4-[2-(4-Fluoro-phenyl)-ethyl]-phenylamine | 64583-46-6

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 4-[2-(4-Fluoro-phenyl)-ethyl]-phenylamine
• 英文别名: 4-[2-(4-fluorophenyl)ethyl]aniline
• CAS: 64583-46-6
• 化学式: C₁₄H₁₄FN
• 分子量: 215.27
• InChiKey: WXLZJFFGXPLTEZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-[2-(4-Fluoro-phenyl)-ethyl]-phenylamine 生成 3-[4-[2-(4-Fluorophenyl)ethyl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
  参考文献：
  名称：

  DOSTERT, P.;LACOUR, A.;LANGLOIS, M.;STROLIN-BENEDETTI, M.

  摘要：

  DOI：
• 作为产物：
  描述：

  (E)-4-fluoro-4’-nitrostilbene 在 钯 作用下， 以yields the 4-[2-(4-fluoro-phenyl)-ethyl]-phenylamine as a light red solid的产率得到4-[2-(4-Fluoro-phenyl)-ethyl]-phenylamine
  参考文献：
  名称：

  4-Pyrrolidino-phenyl-benzyl ether derivatives

  摘要：

  该发明涉及外消旋或对映纯的4-吡咯烷基衍生物，其制备方法，包含该衍生物的制药组合物，以及它们在预防和治疗疾病方面的应用，特别是通过单胺氧化酶B抑制剂介导的疾病，特别是阿尔茨海默病或老年性痴呆症。

  公开号：

  US07037935B2

文献信息

• [EN] N-ACYLAMINOBENZENE DERVATIVES AS SELECTIVE MONOAMINE OXIDASE B INHIBITORS<br/>[FR] DERIVES DE N-ACYLAMINOBENZENE COMME INHIBITEURS DE LA MONOAMINE OXYDASE B SELECTIFS
  申请人：HOFFMANN LA ROCHE

  公开号：WO2003099763A1

  公开（公告）日：2003-12-04

  This invention relates to N-acylamino aryl derivatives of the general formula (I), wherein R1 is halogen, halogen-(C1-C6)-alkyl, cyano, C1-C6-alkoxy or halogen-(C1-C6)-alkoxy; R21, R22, R23 and R24 independently from each other are selected from the group consisting of hydrogen, (C1-C6)-alkyl, halogen, halogen-(C1-C6)-alkyl, hydroxy, C1-C6-alkoxy or -CHO; R3 is hydrogen or C1-C3-alkyl; R4, R5 independently from each other are selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-alkoxy or -COO(C1-C6)alkyl; or R4 and R5 form together with the C-atom to which they are attach a C3-C7-cycloalkyl ring; R6 is -CO-NR7R8; -COO(C1-C6)-alkyl, -CN, -NR2 or -NHC(O)R; R7 and R8 independently from each other are selected from the group consisting of hydrogen, C1-C6-alkyl, NH2 or hydroxy; R is hydrogen or C1-C6-alkyl; n is 0, 1, 2 or 3. X is -CHRO, -OCHR, -CH2S-, -SCH2-, -CH2CH2-, -CH=CH- or -C≡C-; and to pharmaceutically active acid addition salts thereof. It has been found that the compounds of general formula (I) are selective monoamine oxidase B inhibitors and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B inhibitors, for example for the treatment of Alzheimer’s disease or senile dementia.

  这项发明涉及一般式(I)的N-酰氨基芳基衍生物，其中R1是卤素，卤代-(C1-C6)-烷基，氰基，C1-C6-烷氧基或卤代-(C1-C6)-烷氧基；R21、R22、R23和R24彼此独立地选自氢，(C1-C6)-烷基，卤素，卤代-(C1-C6)-烷基，羟基，C1-C6-烷氧基或-CHO的群；R3是氢或C1-C3-烷基；R4、R5彼此独立地选自氢，C1-C6-烷基，C1-C6-烷氧基或-COO(C1-C6)烷基的群；或R4和R5与它们连接的C原子一起形成一个C3-C7-环烷基环；R6是-CO-NR7R8；-COO(C1-C6)-烷基，-CN，-NR2或-NHC(O)R；R7和R8彼此独立地选自氢，C1-C6-烷基，NH2或羟基；R是氢或C1-C6-烷基；n为0、1、2或3。X是-CHRO，-OCHR，-CH2S-，-SCH2-，-CH2CH2-，-CH=CH-或-C≡C-；以及其药用活性酸盐。已发现一般式(I)的化合物是选择性单胺氧化酶B抑制剂，因此它们在治疗由单胺氧化酶B抑制剂介导的疾病中很有用，例如用于治疗阿尔茨海默病或老年性痴呆症。
• N-acylamino benzyl ether derivatives
  申请人：——

  公开号：US20030232883A1

  公开（公告）日：2003-12-18

  This invention relates to N-acylamino aryl derivatives of the formula 1 where R 1 , R 21 , R 22 , R 23 , R 3 , R 4 , R 5 R 6 , R 7 , R 8 , R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH 2 S—, —SCH 2 —, —CH 2 CH 2 —, —CH═CH— or —C≡C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.

  这项发明涉及公式1的N-酰氨基芳基衍生物，其中R1、R21、R22、R23、R3、R4、R5、R6、R7、R8、R和n如本文所定义，且X为—CHRO、—OCHR—、—CH2S—、—SCH2—、—CH2CH2—、—CH═CH—或—C≡C—。该发明的化合物是选择性的单胺氧化酶B抑制剂，因此它们在治疗由单胺氧化酶B介导的疾病中具有用途，例如用于治疗阿尔茨海默病或老年性痴呆症。
• 4-Pyrrolidino-phenyl-benzyl ether derivatives
  申请人：——

  公开号：US20040106650A1

  公开（公告）日：2004-06-03

  The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.

  本发明涉及外消旋或对映纯的4-吡咯烷基衍生物，其制备方法，包含该衍生物的制药组合物，以及它们在预防和治疗疾病方面的应用，特别是通过单胺氧化酶B抑制剂介导的疾病，特别是阿尔茨海默病或老年性痴呆症。
• Gascoyne,J.M. et al., Journal of the Chemical Society. Perkin transactions II, 1977, p. 1051 - 1057
  作者：Gascoyne,J.M. et al.

  DOI：——

  日期：——
• DOSTERT, P.;LACOUR, A.;LANGLOIS, M.;STROLIN-BENEDETTI, M.
  作者：DOSTERT, P.、LACOUR, A.、LANGLOIS, M.、STROLIN-BENEDETTI, M.

  DOI：——

  日期：——