【作者】 曹高； 胡艾希；

【Author】 Cao Gao Hu Ai-xi* ( The School of Chemical and Energy Engineering, South China University of Technology, Guangzhou 510640)

【机构】 华南理工大学化工与能源学院；

【摘要】 目的合成目标化合物2-芳基-3,5-二甲基-2-吗啉醇及其盐酸盐,并研究其抗抑郁活性。方法选择手性2-氨基丙醇分别与α-溴苯丙酮、α-溴-3-氯苯丙酮、α-溴-4-苄氧基苯丙酮和6-甲氧基-2-(2-溴丙酰基)萘反应,不对称合成2-芳基-3,5-二甲基-2-吗啉醇及其盐酸盐。用小鼠强迫游泳药理实验模型检查标题化合物的抗抑郁活性。结果盐酸2-芳基-3,5-二甲基-2-吗啉醇的收率为56%~77%。其结构经1HNMR、IR、MS确证。典型化合物的绝对构型由X-单晶衍射确定。结论小鼠强迫游泳药理实验模型结果显示被检测化合物具有良好的抗抑郁活性。更多还原

【Abstract】 OBJECTIVE To study the asymmetric synthesis and antidepressing activities of 2-Aryl -3,5-dimethyl-2-morpholinols hydrochloride. METHODS 2-Aryl-3,5-dimethyl-2-morpholingols were synthesized from the reactions of chiral 2-aminopropan-1-ol with 2-bromo-1- phenylpropan-1-one, 2- bromo-1-(3-chlorophenyl)propan-1-one, 1-(4-(benzyloxy)phenyl)-2-bromopropan-1-one and 2-bromo-1- (6-methoxynaphthalen-2-yl)propan-1-one, respectively. The antidepressing activities of the title compounds were assayed by the mouse forced swimming test (FST). RESULTS The 2-aryl-3,5-dimethyl-2- morpholinols were reacted with hydrochloride to give the hydrochloride salt with yields of 56%~77%. The structures of the products were proved by means of their 1H NMR, IR, MS spectroscopic data and X-ray crystal structure analysis. CONCLUSION The FST results confirm antidepressant proprieties of the title compounds.更多还原