N-乙基-2-氨甲基吡咯烷的合成  

Synthesis of N-ethyl-2-aminomethyl pyrrolidine

作　　者：吴廷照[1] 朱占元[1] 

机构地区：[1]江苏淮阴华新药业有限公司,江苏淮阴223002

出　　处：《应用化工》2001年第4期33-34,共2页Applied Chemical Industry

摘　　要：以四氢糠醇为原料 ,合成了抗精神病药舒必利的重要中间体N 乙基 2 氨甲基吡咯烷。本工艺共有六步。首先 ,四氢糠醇用氯化亚砜氯化制成四氢糠氯 ,再经加压氨化制成四氢糠氨 ,压力 0 .7MPa～ 1.0MPa;然后用苯甲酰氯保护氨基 ,用氯化亚砜开环 ,与乙胺 ( 70 % )环合 ;最后经盐酸 ( 3 0 % )水解。总收率 3 7%。N Ethyl 2 aminomethyl pyrrolidine which is a useful intermediate for the synthesis of sulpiride,an important antipsychotic agent,was synthesiszed from tetrahydrofurfuryl alcohol.The procedure involved six steps.Firstly,tetrahydrofurfuryl alcohol was chlorizated with thionyl chloride to produce tetrahydrofurfuryl chloride,then,tetrahydrofurfuryl amine was preparated by ammoniation under pressure of 0.7 MPa～1.0 MPa and the amino was protected with benzoyl chloride,finally,decyclization with thionyl chloride,cyclization with ethyl amine(70%),hydrolyzed with hydrochloric acid(30%).The overall yield was 37%.

关 键 词：N-乙基-2-氨甲基吡咯烷 四氢糠胺 合成 抗精神病药 中间体 

分 类 号：TQ251.3[化学工程—有机化工] TQ460.4