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 

机构地区：[1]Shanghai Key Lab of Chemistry Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China [2]Shanghai Collaborative Innovation Center for Biomanufacturing Technology, Shanghai 200237, China

出　　处：《Chinese Chemical Letters》2016年第1期7-10,共4页中国化学快报（英文版）

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

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.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.

关 键 词：NEONICOTINOIDS Tetrahydroimidazo[1 2-a]pyridin-5（1H） ONE Configuration Insecticidal activity 

分 类 号：TQ453.2[化学工程—农药化工]