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有机化学
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有机化学 ›› 2012, Vol. 32 ›› Issue (06): 1084-1092.DOI: 10.6023/cjoc1111021 上一篇    下一篇

研究论文

弥拜霉素类似物的合成、表征和杀虫活性研究

徐小军a,b, 赖声洪a, 季明华c, 朱国念a, 赵金浩a,b   

  1. a 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;
    b 浙江工业大学药学院 杭州 310014;
    c 浙江理工大学科学研究所 杭州 310032
  • 收稿日期:2011-11-10 修回日期:2012-01-07 发布日期:2012-02-27
  • 通讯作者: 赵金浩 E-mail:jinhaozhao@zju.edu.cn
  • 基金资助:
    浙江省科技厅重大(No. 2008C02007-3)资助项目.

Synthesis, Characterization and Insecticidal Activity of Milbemycin Analogues

Xu Xiaojuna,b, Lai Shenghonga, Ji Minghuac, Zhu Guoniana, Zhao Jinhaoa,b   

  1. 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
  • Received:2011-11-10 Revised:2012-01-07 Published:2012-02-27
  • Supported by:
    Project supported by the Important Technology Special Topic Project of Zhejiang Province (No. 2008C02007-3).

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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

Two series of milbemycin analogues containing ester and methoxy oxime groups were designed according to analog synthesis and sub-structure ligation from deglycosyl ivermectin, which is the analogue of milbemycin. The analogues reaction was carried out with the corresponding aromatic chloride, and the structures of the target compounds were confirmed by 1H NMR and high resolution mass spectra (HRMS). The insecticidal activities of 18 analogues against Tetranychus cinnabarinus, Mythimna sepatara and Aphis fabae were tested. The results showed that all analogues had different degree of insecticidal activity, especially compounds 4IIa and 4IIb showed the highest insecticidal activities against Mythimna sepatara and Aphis fabae.

Key words: milbemycin analogues, synthesis, biological activity