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目的合成6种含氟吗啉衍生物并对目标化合物进行抗抑郁活性筛选。方法以三氟甲基苯丙酮为起始原料,经过溴化、胺化、环合、还原、酸化反应合成6种新型含氟吗啉衍生物,采用小鼠强迫游泳模型,对目标化合物进行实验性抗抑郁药理活性研究。结果目标化合物物经1H-NMR、IR和MS分析确证。化合物Vb和Ve小鼠强迫游泳不动时间分别为(110.1±27.5)s和(107.1±29.4)s,显著低于空白对照组[(150.4±38.5)s](P<0.05)。结论该合成路线反应条件温和、操作简便,目标化合物Vb和Ve显示出一定的抗抑郁活性。
Objective To synthesize six kinds of fluorine-containing morpholine derivatives and screen the target compounds for their antidepressant activity. Methods Six novel fluoromorpholine derivatives were synthesized by bromination, amination, cyclization, reduction and acidification using trifluoromethyl propiophenone as a starting material. The mice were forced to swim and the target compounds were tested Study on pharmacological antidepressant activity. Results The target compounds were confirmed by 1H-NMR, IR and MS. The forced immobilization time of compound Vb and Ve mice was (110.1 ± 27.5) s and (107.1 ± 29.4) s, respectively, which was significantly lower than that of the control group [(150.4 ± 38.5) s] (P <0.05). Conclusion The synthetic route is mild and easy to operate. The target compounds Vb and Ve show some antidepressant activities.