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  

Design, synthesis and biological activity of the novel lead compound ethyl 2-(2-chloro-4-trifluoromethylphenoxy)-4-trifluoromethyl-thiazole-5-carbonate

作　　者：刘长令[1,2] 李正名[2] 

机构地区：[1]沈阳化工研究院新药合成室,辽宁沈阳110021 [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

出　　处：《农药》2006年第4期246-247,共2页Agrochemicals

基　　金：国家重点基础研究发展规划项目(2003CB114400)资助

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/hm2剂量下对叶蝉和二点叶螨的防效均为100%;在300g/hm2剂量下对马铃薯晚疫病的防效为90%。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. Biological activity studies indicated that the lead compound at 600 g a.i./ha provided 100% control of both potato leafhopper and two-spotted spider mites while at 300 g a.i./ha provided 90% control of potato late blight.

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 

分 类 号：TQ455[化学工程—农药化工]