| 新型含硫间二酰胺类化合物合成路线的设计与探索 |
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| 引用本文：吴静文,魏思琪,党帅慧,张燕,王继芬.新型含硫间二酰胺类化合物合成路线的设计与探索[J].上海第二工业大学(中文版),2024,41(1):37-45 |
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| 基金项目:上海市青年科技英才扬帆计划(21YF1414400), 上海市第二工业大学研究生副导师计划(EGD22DS10), 2023 年上海市大学生创新创业项目(202312044053) 资助 |
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| 中文摘要:具有高效、低毒且与传统杀虫剂无交互抗性的间二酰胺类GABA 受体杀虫剂—— 溴虫氟苯双酰胺(Broflanilide) 于2020 年获得全球首次登记, 目前关于其结构改造和生物活性研究相对较少, 拥有广阔的研究空间。
根据农药分子设计原理拟将生物活性多样和易于衍生化的硫元素引入Broflanilide 中, 结合文献调研结果和经典的有机反应, 设计了两条合成路线, 通过探索以2-氟-3-硝基苯甲酸甲酯为起始原料的双线型合成路线2 实现了目标化
合物的制备, 并利用理化数据表征对目标化合物结构进行了确证, 为后期含硫间二酰胺类化合物的合成和生物活性探究工作奠定了坚实的基础。 |
| 中文关键词:间二酰胺 硫 设计 合成路线 |
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| Design and Exploration of the Synthetic Routes of Novel M-Diamide Compounds Containing Sulfur |
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| Abstract:Broflanilide which possessed high efficiency, low toxicity, and no cross resistance with traditional insecticides acting on GABA receptor was globally registered in 2020. The research on its structural modification and biological activity was extremely rare, so possessed broad research market. Based on the literature research results and the classic organic reactions, two synthesis routes were
designed according to the principle of pesticide designing. The easy derivatization sulfur elements with diverse biological activities were introduced into Broflanilide. The corresponding target compounds were successfully prepared by the second synthesis route for two-line with methyl 2-fluoro-3-nitrobenzoate as the starting material, and the structures were confirmed by combining the physical and chemical data characterization, which provide a solid foundation for the synthesis of m-diamide compounds containing sulfur and their biological activities. |
| keywords:m-diamine sulfur design synthesis route |
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