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为研究吸电子基-氟,对苯甲氧基乙酸酯类小鼠学习记忆促进作用的影响,合成了(4-氟苯甲氧基)乙酸衍生物(5～9)。4-氟甲笨经Wohl-Ziegler反应及Williamson反应得到(4-氟苯甲氧基)乙酸乙酯(5)。(5)的氨解,肼解分别得到相应的酰胺(6)和酰肼(7)。5与过量的二甲(乙)氨基乙醇酯交换,继而通入氯化氢得到(4-氟苯甲氧基)乙酸-2-二甲(乙)氨基乙酯盐酸盐(8,9),药理实验表明,8对于40％乙醇引起的记忆再现障碍具有显著拮抗作用。5的合成方法为尚未见报道的新方法。化合物(6～9)为尚未见报道的新化合物,其结构经核磁共振谱,红外光谱及元素分析所证实。
In order to study the effect of electron-withdrawing group-fluorine on the learning and memory of benzyloxyacetates in mice, (4-fluorobenzyloxy) acetic acid derivatives (5 ~ 9) were synthesized. The 4-fluorometholone was subjected to Wohl-Ziegler reaction and Williamson reaction to give ethyl (4-fluorobenzyloxy) acetate (5). Hydrolysis of (5) gives the corresponding amide (6) and hydrazide (7), respectively, by hydrazinolysis. 5 is exchanged with an excess of dimethyl (ethyl) aminoethanol, followed by hydrogen chloride to give (4-fluorobenzyloxy) acetic acid 2-dimethylaminoethyl ester hydrochloride (8,9) Experiments show that 8 has a significant antagonistic effect on 40% ethanol-induced memory impairment. 5 synthesis method has not been reported for the new method. Compounds (6 ~ 9) are new compounds that have not been reported yet. Their structures were confirmed by NMR, IR and elemental analysis.