| 新型先导化合物2-(2-氯-4-三氟甲基苯氧基)-4-三氟甲基噻唑-5-甲酸乙酯的设计、合成与生物活性 |
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| 引用本文： | 刘长令,李正名.新型先导化合物2-(2-氯-4-三氟甲基苯氧基)-4-三氟甲基噻唑-5-甲酸乙酯的设计、合成与生物活性[J].农药,2006,45(4):246-247. |
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| 作者姓名： | 刘长令 李正名 |
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| 作者单位： | 1. 沈阳化工研究院,新药合成室,辽宁,沈阳,110021;南开大学,元素有机化学国家重点实验室,元素有机化学研究所,天津,300071
2. 南开大学,元素有机化学国家重点实验室,元素有机化学研究所,天津,300071 |
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| 基金项目： | 国家重点基础研究发展计划(973计划) |
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| 摘 要： | 以3-氨基-4，4，4-三氟甲基丁烯酸乙酯为原料，经环化、氯化、醚化制得新型先导化合物2-（2-氯-4-三氟甲基苯氧基）-4-三氟甲基噻唑-5-甲酸乙酯，其结构经红外、核磁、高分辨质谱确认。生物活性测定结果表明新型先导化合物在600g／hm^2剂量下对叶蝉和二点叶螨的防效均为100％；在300g／hm^2剂量下对马铃薯晚疫病的防效为90％。
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| 关 键 词： | 合成 生物活性 先导化合物 2-(2-氯-4-三氟甲基苯氧基)-4-三氟甲基噻唑-5-甲酸乙酯 |
| 文章编号： | 1006-0413（2006）04-0246-02 |
| 收稿时间： | 2005-12-29 |
| 修稿时间： | 2005-12-29 |
Design, synthesis and biological activity of the novel lead compound ethyl 2-(2-chloro-4-trifluoromethylphenoxy)-4-trifluoromethyl-thiazole-5-carbonate |
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| LlU Chang-ling,LI Zheng-ming.Design, synthesis and biological activity of the novel lead compound ethyl 2-(2-chloro-4-trifluoromethylphenoxy)-4-trifluoromethyl-thiazole-5-carbonate[J].Pesticides,2006,45(4):246-247. |
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| Authors: | LlU Chang-ling LI Zheng-ming |
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| Affiliation: | 1 .Agrochemical Discovery Department, Shenyang Research Institute of Chemical Industry, Shenyang 110021, Liaoning, China ; 2.Institute of Elemento-Organic Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China |
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| Abstract: | Using ethyl 3-amino-4,4,4-trifluoro-butyrate as the starting reagent, cyclization, chlorination, and esterifi-cation reactions were conducted to yield the novel lead compound ethyl 2-(2-chloro-4-trifluoromethylphenoxy)-4-trifluoromethyl-thiazole-5-carbonate. The chemical structure was confirmed by IR, 1H NMR, and HRMS. Biologicalactivity studies indicated that the lead compound at 600 g a.i./ha provided 100% control of both potato leafhopper andtwo-spotted spider mites while at 300 g a.i./ha provided 90% control of potato late blight. |
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| Keywords: | synthesis biological activity lead compound ethyl 2-(2-chloro-4-trifluoromethylphenoxy)-4-trifluoromethyl-thiazole-5-carbonate |
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