(S)-1-苯基-1,2,3,4-四氢异喹啉的合成工艺研究  

Research on the synthesis of(S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline

作　　者：杨勇 陈安丰 何雷 刘学良 朱后田 YANG Yong;CHEN An-feng;HE Lei;LIU Xue-liang;ZHU Hou-tian(Jiangsu Hansoh Pharmaceutical Co.,Ltd.,Lianyungang 222000,China)

机构地区：[1]江苏豪森药业集团有限公司,江苏连云港222000

出　　处：《精细与专用化学品》2025年第2期52-55,共4页Fine and Specialty Chemicals

摘　　要：采用2-苯乙胺为起始原料,经酰化、环合及还原反应得到外消旋化合物1-苯基-1,2,3,4-四氢异喹啉(化合物5),化合物5经拆分、游离和精制得到(S)-1-苯基-1,2,3,4-四氢异喹啉(化合物1),总收率为35.8%(以2-苯乙胺计),纯度为99.8%,结构经MS、^(1)H-NMR确认。该合成工艺所用原料价格便宜且易得,操作简便,反应条件温和,所得成品纯度高,避免使用有毒重金属试剂,适合工业化生产。Using2-phenylethylamineasstarting material,the racemic compound 1-phenyl-1,2,3,4-tetrahydroisoquinoline(compound 5)was obtained through acylation,cyclization,and reduction reactions.(S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline(compound 1)was obtained by being split,freed,and refined,with a total yield of 35.8%(based on 2-phenylethylamine)and a purity of 99.8%.The structure was confirmed by MS and ^(1)H-NMR.The raw materials used in this synthesis process were cheap and easy to obtain,the operation was simple,the reaction conditions were mild,the resulting product has high purity,the use of toxic heavy metal reagents was avoided,which was suitable for industrial production.

关 键 词：2-苯乙胺 Bischler-Napieralski环合 拆分 索非那新 

分 类 号：TQ317[化学工程—高聚物工业] TQ463