对羟基苯甲醛磷酸酯席夫碱衍生物的合成及其抗抑郁活性  

Synthesis and Antidepressant Activities of 4-Hydroxybenzal-dehyde Schiff Base Derivatives with Phosphate Ester Group

作　　者：刘进兵[1] 吴凤艳[1] 

机构地区：[1]邵阳学院生物与化学工程系,湖南邵阳422000

出　　处：《合成化学》2015年第10期934-937,共4页Chinese Journal of Synthetic Chemistry

基　　金：邵阳学院创新团队资助项目

摘　　要：以对羟基苯甲醛为起始原料,经醚化和酯化反应制得中间体4-(2-羟乙氧基)苯甲醛磷酸二甲酯(2);2分别与伯胺经缩合反应合成了4个对羟基苯甲醛磷酸酯席夫碱衍生物(4a^4d),其结构经1H NMR,13C NMR,IR和ESI-MS确证。采用应急模型对4a^4d进行抗抑郁活性研究。初步结果表明:2和4-(2-羟乙氧基)苯甲醛磷酸二甲酯甲氧基胺席夫碱(4d)表现出较好的抗抑郁活性,2的活性优于丙咪嗪,4d的活性与丙咪嗪接近。Four 4-hydroxybenzaldehyde Schiff base derivatives（ 4a - 4d） with phosphate ester group were synthesized by condensation reaction of primary amine with 2-（ 4-formylphenoxy） ethyl dimethyl phosphate（ 2）,which was prepared by etherification and esterification from 4-hydroxybenzaldehyde.The structures were confirmed by^1 H NMR,^13 C NMR,IR and ESI-MS. Their antidepressant activities were investigated by emergency model. The results showed that 2 and 2-{ 4-[（ methoxyimino）methyl]phenoxy} ethyl dimethyl phosphate（ 4d） had certain antidepressant activities in vivo. And 2showed the better antidepressant activity than imipramine.

关 键 词：对羟基苯甲醛 磷酸酯 席夫碱 合成 抗抑郁活性 

分 类 号：O625.632[理学—有机化学] O627.51[理学—化学]