Synthesis and insecticidal evaluation of tetrahydroimidazo[1,2-a]pyridin-5(1H)-one derivatives

作     者：Xuan-Qi Liu Ya-Qin Liu Xu-Sheng Shao Zhi-Ping Xu Xiao-Yong Xu Zhong Li 

作者机构：Shanghai Key Lab of Chemistry Biology School of Pharmacy East China University of Science and Technology Shanghai 200237 China Shanghai Collaborative Innovation Center for Biomanufacturing Technology Shanghai 200237 China 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2016年第27卷第1期

页      面：7-10页

核心收录：

学科分类：090403[农学-农药学(可授农学、理学学位）] 09[农学] 0904[农学-植物保护] 

基　　金：financial supported by National High Technology Research Development Program of China (863 Program, No. 2011AA10A207) National Natural Science Foundation of China (Nos. 21472046, 21372079) Shanghai Pujiang Program (No. 14PJD012) the Fundamental Research Funds for the Central Universities (No. 222201414015) partly supported by Australia DC Foundation 

主　　题：Neonicotinoids Tetrahydroimidazo[1,2-a]pyridin-5(1H) one Configuration Insecticidal activity 

摘      要：A series of novel tetrahydroimidazo[1,2-a]pyridine-5（1H）-one derivatives containing a electronegative pharmacophore（=CNO_2） were synthesized via practical aza-ene reaction and characterized by ~1H NMR,^（13）C NMR,^（19）F NMR and HRMS. Preliminary bioassays showed that some of the target compounds exhibited good insecticidal activity against brown planthopper（Nilaparvata lugens） and cowpea aphids（Aphis craccivora） at 500 mg L^（-1）. Among them, compound 11 h was active against brown planthopper at100 mg L^（-1）. The insecticidal activities varied significantly depending on the types and patterns of the substituents, which provided guidance for further investigation on structure modifications.