首页> 外国专利> METHOD OF TRANSFORMING TRANS-ISOMERIC N-METHYL-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPHTALENE AMINE INTO CIS-ISOMERIC ONE

METHOD OF TRANSFORMING TRANS-ISOMERIC N-METHYL-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPHTALENE AMINE INTO CIS-ISOMERIC ONE

机译:将反式N-甲基-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘胺转化为CIS-异构体一的方法

摘要

A novel process for converting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine to cis-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine is disclosed. The process involves contacting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine, or a mixture of same with up to about an equal part by weight of the corresponding cis-isomer, with a basic equilibration agent like potassium tert.-butoxide in a reaction-inert polar organic solvent to ultimately afford a cis/trans-mixture wherein the amount of cis-amine present in said mixture achieves a constant value of about 2:1 on a weight-by-weight basis. The aforesaid resultant mixture is useful as an intermediate product that ultimately leads to pure cis-(1S) (4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenea mine (sertraline), which is a known antidepressant agent.
机译:将反式异构N-甲基-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘胺转化为顺式异构N-甲基-4-(3,4-公开了二氯苯基)-1,2,3,4-四氢-1-萘胺。该方法涉及使反式异构体N-甲基-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘胺或它们的混合物与最多约等重量份的相应的顺式异构体,与碱性平衡剂(如叔丁醇钾)在反应惰性的极性有机溶剂中反应,最终得到一种顺式/反式混合物,其中所述混合物中存在的顺式胺量达到恒定值重量比约为2:1。上述所得混合物可用作最终产生纯的顺式-(1S)(4S)-N-甲基-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-基的中间产物。萘矿(sertraline),是一种已知的抗抑郁药。

著录项

  • 公开/公告号PL166756B1

    专利类型

  • 公开/公告日1995-06-30

    原文格式PDF

  • 申请/专利权人 PFIZER INC;

    申请/专利号PL19920300586

  • 发明设计人 BRAISH TAMIM F.;

    申请日1992-02-07

  • 分类号C07C211/38;C07C209/68;

  • 国家 PL

  • 入库时间 2022-08-22 04:18:36

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号