摘要
芳香羧酸经酯化、肼解、成盐、环化成3-芳基-4-氨基-5-巯基-1,2,4-三唑(1a～1h),然后与噻吩-2,5-二羧酸在相转移催化剂四丁基碘化铵和POCl3作用下,高产率地制得了8种2,5-双-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑噻吩类衍生物(3a～3h),并利用IR、1H NMR、MS和元素分析对目标化合物的结构进行了表征.初步的抗菌试验表明,部分目标化合物表现出较好的抑菌活性.
The aroylhydrazides were prepared by esterification and hydrazinolysis of corresponding aromatic carboxylic acids.The reaction of aroylhydrazides with CS2/KOH in absolute ethanol gave potassium aroyldithiocarbazates and then hydrazinolysis of potassium aroyldithiocarbazates with hydrazine hydrate afforded 3-aryl-4-amino-5-mercapto-1,2,4-triazoles（1a～1h）.New eight compounds of 2,5-thiophene derivatives containing bis-triazolo[3,4-b]-[1,3,4]thiadiazole（3a～3h） were synthesized in high yields by cyclization of thiophene-2,5-dicarboxylic acid with 3-aryl-4-amino-5-mercapto-1,2,4-triazoles（1a～1h）.The structures of 3a～3h were confirmed by elementary analyses,IR,1H NMR,and MS spectra.The preliminary antibacterial tests showed that most of them had good antibacterial activities.
出处
《江西师范大学学报（自然科学版）》
CAS
北大核心
2010年第6期560-563,共4页
Journal of Jiangxi Normal University(Natural Science Edition)
基金
湖北省2010年高校产学研合作(C2010027)资助项目
