含1,2,4-三唑-5-硫酮席夫碱的新型1,2,4-三唑并[1,5-a]嘧啶衍生物的合成及生物活性研究  

Synthesis and Bioactivities of Novel 1,2,4-Triazolo[1,5-a]pyrimidine Derivatives Containing 1,2,4-Triazole-5-thione Schiff Base Unit

作　　者：熊启中[1] 林选福[1] 刘军虎[1] 毕亮[1] 鲍小平[1] 

机构地区：[1]贵州大学精细化工研究开发中心教育部绿色农药与农业生物工程重点实验室,贵阳550025

出　　处：《有机化学》2012年第7期1255-1260,共6页Chinese Journal of Organic Chemistry

基　　金：贵州省优秀科技教育人才省长专项资金(No.200817);贵州省自然科学基金(No.20082265)资助项目~~

摘　　要：以2-苄硫基-5-甲基-7-羟基-1,2,4-三唑并[1,5-a]嘧啶为原料,经醚化、肼解、成盐、关环和席夫碱反应合成了20个新型的含1,2,4-三唑-5-硫酮席夫碱的1,2,4-三唑并[1,5-a]嘧啶类化合物,通过IR,1H NMR,MS和元素分析对所合成的化合物进行了结构表征.初步生物活性测试结果表明,部分化合物表现出一定的抑菌或较好的抗烟草花叶病毒(TMV)活性.在500μg/mL浓度下,化合物6b,6f和6p对TMV的抑制率分别为41%,43%和40%.Using 2-benzylthio-5-methyl-7-hydroxyl-l,2,4-triazolo[1,5-a]pyrimidine as starting compound, twenty novel 1,2,4-triazolo[1,5-a]pyrimidine derivatives containing 1,2,4-triazole-5-thione Schiff-base unit were synthesized through se- quential reactions of etherification, hydrazinolysis, salification, cyclization and condensation. Target compounds were fully characterized by IR, IH NMR, MS techniques and elemental analysis. Preliminary bioassay indicated that some compounds exhibited certain fungicidal or good anti-TMV activities. At the concentration of 500 μg/mL, the inhibition rates of compounds 6b, 6f and 6p against tobacco mosaic virus （TMV） were 41%, 43% and 40%, respectively.

关 键 词：1 2 4-三唑并[1 5-a]嘧啶 1 2 4-三唑-5-硫酮席夫碱 合成 生物活性 

分 类 号：O626.4[理学—有机化学] TQ450.1[理学—化学]