5-脱氧阿维菌素B2a肟酯衍生物的合成及其杀虫活性
Synthesis and insecticidal activities of 5-deoxyavermectin B2a oxime ester derivatives.
作者信息
Sun Guoshao, Zhang Jingjing, Jin Shuhui, Zhang Jianjun
机构信息
Department of Applied Chemistry, College of Science, China Agricultural University Beijing 100193 P. R. China
出版信息
RSC Adv. 2018 Jan 22;8(7):3774-3781. doi: 10.1039/c7ra13258a. eCollection 2018 Jan 16.
Three series of avermectin B2a oxime ester derivatives were synthesized using avermectin B2a as starting material. All of the compounds were characterized by H NMR, C NMR, and HRMS. Bioassay results indicated that some of the derivatives (8b, 8c, 8d, 8f, 11k, 11l, 14c, 14j) showed potent insecticidal activities against , , or . As shown by initial insecticidal activity data, compound 8d showed excellent activities (>90%) against and , which were more potent than that of avermectin B2a. Compound 8d might be a lead compound for designing new avermectin B2a derivatives.
以阿维菌素B2a为起始原料，合成了三个系列的阿维菌素B2a肟酯衍生物。所有化合物均通过1H NMR、13C NMR和HRMS进行了表征。生物测定结果表明，部分衍生物（8b、8c、8d、8f、11k、11l、14c、14j）对[具体害虫1]、[具体害虫2]或[具体害虫3]表现出较强的杀虫活性。根据初步杀虫活性数据，化合物8d对[具体害虫1]和[具体害虫2]表现出优异的活性（>90%），其活性比阿维菌素B2a更强。化合物8d可能是设计新型阿维菌素B2a衍生物的先导化合物。
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