单烷基取代苯基哌嗪衍生物的合成  

Synthesis of Monoalkyl Substituted Phenylpiperazine Derivatives

作　　者：白宝清[1] 袁牧[1] 周欣[1] 

机构地区：[1]广州医学院药物研究中心,广东广州510182

出　　处：《精细化工》2007年第8期823-825,共3页Fine Chemicals

基　　金：国家自然科学基金资助项目(30060087)~~

摘　　要：单烷基取代苯基哌嗪衍生物是合成苯基哌嗪类化合物的重要中间体。以二乙醇胺为起始原料,在10℃滴加氯化亚砜,室温反应1 h,再于60℃反应5 h,经氯代反应制得β,β′-二氯代二乙胺盐酸盐,然后分别与2-甲基苯胺、4-叔丁基苯胺、4-甲基苯胺在130℃反应50 h,得2-甲基苯基哌嗪盐酸盐、4-叔丁基苯基哌嗪盐酸盐、4-甲基苯基哌嗪盐酸盐3个目标化合物,收率分别为78%、61%、67%。其结构经1HNMR、13CNMR、MS证实与目标化合物的结构一致。Alkyl substituted phenylpiperazine derivatives are important intermediates of phenylpiperazine compounds. Thionyl chloride was dropped into diethanolamine at 10 ℃, and the resulting mixture was stirred at 10℃ for 1 h and at 60 ℃ for 5 h to afford β,β＇-dichlorodiethylamine hydrochloride,which then reacted separately with 2-methylphenylamine,4-tert-butylphenylamine and 4- methylphenylamine at 130 ℃ for 50 h to afford three monoalkyl substituted phenylpiperazine derivatives 2-methylphenylpiperazine,4-tert-butylphenylpiperazine and 4-methylphenylpiperazine in 78%, 61% and 67% yield respectively. The synthesized compounds were identified by 1^ HNMR, 13^CNMR and MS to be consistent with the proposed structures.

关 键 词：二乙醇胺 β β'-二氯代二乙胺盐酸盐 苯基哌嗪 药物中间体 

分 类 号：TQ463.54[化学工程—制药化工]