【摘要】 目的:合成抗抑郁药安非他酮类似物3,5-二甲基-2-(3′,5′-二氟苯基)-2-吗啉醇盐酸盐。方法:以3,5-二氟苯丙酮为原料,经溴代、胺化、环合、酸化合成了目标产物。结果:合成目标产物的总收率为77．3%,中间体和产物经红外光谱和核磁共振谱确证。结论:以溴化铜为α-澳代反应溴化剂进行溴代反应,选择性高,产物易于分离。在非质子极性溶剂中进行胺化反应,反应时间短,溶剂无毒性,具有较高的应用价值。更多还原

【Abstract】 Objective:To synthesize 2-(3’,5’-difluorophenyl)-3,5-dimethyl-2-morpholinol hydroehloride.Methods:The target compound was synthesized from 3,5-difluoropropiophenone as a start- ing agent via several steps including bromination,amination,cyclization and acidification.Results:The total yield of the target compound was 77.3%.The structures were verified using IR and H~1-NMR spec- tra.Conclusion:The halogen substituent toα-H of arylalkyketone with cupric bromide was much highly selective.The amination in nonproton polar solvent without toxicity shortens reaction time.更多还原