2-苄硫(砜)基-5-甲基-7-取代苄氧基-1,2,4-三唑并[1,5-a]嘧啶类衍生物的合成及抑菌活性研究  

Synthesis and Fungicidal Activities of 2-Benzylthio(sulfonyl)-5-methyl-7-substituted benzyloxy-1,2,4-triazolo[1,5-a] pyrimidine Derivatives

作　　者：林选福[1] 谭赞[1] 刘勇[1] 贺银菊[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》2013年第2期353-358,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)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]嘧啶为起始原料,经过醚化、氧化反应分别合成了12个新型的2-苄硫基-5-甲基-7-取代苄氧基-1,2,4-三唑并[1,5-a]嘧啶类化合物5a～5l及其砜基类似物6a～6l,并通过1H NMR,IR,MS和元素分析对所有目标化合物进行了结构表征.初步生物活性测试结果表明,在50μg/mL浓度下,部分化合物表现出了一定的抑菌活性,其中化合物5c,5k和5l对黄瓜灰霉病菌的抑制率分别为61%,69%和85%.Using 2-benzylthio-5-methyl-7-hydroxyl-l,2,4-triazolo[1,5-a]pyrimidine as starting material, twelve novel 2-benzylthio-5-methyl-7-substituted benzyloxy-l,2,4-triazolo[1,5-a]pyrimidine derivatives 5a^51 and their sulfonyl ana- logues 6a-61 were synthesized through sequential reactions of etherification and oxidation, respectively. Their structures were characterized by 1H NMR, IR, MS and elemental analysis. The preliminary bioassay indicated that some compounds exhibited certain fungicidal activities, for example, the inhibition rates of compounds 5c, 5k and 51 （50/ag/mL） against Botrytis cinerea were 61%, 69% and 85%, respectively.

关 键 词：1 2 4-三唑并[1 5-a]嘧啶 硫醚(砜) 氧醚 合成 抑菌活性 

分 类 号：O626.41[理学—有机化学]