间二氟吗啉醇衍生物分子设计、合成及抗实验性抑郁活性研究

以3,5_二氟苯腈为起始原料与乙基溴化镁反应合成的3,5_二氟苯丙酮,经过溴代、胺化、环合、酸化反应,合成4个间二氟吗啉醇盐酸盐化合物,目标化合物的结构经1 H NMR,IR和MS分析确证,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试验。结果表明,目标化合物Ⅵ4具有一定的抗抑郁活性。

Molecule Design,Synthesis and Antidepressive Activity ofM-difluorinemorpholinol Derivatives

In this paper,3,5_difluoropropiophenone is synthetised using 3,5_difluorine ben_zene nitriles as the raw material reaction with ethyl magnesium bromide. Starting from 3,5_difluoropropiophenone,the four m_difluorine morpholinol hydrochloride are synthetised via several steps including bromination, amination, cyclization and acidification. Using the forced swim mice model of antidepressant pharmacology,the pharmacological effects of an_tidepressant of the synthesized compounds were observed. The target compound is synthe_tised and its structure is proved by 1 H NMR,IR and MS. Results show that compound Ⅵ4 have potent antidepressant activities.