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[目的]合成2-[1-(2-吡啶)乙氧基]乙酸2-[4-苄基取代哌嗪]乙酯类化合物,探讨其对小鼠学习记忆能力的影响.[方法]使用2-乙基吡啶为起始原料,经Whol-ziegler反应得到2-(1-溴乙基)吡啶,再与羟基乙酸乙酯的醇钠盐缩合得到2-[1-(2-吡啶)乙氧基]乙酸乙酯.无水哌嗪与不同取代的氯苄反应分别得到化合物4a～4l.化合物4a～4l分别与溴乙醇反应得到化合物5a～5l.化合物2-[1-(2-吡啶)乙氧基]乙酸乙酯与化合物5a～5l经酯交换反应得到目标化合物6a～6l.采用通道式水迷宫法测定化合物6j的促进小鼠学习记忆活性.[结果]设计合成了12个尚未见文献报道的新化合物,结构经核磁共振谱、红外光谱等确证.与模型对照组比较,化合物6j大、小剂量组到达时间显著缩短,错误次数明显减少,相比较差异均有统计学意义(P<0.05).[结论]化合物6j具有良好的促进小鼠学习记忆作用.
[Objective] The purpose was to synthesize 2- [4-benzyl substituted piperazine] ethyl 2- [1- (2-pyridyl) ethoxy] acetate and study its effect on learning and memory of mice. [Method] 2-ethylpyridine as the starting material to obtain 2- (1-bromoethyl) pyridine by Whol-ziegler reaction, which was condensed with alcohol sodium salt of ethyl glycolate to give 2- [1- (2-pyridyl) (2-pyridyl) oxy] acetate.Another step of reaction of anhydrous piperazine with different substituted benzyl chlorides gave compounds 4a ~ 4l, respectively.The compounds 4a ~ 4l were reacted with bromoethanol to give compounds 5a ~ ) Ethoxy] acetate with compounds 5a ~ 5l to give the target compounds 6a ~ 6l. The channel-like water maze method was used to determine the effect of compound 6j on learning and memory in mice. [Results] Twelve The new compounds reported in the literature were confirmed by nuclear magnetic resonance spectroscopy, infrared spectroscopy, etc. Compared with the model control group, the arrival time of compound 6j in the large and small dose groups was significantly shortened and the number of errors significantly decreased, with statistical significance compared with that of the model control group P <0.05). [Conclusion] Compound 6j has a good effect on learning and memory in mice.