新环6-甲基咪唑[1,2-d]并-1,2,3,4-噻三唑-5-羧酸衍生物的合成

Synthesis of Neoring 6-Methylimidazo[1,2-d][1,2,3,4]thiatriazole-5-carboxylic Acid Derivatives

目的:为了寻找抑制细胞分裂周期磷酸酯酶CDC25B的抗肿瘤新药,设计和合成6-甲基-咪唑[1,2-d]并-1,2,3,4-噻三唑-5-羧酸衍生物是有意义的。方法:以5-氨基-1,2,3,4-噻三唑和溴代乙酰乙酸乙酯为原料,经过关环,肼解,缩合等反应合成目标化合物。结果:合成了5种新的化合物。结论:所得化合物,通过元素分析、IR、1H NMR和质谱分析确定了其结构,并且化合物3和4a对CDC25B的抑制率(%抑制率)分别为85.4和82.3,具有一定的生物活性。

Objective: In order to searchthe new anti-cancer drugsinhibiting with cell division cycle CDC25B phosphatase, designing and synthesizing6-Methylimidazo[1,2-d][1,2,3,4]thiatriazole-5-carboxylic acid derivatives is meaningful. Methods: The objectivecompounds were synthesized by cyclization, hydrazinolysis, condensation in thebasis of 5-amino-1,2,3,4-triazole and bromine ethyl acetoacetate. Result: The five new kinds of compounds were synthesized. Conclusion: The structures of the compounds were determinedby elemental analysis, IR, 1H NMR and MS, furthermore, it was foundthat the inhibition rates (% inhibition) of the CDC25B were 85.4 and 82.3 bycompounds 3 and 4a witha certain biological activity.