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

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.