantages of wide functional groups tolerance, high yield and simple operation, providing an efficient synthetic approach to 3-trifluoromethyl- quinoxalin-2(1H)-ones.
Key words: ammonium persulfate, trifluoromethylation, quinoxalin-2(1H)-one derivatives, CF₃SO₂Na


PDF全文下载地址:

点我下载PDF