咪唑[1,2-d]并-1,2,3,4-噻三唑衍生物的合成

Synthesis of Imidazo[1,2-d][1,2,3,4]-thiatriazole Derivatives

为寻找CDC25B磷酸酯酶抑制剂,设计、合成咪唑[1,2-d]并-1,2,3,4-噻三唑衍生物。以溴代乙酰乙酸乙酯和5-氨基-1,2,3,4-噻三唑为原料,经过关环、肼解、缩合3步反应合成了5个目标化合物。通过元素分析、IR、1HNMR和MS分析确定了其结构。活性结果表明,6-甲基咪唑[1,2-d]并-1,2,3,4-噻三唑-5-甲酰肼和N'-苄基-6-甲基咪唑并[1,2-d]并-1,2,3,4-噻三唑-5-甲酰肼对CDC25B有一定的抑制作用。

In order to develop the new CDC25 B phosphatase inhibitor,imidazole[1,2-d]-1,2,3,4-thiophene triazole derivatives have been synthesized. By cyclization,hydrazinolysis,three-step condensation reaction with ethyl acetoacetate and 5-bromo-1,2,3,4 thiatriazole acting as raw material,five kinds of target compounds were synthesized. The structures of the compounds were confirmed by elemental analysis,IR,1HNMR and MS. The results showed that the compounds 6-methylimidazo-[1,2-d]-1,2,3,4-thiadiazole-5-carboxylic acid hydrazide and N-benzyl-6-methylimidazo-[1,2-d]-1,2,3,4-thiadiazole-5-carboxylic acid hydrazide have certain inhibitory effect on the CDC25 B.