首页> 外国专利> Stereoselective hydrogenation process for preparing cis-6-phenyl-5- 4- (2-pyrrolidin-1-yl-ethoxy) -phenyl 2-methoxy-5,6,7,8-tetrahydronaphthalene hydrochloride.

Stereoselective hydrogenation process for preparing cis-6-phenyl-5- 4- (2-pyrrolidin-1-yl-ethoxy) -phenyl 2-methoxy-5,6,7,8-tetrahydronaphthalene hydrochloride.

机译:立体选择性加氢制备顺式6-苯基-5- [4-(2-吡咯烷-1-基-乙氧基)-苯基] 2-甲氧基-5,6,7,8-四氢萘盐酸盐的方法。

摘要

A process for preparing cis-6-phenyl-5- [4- (2-pyrrolidin-1-yl-ethoxy) -phenyl] -2-methoxy 5,6,7,8-tetrahydronaphthalene hydrochloride, comprising said cis-6-phenyl -5- [4- (2-pyrrolidin-1-yl-ethoxy) -phenyl] -2-methoxy-5,6,7,8-tetrahydronaphthalene hydrochloride contains less than 2.5% of 1- {2- [4- (6- methoxy-2-phenyl-naphthalen-1-yl) -phenoxy] -ethyl} -pyrrolidine hydrochloride, the method, in the following order, the steps of: (a) charging a hydrogenation reaction vessel with a catalyst suitable hydrogenation and a solution of 1- {2- [4- (6-methoxy-2-phenyl-3,4-dihydro-1-yl) phenoxy] ethyl} pyrrolidine hydrochloride in a suitable solvent; (B) pressurizing the hydrogenation reaction vessel with hydrogen to a pressure of 137.9 to 689.4 kPa to provide a hydrogenation reaction mixture; (B) (c) heating the hydrogenation reaction mixture of step (b) at a temperature of 45 to 55 until it is 1% or less of 1- {2- [4- (6-methoxy-2- phenyl-3,4dihidronaftaleno-1 yl) phenoxy] ethyl} pyrrolidine hydrochloride remains to provide cis-6-phenyl-5- [4- (2-pyrrolidin-1-yl-ethoxy) -phenyl] -2-methoxy-5,6,7 , 8-tetrahydronaphthalene hydrochloride: (d) isolating the cis-6 phenyl-5- [4- (2-pyrrolidin-1-yl-ethoxy) -phenyl] -2-methoxy-5,6,7,8-tetrahydronaphthalene hydrochloride in wherein the cis-6-phenyl-5- [4- (2-pyrrolidin-1-yl-ethoxy) phenyl] -2-methoxy-5,6,7,8-tetrahydronaphthalene hydrochloride contains less resulting 2.5% 1 {2- [4- (6-methoxy-2-phenyl-naphthalen-1-yl) phenoxy] -ethyl} -pyrrolidine hydrochloride.
机译:一种制备顺式6-苯基-5- [4-(2-吡咯烷-1-基-乙氧基)-苯基] -2-甲氧基5,6,7,8-四氢萘盐酸盐的方法,该方法包括所述顺式6-苯基-5- [4-(2-吡咯烷-1-基-乙氧基)-苯基] -2-甲氧基-5,6,7,8-四氢萘盐酸盐含有少于2.5%的1- {2- [4- (6-甲氧基-2-苯基-萘-1-基)-苯氧基]-乙基}-吡咯烷盐酸盐,该方法按以下顺序进行以下步骤:(a)在氢化反应容器中加入适合的氢化催化剂以及1- {2- [4-(6-甲氧基-2-苯基-3,4-二氢-1-基)苯氧基]乙基}吡咯烷盐酸盐在适当溶剂中的溶液; (B)用氢气将氢化反应容器加压至137.9〜689.4kPa的压力,得到氢化反应混合物。 (B)(c)在45-55℃的温度下加热步骤(b)的氢化反应混合物,直至其为1- {2- [4-(4-(6-甲氧基-2-苯基-3,保留4dihidronaftaleno-1(基)苯氧基]乙基}吡咯烷盐酸盐,以提供顺式-6-苯基-5- [4-(2-吡咯烷-1-基-乙氧基)-苯基] -2-甲氧基-5,6,7, 8-四氢萘盐酸盐:(d)分离出顺式-6苯基-5- [4-(2-吡咯烷-1-基乙氧基)-苯基] -2-甲氧基-5,6,7,8-四氢萘盐酸盐其中顺式-6-苯基-5- [4-(2-吡咯烷-1-基-乙氧基)苯基] -2-甲氧基-5,6,7,8-四氢萘盐酸盐含有更少的2.5%1 {2- [4-(6-甲氧基-2-苯基-萘-1-基)苯氧基]-乙基}-吡咯烷盐酸盐。

著录项

  • 公开/公告号ES2350853T3

    专利类型

  • 公开/公告日2011-01-27

    原文格式PDF

  • 申请/专利权人 PFIZER PRODUCTS INC.;

    申请/专利号ES20060779787T

  • 发明设计人 TABER GERALDINE P.;LEHNER RICHARD SHELTON;

    申请日2006-06-12

  • 分类号C07D295/08;

  • 国家 ES

  • 入库时间 2022-08-21 18:02:49

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