(S)-N,N-diisopropyl-3-(2-benzyloxy-5-bromophenyl)-3-phenylpropanamine | 156755-28-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (S)-N,N-diisopropyl-3-(2-benzyloxy-5-bromophenyl)-3-phenylpropanamine
• 英文别名: (3S)-3-(5-bromo-2-phenylmethoxyphenyl)-3-phenyl-N,N-di(propan-2-yl)propan-1-amine
• CAS: 156755-28-1
• 化学式: C₂₈H₃₄BrNO
• 分子量: 480.488
• InChiKey: UCYJWCSOSZIQLQ-SANMLTNESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.8
• 重原子数：
  31
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (S)-N,N-diisopropyl-3-(2-benzyloxy-5-bromophenyl)-3-phenylpropanamine 、 乙烯 、 三(邻甲基苯基)磷 在 palladium diacetate sodium hydroxide 、 三正丁胺 、 氨 作用下， 以 甲醇乙酸乙酯 、 异丁酰胺 、 水 、 甲苯 为溶剂， 以1 g (18%)的产率得到(S)-N,N-Diisopropyl-3-(2-benzyloxy-5-ethenylphenyl)-3-phenylpropanamine
  参考文献：
  名称：

  Therapeutically active diarylpropylamines; their pharmaceutically acceptable salts; a method for their preparation and method for their use

  摘要：

  该发明涉及以下式（I）的新化合物，其中R1、R2、R3、R4、R5、R6、R7和Ar如权利要求1中所定义，它们与生理学上可接受的酸盐形式，当该化合物可以是光学异构体形式时，包括消旋混合物和各个对映体。这些化合物具有抗胆碱能活性，该发明还涉及式（I）的化合物，使用式（I）的化合物制备抗胆碱药物，使用式（I）的化合物治疗尿道失禁，以及制备式（I）的化合物的方法。

  公开号：

  US06313132B1

文献信息

• [EN] PROCESS FOR OBTAINING 3,3-DIPHENYLPROPYLAMINES<br/>[FR] PROCÉDÉ POUR L'OBTENTION DE 3,3-DIPHÉNYLPROPYLAMINES
  申请人：RAGACTIVES S L U

  公开号：WO2011012584A1

  公开（公告）日：2011-02-03

  The invention relates to a process for obtaining 3,3- diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, comprising a chemoselective reduction of the acid group against the ester group in compounds of general formula (V), wherein R1 is C1-C8 alkyl; and R3 and R4, independently of one another, represent H or C1-C8 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound. The invention also relates to the compounds of formula (V), as well as their enantiomers, solvates and salts.

  该发明涉及一种用于获得通式（I）所示的3,3-二苯基丙胺，特别是非索特罗定（Fesoterodine）的过程，以及它们的对映体、溶剂合物和盐，包括在通式（V）所示化合物中对酸基进行化学选择性还原以对抗酯基，其中R1为C1-C8烷基；R3和R4，彼此独立地，代表H或C1-C8烷基，或者一起与它们结合的氮形成一个由3到7个成员组成的环。该发明还涉及通式（V）所示的化合物，以及它们的对映体、溶剂合物和盐。
• Novel derivatives of 3,3-diphenylpropylamines
  申请人：Schwarz Pharma AG

  公开号：US20040186061A1

  公开（公告）日：2004-09-23

  The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compouds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

  本发明涉及3,3-二苯基丙胺衍生物的新型衍生物，其制备方法，含有新型化合物的药物组合物以及用于制备药物的化合物的用途。更具体地说，本发明涉及优于现有药物如奥克西布丁和托尔特罗定的抗胆碱药物的新型前药，其药代动力学性质更优，其制备方法，含有它们的药物组合物，一种使用所述化合物和组合物治疗尿失禁，胃肠道过度活跃（肠易激综合征）和其他平滑肌收缩症状的方法。
• NOVEL DERIVATIVES OF 3,3-DIPHENYLPROPYLAMINES
  申请人：Meese Claus

  公开号：US20090042981A1

  公开（公告）日：2009-02-12

  The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

  本发明涉及3,3-二苯基丙胺的新衍生物，其制备方法，含有新化合物的药物组成物以及用于制备药物的化合物的使用。更具体地说，本发明涉及抗胆碱能药物的新型前药，其药代动力学性质优于现有药物，如奥沙利铂和托尔吡啶，其制备方法，含有它们的药物组成物，使用上述化合物和组成物治疗尿失禁，胃肠道高活性（肠易激综合征）和其他平滑肌收缩症状的方法。
• Derivatives of 3,3-diphenylpropylamines
  申请人：SCHWARZ PHARMA AG

  公开号：EP1254890A1

  公开（公告）日：2002-11-06

  The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

  本发明涉及 3,3-二苯基丙胺的新型衍生物、其制备方法、含有该新型化合物的药物组合物以及使用该化合物制备药物。更具体地说，本发明涉及与现有药物（如奥昔布宁和托特罗定）相比具有更优越的药代动力学特性的新型抗心绞痛药物原药、其制备方法、含有这些原药的药物组合物、使用所述化合物和组合物治疗尿失禁、胃肠动力亢进（肠易激综合征）和其他平滑肌收缩疾病的方法。
• Process for obtaining 3,3-diphenylpropylamines
  申请人：Ragactives, S.L.U.

  公开号：EP2281801A1

  公开（公告）日：2011-02-09

  The invention relates to a process for obtaining 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, comprising a chemoselective reduction of the acid group against the ester group in compounds of general formula (V), wherein R1 is C1-C8 alkyl; and R3 and R4, independently of one another, represent H or C1-C8 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound. The invention also relates to the compounds of formula (V), as well as their enantiomers, solvates and salts.

  本发明涉及一种获得通式(I)的 3,3-二苯基丙胺，特别是非索特罗定，以及它们的对映体、溶液剂和盐的工艺，包括通式(V)化合物中酸基对酯基的化学选择性还原，其中 R1 是 C1-C8 烷基；R3 和 R4 相互独立地代表 H 或 C1-C8 烷基，或与它们结合的氮一起形成 3 至 7 个成员的环。本发明还涉及式（V）化合物及其对映体、溶剂和盐。