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

doi:10.6023/cjoc201310022

Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (3): 526-536.DOI: 10.6023/cjoc201310022 Previous Articles Next Articles

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2,3-二取代喹唑啉-4（3H）-酮化合物的合成及生物活性研究

欧俊军^a, 刘克昌^a, 王毅^a, 张浩^a, 刘瑞全^a, 李奇博^a, 汪清民^b, 李永强^b, 芮昌辉^c, 刘尚钟^a

a 中国农业大学理学院应用化学系北京 100193;
b 南开大学元素有机化学国家重点实验室天津 300071;
c 中国农业科学研究院植物保护研究所北京 100193

收稿日期:2013-10-16 修回日期:2013-11-13 发布日期:2013-11-21
通讯作者: 刘尚钟 E-mail:shangzho@cau.edu.cn
基金资助:
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）和绿色生态农药的研发及产业化（No. 2011BAE06B03）资助项目.

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

Ou Junjun^a, Liu Kechang^a, Wang Yi^a, Zhang Hao^a, Liu Ruiquan^a, Li Qibo^a, Wang Qingmin^b, Li Yongqiang^b, Rui Changhui^c, Liu Shangzhong^a

a Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193;
b State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071;
c Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing 100193

Received:2013-10-16 Revised:2013-11-13 Published:2013-11-21
Supported by:
Project supported by the National Natural Science Foundation of China (Nos. 20972186, 21172256), the National Basic Research Program of China (No. 2010CB126104) and the Project of Green Pesticide Research, Development and Industrialization (No. 2011BAE06B03).

In this research, a series of new 2,3-disubstituted quinazolin-4(3H)-ones were designed and synthesized. The influence 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 graminis) in vivo at a concentration of 200 mg/L.

Key words: 2,3-disubstituted quinazolin-4(3H)-ones, synthesis, bioactivitys, crystal structure

Cite this article

Ou Junjun, Liu Kechang, Wang Yi, Zhang Hao, Liu Ruiquan, Li Qibo, Wang Qingmin, Li Yongqiang, Rui Changhui, Liu Shangzhong. Synthesis and Bioactivity Studies of 2,3-Disubstituted Quinazolin-4(3H)-one[J]. Chin. J. Org. Chem., 2014, 34(3): 526-536.

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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

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