2-取代-2,3-二氢-4(1H)-喹唑啉酮衍生物合成方法  

Synthetic Method for 2-Substituted-2,3-Dihydro-4(1H)-Quinazolinones Derivatives

作　　者：王敏[1] 高晶晶[1] 向刚伟[2] 王磊[1] 

机构地区：[1]渤海大学化学化工与食品安全学院,辽宁锦州121000 [2]中国石油四川石化有限责任公司生产一部,四川成都611930

出　　处：《石油化工高等学校学报》2011年第3期13-16,21,共5页Journal of Petrochemical Universities

基　　金：辽宁省博士科研启动基金资助项目(2009A033)

摘　　要：在氯化铝催化作用下,以水为溶剂,将2-氨基苯甲酰胺和醛/酮室温研磨后,温度为60℃时加热反应,可有效环化合成一系列2-取代-2,3-二氢-4(1H)-喹唑啉酮衍生物。比较不同催化剂的催化活性,考察了催化剂和水的用量对收率的影响。结果表明,在n(2-氨基苯甲酰胺)/n(醛/酮)=1∶1,催化剂摩尔分数为1%,水体积2 mL的反应条件下,实验结果最好。产品结构经IR,1H-NMR,质谱,元素分析进行表征,并提出可能的催化反应机理。A series of 2-substituted-2,3-dihydro-4（1H）-quinazolinones derivatives were synthesized efficiently by the cyclocondensation of 2-anthranilamide with an aldehyde or ketone in the presence of aluminum chloride in water at 60 ℃ after grinding at room temperature. The catalytic activity of different catalysts was compared. The effects of the amount of catalyst and the amount of solvent on the yields were investigated. The results show that the best reaction results could be obtained when the molar ratio of 2-anthranilamide to an aldehyde or ketone is 1 ： 1, the amount of catalyst is 1% （based on the mole of reactant）, and water is 2 mL. The structures of products were characterized by IR, ^1H- NMR, mass spectrum and elemental analysis. The probable catalytic mechanism for the reaction was proposed.

关 键 词：2 3-二氢-4(1H)-喹唑啉酮 氯化铝 2-氨基苯甲酰胺 醛 酮 

分 类 号：TQ215[化学工程—有机化工] O626.41[理学—有机化学]