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弥拜霉素类似物的合成、表征和杀虫活性研究
引用本文:徐小军,赖声洪,季明华,朱国念,赵金浩.弥拜霉素类似物的合成、表征和杀虫活性研究[J].有机化学,2012,32(6):1084-1092.
作者姓名:徐小军  赖声洪  季明华  朱国念  赵金浩
作者单位:1. 浙江大学农药与环境毒理研究所 农业部作物病虫分子生物学重点开放实验室 杭州310029;浙江工业大学药学院 杭州310014
2. 浙江大学农药与环境毒理研究所 农业部作物病虫分子生物学重点开放实验室 杭州310029
3. 浙江理工大学科学研究所 杭州310032
摘    要:以弥拜霉素类似物依维菌素为原料,根据类同合成法和亚结构连接法原理,对依维菌素进行脱糖,再与相应的酰氯进行酯化、肟化反应制得两个系列弥拜霉素类似物化合物4Ia~5IId,所有目标化合物都通过核磁共振氢谱、高分辨质谱的确认,并分别对朱砂叶螨(Tetranychus cinnabarinus)、南方粘虫(Mythimna sepatara)和蚕豆蚜(Aphis fabae)进行室内杀虫活性测定,结果表明所有衍生物均表现出不同程度的杀虫活性,其中化合物4IIa和4IIb对粘虫和蚜虫表现出很高的杀虫活性.

关 键 词:弥拜霉素类似物  合成  杀虫活性

Synthesis, Characterization and Insecticidal Activity of Milbemycin Analogues
Xu,Xiaojun , Lai,Shenghong , Ji,Minghua , Zhu,Guonian , Zhao,Jinhao.Synthesis, Characterization and Insecticidal Activity of Milbemycin Analogues[J].Chinese Journal of Organic Chemistry,2012,32(6):1084-1092.
Authors:Xu  Xiaojun  Lai  Shenghong  Ji  Minghua  Zhu  Guonian  Zhao  Jinhao
Institution:Xu,Xiaojuna,b Lai,Shenghonga Ji,Minghuac Zhu,Guoniana Zhao,Jinhao,a,b(a Ministry of Agriculture Key Laboratory of Molecular Biology of Crop Pathogens and Insects,Institute of Pesticide and Environmental Toxicology,Zhejiang University,Hangzhou 310029)(b College of Pharmacy,Zhejiang University of Technology,Hangzhou 310014)(c Instituent of Science,Zhejiang Sci-Tech University,Hangzhou 310032)
Abstract:Two series of milbemycin analogues containing ester and methoxy oxime groups were designed according to ana-1H NMR and high resolution mass spectra(HRMS).The insecticidal activities of 18 analogues against Tetranychus cinna-log synthesis and sub-structure ligation from deglycosyl ivermectin,which is the analogue of milbemycin.The analogues reac-tion was carried out with the corresponding aromatic chloride,and the structures of the target compounds were confirmed by barinus,Mythimna sepatara and Aphis fabae were tested.The results showed that all analogues had different degree of insec-ticidal activity,especially compounds 4IIa and 4IIb showed the highest insecticidal activities against Mythimna sepatara and Aphis fabae.
Keywords:milbemycin analogues  synthesis  biological activity
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