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研究以二种基于磺酸基官能团的Brφnsted酸性功能化离子液体:1-(4-磺酸基)苄基-3-甲基咪唑硫酸氢盐(a),N-(4-磺酸基)苄基吡啶硫酸氢根盐(b)作为反应介质与催化剂,2-氨基苯甲酸、原甲酸酯或甲酸、芳香胺或脂肪胺三组分为原料,在微波辐射下实现了3-取代-4(3H)-喹唑啉酮的一锅法快速合成.离子液体加入量10 mol%,反应时间4~6 min,目标化合物产率74%~94%.离子液体可循环使用3次,催化活性基本保持不变.此合成方法通用性强,3-位可引入芳基或烷基取代基,取代基电性效应小,拉电子取代基底物也可顺利反应.另外,反应可直接以85%甲酸作为C-2引入单元,目标化合物产率72%~91%.
Two types of Brønsted acidic functional ionic liquids based on sulfonic acid functional groups were studied: 1- (4-sulfonato) benzyl-3-methylimidazolium hydrogensulfate (a) Benzylpyridinium hydrogen sulfate salt (b) as reaction medium and catalyst, 2-aminobenzoic acid, orthoformate or formic acid, aromatic amine or aliphatic amine as raw materials, under microwave irradiation to achieve a 3-substituted - 4 (3H) -quinazolinone was synthesized by one-pot method.The ionic liquid was added in an amount of 10 mol% and the reaction time was 4 ~ 6 min.The yield of target compound was 74% ~ 94% Activity basically unchanged. This synthetic method is versatile, 3-position can be introduced aryl or alkyl substituents, the substituent electrical effect is small, pull the electron-withdrawing substrate can also be smooth response. In addition, the reaction can be directly 85 % Formic acid as C-2 introduction unit, the target compound yield 72% ~ 91%.