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phenylethanolamino and phenylethanolaminomethyltetraline, procedures in the manufacture of intermediates thereof and pharmaceutical compositions containing them.

机译:苯乙醇氨基和苯乙醇氨基甲基四氢呋喃,其中间体的制备方法以及含有它们的药物组合物。

摘要

Phenylethanolamino- and phenylethanolaminomethyl-tetralins of formula (I) IMAGE in which X represents a hydrogen atom, a halogen atom, a (C1-C4)alkyl group or a trifluoromethyl group, A represents a bond between the group -COOR and the tetralin ring, a (C1-C4)alkylene group or a (C2-C4)alkenylene group, R is a hydrogen atom or a (C1-C4)alkyl group, and n is 0 or 1 and their salts, are prepared, for example, by reaction of an epoxide of formula (IIa) IMAGE with a tetralin of formula (III) IMAGE in which A and n are as defined above and R' is a (C1-C4)alkyl group, if appropriate followed by a basic hydrolysis to give the compounds (I) where R is hydrogen. The novel compounds have very advantageous properties as antidepressant agents and intestinal spasmolytics. The novel intermediates of formula (III) are also claimed.
机译:式(I)的苯基乙醇氨基-和苯基乙醇氨基甲基-四氢萘酚(IMAGE),其中X表示氢原子,卤素原子,(C1-C4)烷基或三氟甲基,A表示-COOR基团与-COOR之间的键。制备四氢萘环,(C1-C4)亚烷基或(C2-C4)亚烯基,R为氢原子或(C1-C4)烷基,n为0或1及其盐。例如,通过使式(IIa)的环氧化物与式(III)的四氢化萘进行反应,其中A和n如上所定义且R'为(C1-C4)烷基然后进行碱性水解,得到化合物(Ⅰ),其中R是氢。该新型化合物作为抗抑郁药和肠解痉剂具有非常有利的性质。还要求保护式(III)的新型中间体。

著录项

  • 公开/公告号AT121723T

    专利类型

  • 公开/公告日1995-05-15

    原文格式PDF

  • 申请/专利权人 SANOFI;

    申请/专利号AT19920400416T

  • 申请日1992-02-17

  • 分类号C07C229/50;A61K31/24;C07C271/24;A61K31/325;C07C229/34;

  • 国家 AT

  • 入库时间 2022-08-22 04:17:14

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