15-氯-18-烷(苄)氧亚胺基次甲基槐定碱类衍生物的合成及其杀虫/杀螨活性  

Synthesis and insecticidal/acaricidal activities of 15-chloro-18-alkyl(benzyl)oxyiminomethyne derivatives of sophoridine

作　　者：周义蒙 丁海霞 李璐璐 郝春阳 徐晖 吕敏 ZHOU Yimeng;DING Haixia;LI Lulu;HAO Chunyang;XU Hui;LYU Min(College of Plant Protection,Northwest A&F University,Yangling 712100,Shaanxi Province,China)

机构地区：[1]西北农林科技大学植物保护学院,陕西杨凌712100

出　　处：《农药学学报》2024年第6期1061-1068,共8页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金(32272592)。

摘　　要：槐定碱是一种从苦参和苦豆子中分离得到的喹诺里西啶类生物碱,具有抗癌、抗炎等医用活性,在农药上的研究较少。为提高槐定碱的农用价值,在其C-14、C-15位上进行结构修饰,设计合成了一系列15-氯-18-烷(苄)氧亚胺基次甲基槐定碱类衍生物。结果表明,化合物4i(R=4-NO2Bn)72 h LC_(50)值为0.408 mg/m L,其对朱砂叶螨(Tetranychus cinnabarinus)雌成螨的杀螨活性是槐定碱(LC_(50)=3.487 mg/m L)的8.5倍;在1 mg/m L质量浓度下,化合物4f(R=4-Br Bn)对东方黏虫(Mythimna separata)的杀虫活性最强,其35 d校正死亡率可达62.3%。这些研究结果为创制槐定碱类衍生物作为杀螨剂和杀虫剂提供了一定的研究基础。Sophoridine is a quinolizidine alkaloid isolated from Sophora flavescens and Sophora alopecuroides.Its medical activities include anticancer,anti-inflammation,etc.,but little pesticide research.To improve the agricultural value of sophoridine,a series of 15-chloro-18-alkyl(benzyl)oxyiminomethyne derivatives were designed and synthesized through structural modification at C-14 and C-15 positions.Compound 4i(R=4-NO2Bn)showed good acaricidal activity against female adults of Tetranychus cinnabarinus.Its 72 h LC_(50)value was 0.408 mg/mL,and its acaricidal activity was 8.5 times that of sophoridine(LC_(50)=3.487 mg/mL).At the concentration of 1 mg/mL,compound 4f(R=4-BrBn)had the best insecticidal activity against Mythimna separata,with a 35 d corrected mortality rate of 62.3%.These results will provide a basis for using sophoridine derivatives as acaricides and insecticides.

关 键 词：槐定碱 结构修饰 肟醚 杀虫/杀螨活性 

分 类 号：TQ450.1[化学工程—农药化工]