2,3-二取代喹唑啉-4(3H)-酮化合物的合成及生物活性研究  

Synthesis and Bioactivity Studies of 2,3-Disubstituted Quinazolin-4(3H)-one

作　　者：欧俊军[1] 刘克昌[1] 王毅[1] 张浩[1] 刘瑞全[1] 李奇博 汪清民[2] 李永强[2] 芮昌辉[3] 刘尚钟[1] 

机构地区：[1]中国农业大学理学院应用化学系,北京100193 [2]南开大学元素有机化学国家重点实验室,天津300071 [3]中国农业科学研究院植物保护研究所,北京100193

出　　处：《有机化学》2014年第3期526-536,共11页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.20972186;21172256);国家重点基础研究发展计划(No.2010CB126104);绿色生态农药的研发及产业化(No.2011BAE06B03)资助项目~~

摘　　要：设计合成了一系列2,3-二取代喹唑啉-4(3H)-酮化合物,并研究了常用无机干燥剂对目标化合物合成的影响,发现无水硫酸镁能够促进2,3-二取代喹唑啉-4(3H)-酮化合物的形成.所有化合物通过核磁共振氢谱、核磁共振碳谱、高分辨质谱等方法进行结构表征,并首次报道了6-氯-3-苄氨基-2-新戊基-8-甲基喹唑啉-4(3H)-酮的单晶结构.通过生物活性测试发现部分化合物在200 mg/L浓度下对小麦白粉病(Blumeria graminis)具有较好的活体防效.In this research, a series of new 2,3-disubstituted quinazolin-4（3H）-ones were designed and synthesized. The in- fluence of common drying agents on the formation of 2,3-disubstituted quinazolin-4（3H）-ones was investigated and firstly reported. It is found that the anhydrous magnesium sulfate can increase the yield of 2,3-disubstituted quinazolin-4（3H）-ones significantly. The structures of new compounds were all confirmed via 1H NMR, 13C NMR and HRMS. At the same time, the crystal structure of 3-（benzylamino）-6-chloro-8-methyl-2-neopentyl-quinazolin-4（3H）-one was firstly reported. The results of bioactivity assay showed that some of these new compounds have some control effects on wheat powdery mildew （Blumeria grarninis） in vivo at a concentration of 200 mg/L.

关 键 词：2  3-二取代喹唑啉-4(3H)-酮 合成 生物活性 单晶结构 

分 类 号：TQ460.1[化学工程—制药化工]