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作 者:余丹[1] 李翔[1] 刘小成[1] 邓嘉伦[1] 刘昱[1] 陈刚[1]
出 处:《化学与生物工程》2014年第5期54-56,共3页Chemistry & Bioengineering
摘 要:以5-氯-2-戊酮为原料,先进行羰基保护、与乙基乙醇胺反应之后脱保护,再进行羰基还原氨化,经4步反应合成5-(N-乙基-N-2-羟乙基胺)-2-戊胺(俗称羟基氯喹侧链),总收率53.8%,纯度99.0%(GC)。重要原料乙基乙醇胺回收率达95%。5-(N-Ethyl-N-2-hydroxyethylamino)-2-pentylamine,which was called as hydroxychloroquine side chain,an important intermediate of hydroxychloroquine,was synthesized from 5-chloro-2-pentanone through four steps including ketalization reaction with monoethylene glycol,condensation with N-ethyl-N-2-hydroxyethyl amine,then hydrolysis in acidic condition and reductive amination in the ammonical alcoholic solvent in the presence of Raney Ni under hydrogen pressure.The overall yield of 5-(N-ethyl-N-2-hydroxyethylamino)-2-pentylamine was 53.8% and its purity was 99.0%,and the recovery rate of excess N-ethyl-N-2-hydroxyethyl amine was 95%.
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