(E)-4-bromophenyl cinnamate | 1104411-50-8

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: (E)-4-bromophenyl cinnamate
• 英文别名: 4-Bromophenyl 3-phenylacrylate；(4-bromophenyl) (E)-3-phenylprop-2-enoate
• CAS: 1104411-50-8
• 化学式: C₁₅H₁₁BrO₂
• 分子量: 303.155
• InChiKey: FXZAPECDHLNXCB-IZZDOVSWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  (2Z)-2-bromo-3-phenyl-2-propenal 、 4-溴苯酚 在 1,3-二苄基-1H-苯并[D]咪唑-3-氯化物 、 caesium carbonate 作用下， 以 1,4-二氧六环 为溶剂， 反应 3.0h， 以50%的产率得到(E)-4-bromophenyl cinnamate
  参考文献：
  名称：

  NHC-catalyzed C–O or C–N bond formation: efficient approaches to α,β-unsaturated esters and amides

  摘要：

  简单高效的NHC催化转化，通过C-O或C-N键形成，将溴代烯酸或α,β-二溴代烯酸高立体选择性地转化为α,β-不饱和酯或酰胺。NHC催化的过程在温和条件下进行。起始原料易于获得，避免使用外部氧化剂，以及产品的实用价值，都使这一策略具有吸引力。

  DOI：

  10.1039/c2cc32862c

文献信息

• [EN] A PROCESS FOR PREPARING FESOTERODINE<br/>[FR] PROCÉDÉ DE PRÉPARATION DE FÉSOTÉRODINE
  申请人：ALEMBIC PHARMACEUTICALS LTD

  公开号：WO2012137047A1

  公开（公告）日：2012-10-11

  The present invention relates to an improved process for the preparation of Fesoterodine and pharmaceutically acceptable salts thereof. The present invention particularly relates to a process for the preparation of fesoterodine and pharmaceutically acceptable salts thereof which involves use and preparation of R(+) benzyl tolterodine and fumarate salt of R(+)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol.

  本发明涉及一种改进的制备Fesoterodine及其药用盐的方法。本发明特别涉及一种制备Fesoterodine及其药用盐的方法，其中涉及使用和制备R(+)苄基托特罗定和R(+)-[4-苄氧基-3-(3-二异丙基氨基-1-苯基丙基)-苯基]-甲醇富马酸盐。
• 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。
• PROCESS FOR PREPARING FESOTERODINE
  申请人：Raman Jayaraman Venkat

  公开号：US20140039216A1

  公开（公告）日：2014-02-06

  The present invention relates to an improved process for the preparation of Fesoterodine and pharmaceutically acceptable salts thereof. The present invention particularly relates to a process for the preparation of fesoterodine and pharmaceutically acceptable salts thereof which involves use and preparation of R(+)benzyl tolterodine and fumarate salt of R(+)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol.

  本发明涉及一种改进的制备Fesoterodine及其药学上可接受的盐的方法。本发明特别涉及一种制备Fesoterodine及其药学上可接受的盐的方法，其中涉及使用和制备R（+）苄基托吡啶和R（+）-[4-苄氧基-3-(3-二异丙基氨基-1-苯基丙基)-苯基]-甲醇富马酸盐。
• 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。