三唑并噻二唑衍生物的合成及抑菌活性  

Synthesis and Fungicidal Activity of Triazolothiadiazole Derivatives

作　　者：杨知昆[1] 孙学军[1] 米娜[2] 张海科[2] 尤进茂[1] 范志金[2] 

机构地区：[1]曲阜师范大学化学科学学院 [2]南开大学元素有机化学国家重点实验室,天津300071

出　　处：《应用化学》2009年第9期1027-1030,共4页Chinese Journal of Applied Chemistry

基　　金：国家自然科学基金(20672062;20872071);国家自然科学基金国际(地区)合作与交流项目/合作研究项目(20911120069);天津市自然科学基金(07JCYBJC01200);国家重点基础研究发展计划"九七三"(2003CB114402);天津市科技支撑计划国际科技合作项目(07ZCGHHZ01400)资助项目

摘　　要：利用活性亚结构拼接原理，将活性基团分别引入1，2，4-均三唑并[3，4-b]-1，3，4．噻二唑杂环的3位和6位，合成了11种3，6-二取代均三唑并[3，4-b]-1，3，4一噻二唑类新化合物，收率为43％-95％。并用IR、^1HNMR、EI—MS及元素分析测试技术对其进行了结构表征。抑菌活性测试表明，所合成的大部分化合物对黄瓜灰霉病菌（Botryt／scinerea）有较好的生长抑制作用，其中，化合物5ae、Sag和5bd的抑制率均达70％，化合物Sad、5cd、5ce的抑制率大于60％，化合物5bd对水稻纹枯病菌（Pellicularia sasakii）抑制率大于60％，化合物5cg对西瓜炭疽病菌（Colletotrichum lagenarium）的抑制率为69％。Eleven novel compounds were designed and synthesized from 3-substituted-4-amino-5-mereapto- 1,2,4-triazoles with heterocyclie carboxylic acid via cyclization in the presence of phosphoryl chloride on the basis of the princple of combination of active structural moieties. All the compounds were characterized by melting point, IR, ^1H NMR and elemental analysis. The results of bioassay experiments with 10 commonly used fungi show that all the compounds had satisfactory fungicidal activity against Botrytis cinerea, with the growth inhibition rate of compounds 5ae, 5ag, 5bd against Botrytis cinerea being up to 70% and that 5cd, 5ce against Botrytis cinerea more than 60% ; compound 5bd exhibited fungicidal activity against laria sasakii with growth inhibition of up to 60% Colletotrichum lagenarium was 69%. and the growth inhibition rate of compound 5cg Keywords triazolothiadiazole,3,6 point-substituted derivatives, synthesis, fungicide of 5ad, PeUicuagainst

关 键 词：均三唑并噻二唑 3 6位取代衍生物 合成 杀菌活性 

分 类 号：O621.2[理学—有机化学]