3-甲基-5-苯基-2-芳基-2-吗啉醇盐酸盐的合成

目的合成3-甲基-5-苯基-2-芳基-2-吗啉醇盐酸盐。方法以安非他酮在人体内的活性代谢物羟基安非他酮为先导化合物,利用化合物2-苯基-2-氨基-1-乙醇与2-溴-3-氯苯丙酮,2-溴苯丙酮,6-甲氧基-2-(2-溴丙酰基)萘反应,合成了吗啉环上5位含苯基的新型吗啉醇类化合物3-甲基-5-苯基-2-(3-氯苯基)-2-吗啉醇,3-甲基-2,5-二苯基-2-吗啉醇,3-甲基-5-苯基-2-(6-甲氧基-2-萘基)-2-吗啉醇,经氯化氢酸化后得到其盐酸盐。结果总收率分别为72.5%,78.6%,68.4%,目标化合物结构经IR,1H-NMR,MS确证。结论本法合成2-芳基-2-吗啉醇类化合物反应时间短,溶剂无毒性,具有较高的应用价值,为开发新的2-芳基-2-吗啉醇类抗抑郁症药物提供了一条新的合成工艺。

Synthesis of 2-Aryl-3-methyl-5-phenyl-2-morpholinol hydrochloride

OBJECTIVE To synthesize 2-Aryl-3-methyl-5-phenyl-2-morpholinol hydrochloride.METHODS 2-Aryl-3-methyl-5-phenyl-2-morpholinol were synthesized via the reactions of 2-amino-2-phenyl-1-alcohol with 2-bromo-3-chloropropiophenone,2-bromopropiophenone,6-methoxy-2-(2-Bromopropionyl)naphthalene,2-Aryl-3-methyl-5-phenyl-2-morpholinol reacted with hydrochloride to obtain the hydrochloride salts; RESULTS The totle yield amounted to 72.5 %,78.6 %,68.4 %,respectively,the structures of target compounds were confirmed by IR,~(1)H-NMR ,MS spectra.CONCLUSION The synthesis method of 2-aryl-2-morpholinol in the article have advantages of shortening reaction time,low-toxicity.And it provide a new synthesis method for developping new antidepression drugs of 2-aryl-2-morpholinol.