Sun Guoshao, Zhang Jingjing, Jin Shuhui, Zhang Jianjun
Department of Applied Chemistry, College of Science, China Agricultural University Beijing 100193 P. R. China
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。
