首页> 外国专利> A PROCESS FOR THE PREPARATION OF CIS-(1S,4S)-N-METHYL-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPHTHALENEAMINE HYDROCHLORIDE

A PROCESS FOR THE PREPARATION OF CIS-(1S,4S)-N-METHYL-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPHTHALENEAMINE HYDROCHLORIDE

机译:制备CIS-(1S,4S)-N-甲基-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘亚胺盐酸盐的方法

摘要

There is disclosed a process for the preparation of cis-(1S,4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine hydrochloride i.e. sertraline hydrochloride and the intermediate cis-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine hydrochloride, which comprises reacting 4-(3,4-dichlorophenyl)-3,4-dihydro-1-(2H)-naphthalenone with methylamine under reducing atmosphere in presence of reducing metal catalyst such as Raney Nickel to produce the intermediate amine, treating the said amine with hydrogen chloride to produce the corresponding cis and trans amine hydrochloride, isolating and purifying the said amine hydrochloride to obtain the intermediate cis-amine hydrochloride, and converting the said cis-amine hydrochloride into cis-(1S,4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine hydrochloride, by known process.
机译:公开了一种制备顺式(1S,4S)-N-甲基-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘胺盐酸盐即盐酸舍曲林的方法和中间体顺式-N-甲基-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘胺盐酸盐,包括使4-(3,4-二氯苯基)-3,4-二氢反应在还原气氛下,在还原金属催化剂如阮内镍的存在下,在还原气氛下用甲胺将-1-(2H)-萘酮与甲胺反应制得中间体胺,并用氯化氢处理所述胺​​,制得相应的顺式和反式胺盐酸盐,并分离纯化。所述胺盐酸盐得到中间体顺式胺盐酸盐,并将所述顺式胺盐酸盐转化为顺式-(1S,4S)-N-甲基-4-(3,4-二氯苯基)-1,2,3,4 -四氢-1-萘胺盐酸盐,通过已知方法。

著录项

  • 公开/公告号WO0116089A1

    专利类型

  • 公开/公告日2001-03-08

    原文格式PDF

  • 申请/专利权人 VYAS SHARAD KUMAR;

    申请/专利号WO2000IB01182

  • 发明设计人 VYAS SHARAD KUMAR;

    申请日2000-08-28

  • 分类号C07C209/26;

  • 国家 WO

  • 入库时间 2022-08-22 01:18:42

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