含三氟甲基吗啉醇衍生物的设计、合成及抗抑郁活性  

Synthesis and Antidepressant Activity of Trifluoromethyl-morpholinol Derivatives

作　　者：郭倩[1] 郑友霖[1] 唐小敏[1] 田芳杰 罗甜[1] 肖新荣[1] 

机构地区：[1]南华大学化学化工学院,湖南衡阳421001

出　　处：《化学试剂》2016年第10期937-939,944,共4页Chemical Reagents

基　　金：湖南省科技计划资助项目(2014FJ3134)

摘　　要：以芳基烷基酮和氨基醇类衍生物为原料,设计合成了8个含三氟甲基吗啉醇盐酸盐。目标化合物结构经IR、~1HNMR和ESI-MS表征确认。通过小鼠强迫游泳抗抑郁药理实验,对目标化合物进行抗抑郁活性筛选。实验结果显示,化合物3,5,5-三甲基-2-（间三氟甲基苯基）-2-吗啉醇盐酸盐、3-甲基-5-苯基-2-（对三氟甲基苯基）-2-吗啉醇盐酸盐和3,5,5-三甲基-2-（对三氟甲基苯基）-2-吗啉醇盐酸盐有良好的抗抑郁活性。Eight trifluoromethyl-morpholinol derivatives were synthesized by using aromatic ketones and amino-alcohol derivatives as starting materials. The structures of title compounds were confirmed by IR, ~ HNMR and ESI-MS. The force swimming test was performed to investigate antidepressant activity of the title compounds. And the result indicated that 3,5,5-trimethyl-2-（ m-triflu- oromethylphenyl ） -2-morphopinol, 3-methyl-5-phenyl-2- （ p-trifluoromethylphenyl ） -2-morphopinol, and 3,5,5 -trimethyl-2- （ p-trif- luoromethylphenyl）-2-morphopinol exhibited good antidepressant activity.

关 键 词：三氟甲基 吗啉醇 合成 抗抑郁活性 

分 类 号：O622.2[理学—有机化学]