3-甲基-2-(3-氯基苯基)吗啉盐酸盐的合成及其抗实验性抑郁活性

以1-(3-氯基苯基)-2-溴-1-丙酮和乙醇胺为原料,经胺化、环合反应、还原,最后酸化得新型吗啉化合物(2):3-甲基-2-(3-氯基苯基)吗啉盐酸盐,产率67.2 %,目标化合物结构经IR、1H NMR、MS测试技术确证,该化合物的合成在国内外从未见有过报道.利用小鼠强迫游泳抗抑郁药理模型对所合成的化合物进行抗抑郁药理活性观察.结果显示此化合物(2)具有一定的抗抑郁活性,值得进一步研究.

Synthesis and Antidepressive Activity of 3-methyl-2-(3-chlorophenyl)Morpholine Hydrochloride

3-methyl-2-(3-chlorophenyl) morpholinhy drochloride was synthesized from 1-(3-chlorophenyl) -2-bromo -1 - Acetone and ethanolamine as raw material,in polar solvents by amine,cyclization reaction,reduction,at last acidification by divergent synthetic method,and the yield is 79.3%.The target compound structure was confirmed by IR,1H NMR,MS tec-hnology,and the synthesis of this compound had never been reported at home and abroad.Using the forced swim mice model of antidepressant pharmacology,the pharmacological effects of antidepressant of the synthesized compounds were observed.That compound (2) have potent antidepress activities,and are worth further development.