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4-氨基-5-吡啶-4-基-均三唑硫醇(1)在复合催化剂DMAP和TBAB作用下与对卤代苯甲酸经环缩合反应以高收率得到中间体6-(5-氯-3-甲基-1-取代苯基-1H-吡唑-4-基)-3-吡啶-3-基-均三唑并[3,4-b][1,3,4]噻二唑(2a～2c),接着苯环卤原子与取代哌嗪在聚乙二醇催化作用下发生亲核取代反应得到相应的哌嗪游离碱(3a～3c).其中,单取代哌嗪游离碱3a与含功能基的卤代物缩合得到功能基取代的哌嗪衍生物(4a～4g).这些产生的游离碱与盐酸反应得到相应的水溶性盐酸盐.所合成新化合物的结构经元素分析和光谱数据表征,并评价了它们的体外抗菌活性及构效关系.
4-Amino-5-pyridin-4-yl-S-triazolethiol (1) The intermediate 6- (5- 1H-pyrazol-4-yl) -3-pyridin-3-yl-triazolo [3,4- b] [1,3,4] thioxo (2a ~ 2c), followed by nucleophilic substitution reaction between the benzene ring halogen atom and the substituted piperazine under the action of polyethylene glycol to obtain the corresponding piperazine free base (3a ~ 3c), wherein the monosubstituted piperazine is free The base 3a is condensed with a functional group-containing halide to give a functionalized substituted piperazine derivative (4a-4g) .The resulting free base is reacted with hydrochloric acid to give the corresponding water-soluble hydrochloride.The structure of the new compound synthesized is characterized by elemental Analysis and spectral data characterization, and evaluate their in vitro antibacterial activity and structure-activity relationship.