| 含氟吡啶羧酸酯类化合物的合成及生物活性 |
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| 引用本文： | 郑辉,刘运奎,赵卿,徐振元.含氟吡啶羧酸酯类化合物的合成及生物活性[J].应用化学,2010,27(2):164-168. |
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| 作者姓名： | 郑辉 刘运奎 赵卿 徐振元 |
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| 作者单位： | 1. 杭州师范大学材料与化学化工学院,杭州
2. 浙江工业大学化学工程与材料学院,杭州,310014 |
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| 基金项目： | 国家九七三计划，长三角重大科技联合攻关项目 |
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| 摘 要： | 为了寻找具有生物活性的新化合物,以氟乙酸甲酯、氰乙酰胺和甲酸乙酯为起始原料,经环合、氯化、水解、酰氯化等反应合成了含氟吡啶酰氯中间体,再与醇类和酚类反应合成了一系列含氟吡啶羧酸酯类化合物,总收率约38%。其结构经1HNMR、13CNMR、IR、MS及元素分析测试技术确证。初步杀虫抑菌活性测试表明,部分化合物1e、1i、1j和1k在500mg/L浓度下,对淡色库蚊的杀死率在61.9%～100%之间,但对几种受试植物病菌的抑制活性很差。化合物1k活性最好,在500mg/L时对粘虫(armyworm)和淡色库蚊(culex mosquito)的杀死率均为100%。初步构效关系分析表明,芳杂环酚的该类化合物有较好的活性,而脂肪醇的该类化合物无活性。
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| 关 键 词： | 含氟化合物，吡啶杂环，羧酸酯类，生物活性 |
| 收稿时间： | 2009-02-20 |
| 修稿时间： | 2009-05-29 |
Synthesis and Biological Activity of Fluorine-Substituted Pyridine-Heterocyclic Carboxylate Compounds |
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| ZHENG Hui,LIU Yun-Kui,ZHAO Qing,XU Zhen-Yuan.Synthesis and Biological Activity of Fluorine-Substituted Pyridine-Heterocyclic Carboxylate Compounds[J].Chinese Journal of Applied Chemistry,2010,27(2):164-168. |
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| Authors: | ZHENG Hui LIU Yun-Kui ZHAO Qing XU Zhen-Yuan |
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| Affiliation: | ZHENG Hui a,LIU Yun-Kui b,ZHAO Qing a,XU Zhen-Yuan b(aChemistry & Chemical Engineering,College of Material,Hangzhou Normal University,Hangzhou,bCollege of Chemical Engineering & Materials,Zhejiang University of Technology,Hangzhou 310014) |
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| Abstract: | In the search of bioactive compounds,a series of fluorine-substituted pyridine-heterocyclic carboxylate compounds were synthesized with methyl fluoroacetate,cyanacetamide,ethyl formic ester,alcoholic and phenolic compounds via ring closure,chlorination,hydrolyzation,acylchloriration and esterification reactions. The overall yield was about 38%. All compounds were characterized by 1H NMR,13C NMR,IR,MS and elemental analysis. The preliminary bioassay results show that compounds 1e,1i,1j and 1k exhibited 61.9%... |
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| Keywords: | fluorinated compound pyridine heterocycle carboxylate bioactivity |
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