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 search the new anti-cancer drugs inhibiting with cell division cycle CDC25B phosphatase, designing and synthesizing 6-Methylimidazo[1,2-d][1,2,3,4]thiatriazole-5-carboxylic acid derivatives is meaningful. Methods: The objective compounds were synthesized by cyclization, hydrazinolysis, condensation in the basis 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 determined by elemental analysis, IR, 1H NMR and MS, furthermore, it was found that the inhibition rates (% inhibition) of the CDC25B were 85.4 and 82.3 by compounds 3 and 4a with a certain biological activity.