摘要
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。
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, ^1H-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.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2006年第6期461-463,共3页
Chinese Journal of Modern Applied Pharmacy
基金
湖南省科技计划资助项目(04SK3053-3)
