acetic acid 2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenyl ester

• 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: acetic acid 2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenyl ester
• 英文别名: [2-[3-[Di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] acetate
• 化学式: C₂₄H₃₃NO₃
• 分子量: 383.531
• InChiKey: COPIGDPPLIVQTA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  28
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  49.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• SHORT SYNTHESIS OF TOLTERODINE, INTERMEDIATES AND METABOLITES
  申请人：Sterk Damjan

  公开号：US20130197082A1

  公开（公告）日：2013-08-01

  A process is described for the preparation of intermediates which can be used for preparation of agents for urinary incontinence therapy, specifically to 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol and its prodrugs.

  描述了一种制备中间体的过程，该中间体可用于制备尿失禁治疗剂，特别是用于制备2-(3-(二异丙基氨基)-1-苯基丙基)-4-(羟甲基)苯酚及其前药。
• [EN] NEW USES OF DIISOPROPYLAMINE DERIVATIVES<br/>[FR] NOUVELLES UTILISATIONS DE DÉRIVÉS DE DIISOPROPYLAMINE
  申请人：PFIZER LTD

  公开号：WO2010018484A1

  公开（公告）日：2010-02-18

  The invention provides a diisopropylamine derivative selected from: (a) a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof; and (b) a pharmaceutically acceptable ester prodrug of the compound of formula I, and its pharmaceutically acceptable salts and solvates; for use in the treatment of stress urinary incontinence or mixed urinary incontinence. A preferred diisopropylamine derivative is fesoterodine, or a pharmaceutically acceptable salt thereof.

  本发明提供了一种二异丙胺衍生物，所述二异丙胺衍生物选自：（a）式I的化合物，或其药学上可接受的盐或溶剂化物；以及（b）式I的药学上可接受的酯前药，以及其药学上可接受的盐和溶剂化物；用于治疗压力性尿失禁或混合性尿失禁。一种优选的二异丙胺衍生物是费索特罗丁或其药学上可接受的盐。
• 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。
• Novel derivatives of 3,3-diphenylpropylamines
  申请人：SCHWARZ PHARMA AG

  公开号：EP0957073A1

  公开（公告）日：1999-11-17

  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 concerns to provide novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to present drugs as oxybutynin and tolterodine, methods for preparing thereof, 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，本发明涉及提供新型抗心绞痛药物原药，与目前的药物（如奥昔布宁和托特罗定）相比，该原药具有更优越的药代动力学特性；提供其制备方法；提供含有这些原药的药物组合物；提供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。
• SYNTHESIS OF PHENOLIC ESTERS OF HYDROXYMETHYL PHENOLS
  申请人：Ennis Seth C.

  公开号：US20100168459A1

  公开（公告）日：2010-07-01

  The present invention provides a process for the production of a compound of formula (I) or a salt thereof, wherein R is hydrogen, a straight, branched or cyclic C 1 -C 6 alkyl group or an aryl group which may optionally be substituted. This process comprises: (a) reacting a compound of formula (II), with a compound of formula (III), wherein R is as defined above and X is a leaving group, in the presence of N,N-di-isopropylethylamine.