新型异恶唑啉/2'（2'，6'）-（二）氯鬼臼毒素肟磺酸酯作为杀虫剂的设计、合成与评价
Design, Synthesis and Evaluation of Novel Isoxazolines/Oxime Sulfonates of 2'(2',6')-(Di)Chloropodophyllotoxins as Insecticidal Agents.
作者信息
Yu Mingqiao, Liu Guangci, Zhang Yuanyuan, Feng Tao, Xu Ming, Xu Hui
机构信息
Research Institute of Pesticidal Design &Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, Shaanxi Province, P. R. China.
Shaanxi Key Laboratory of Natural Products &Chemical Biology, College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi Province, P. R. China.
出版信息
Sci Rep. 2016 Sep 26;6:33062. doi: 10.1038/srep33062.
A series of 2'(2',6')-(di)halogeno-isoxazolopodophyllic acids-based esters, and oxime sulfonates of 2'(2',6')-(di)halogenopodophyllones were prepared by structural modifications of podophyllotoxin as insecticidal agents against Mythimna separata Walker. It was found that when 2'(2',6')-(di)halogenopodophyllones or 2'(2',6')-(di)chloropicropodophyllones reacted with hydroxylamine hydrochloride, the desired products were related with the configuration of their lactones. Three key single-crystal structures of Ie, IIe and IIIb were determined by X-ray diffraction. Especially compounds IIc and Vc showed the highest insecticidal activity. Moreover, some interesting results of structure-insecticidal activity relationships of tested compounds were also observed.
通过对鬼臼毒素进行结构修饰，制备了一系列基于2'(2',6')-(二)卤代异恶唑鬼臼酸的酯类以及2'(2',6')-(二)卤代鬼臼毒素的肟磺酸酯，作为防治粘虫（Mythimna separata Walker）的杀虫剂。研究发现，当2'(2',6')-(二)卤代鬼臼毒素或2'(2',6')-(二)氯苦鬼臼毒素与盐酸羟胺反应时，所需产物与它们内酯的构型有关。通过X射线衍射确定了Ie、IIe和IIIb的三个关键单晶结构。特别是化合物IIc和Vc表现出最高的杀虫活性。此外，还观察到了受试化合物结构-杀虫活性关系的一些有趣结果。
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