(R)-2-amino-1-(3’-indolyl)butane | 10215-73-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (R)-2-amino-1-(3’-indolyl)butane
• 英文别名: (R)-1-(1H-indol-3-yl)butan-2-amine；(R)-α-ethyltryptamine；(-)-Etryptamine；Etryptamine, (R)-；(2R)-1-(1H-indol-3-yl)butan-2-amine
• CAS: 10215-73-3
• 化学式: C₁₂H₁₆N₂
• 分子量: 188.272
• InChiKey: ZXUMUPVQYAFTLF-SNVBAGLBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  41.8
• 氢给体数：
  2
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  (R)-2-amino-1-(3’-indolyl)butane 在 水 、 溶剂黄146 、 sodium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 、 甲苯 为溶剂， 反应 26.0h， 生成 (E)-3-(4-((3R)-3-ethyl-2-(tetrahydrofuran-3-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)-3,5-difluorophenyl)acrylic acid
  参考文献：
  名称：

  [EN] ESTROGEN RECEPTOR MODULATORS
  [FR] MODULATEURS DU RÉCEPTEUR DES ŒSTROGÈNES

  摘要：

  化合物的化学式（I）是雌激素受体α调节剂，其中化学式（I）中的变量在披露中有描述。这些化合物以及其药学上可接受的盐和组合物对于治疗依赖雌激素受体α和/或由雌激素受体α介导的疾病或症状是有用的，包括由细胞过度增殖所特征化的疾病，如乳腺癌。

  公开号：

  WO2017172957A1
• 作为产物：
  描述：

  1-Boc-吲哚 在 吡啶 、 N-溴代丁二酰亚胺(NBS) 、 正丁基锂 、 sodium azide 、 palladium 10% on activated carbon 、 氢气 、 苯甲醚 、 三氟乙酸 作用下， 以 四氢呋喃 、 甲醇 、 正己烷 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 91.17h， 生成 (R)-2-amino-1-(3’-indolyl)butane
  参考文献：
  名称：

  Alpha-ethyltryptamines as dual dopamine–serotonin releasers

  摘要：

  The dopamine (DA), serotonin (5-HT), and norepinephrine (NE) transporter releasing activity and serotonin-2A (5-HT2A) receptor agonist activity of a series of substituted tryptamines are reported. Three compounds, 7b, (+)-7d and 7f, were found to be potent dual DA/5-HT releasers and were > 10-fold less potent as NE releasers. Additionally, these compounds had different activity profiles at the 5-HT2A receptor. The unique combination of dual DA/5-HT releasing activity and 5-HT2A receptor activity suggests that these compounds could represent a new class of neurotransmitter releasers with therapeutic potential. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.07.062

文献信息

• PESTICIDAL COMPOSITION COMPRISING INDOLE DERIVATES
  申请人：Bednarek Pawel

  公开号：US20090028796A1

  公开（公告）日：2009-01-29

  The present invention is directed to pesticidal compositions comprising indole derivatives. These indole derivatives are especially active against phytopathogenic fungi. Furthermore, the invention relates to the use of indole derivatives for the production of pesticides and the use of the compositions according to the invention as pesticides. The present invention is also directed to a process for producing a pesticidal composition and to pesticidal compositions prepared by this process. In addition, the invention relates to a process for preventing or combating pests and to a process for protecting plants against pests, especially against phytopathogenic fungi. Further, the invention is directed to plants or seeds as well as objects or materials which have been protected against pests by treatment with a composition according to the invention. Further, the invention is directed to a method for identifying a substance having pesticidal activity. Further, the invention is directed to a method of identifying the mode of action of and/or of providing binding proteins for a pesticidal compound of the present invention. Finally, the invention is directed to a method for diagnosing pest infection of a plant and to the use of a pesticidal compound of the present invention as diagnostic markers.

  本发明涉及包含吲哚衍生物的杀虫组合物。这些吲哚衍生物特别对植物病原真菌具有活性。此外，本发明涉及使用吲哚衍生物制备杀虫剂以及使用本发明中的组合物作为杀虫剂。本发明还涉及制备杀虫组合物的过程以及通过该过程制备的杀虫组合物。此外，本发明还涉及预防或对抗害虫的过程以及保护植物免受害虫，特别是植物病原真菌的过程。此外，本发明还涉及经过本发明中的组合物处理后受到保护的植物或种子以及物体或材料。本发明还涉及识别具有杀虫活性的物质的方法。此外，本发明还涉及识别本发明中杀虫化合物的作用方式和/或提供结合蛋白的方法。最后，本发明涉及诊断植物害虫感染的方法以及使用本发明中的杀虫化合物作为诊断标记的方法。
• SUSPENSION FORMULATIONS
  申请人：Lewis David Andrew

  公开号：US20110182997A1

  公开（公告）日：2011-07-28

  The present invention relates to suspension formulations, especially those for delivering a pharmaceutically active agent in aerosol form using a spray or aerosol device, such as a pressurised metered dose inhaler (pMDI). The formulations may be for pulmonary, nasal, buccal or topical administration, but are preferably for pulmonary inhalation.

  本发明涉及悬浮液配方，特别是用于使用喷雾或气雾装置以气雾形式传递药物活性剂的配方，例如压力计量剂量吸入器（pMDI）。这些配方可以用于肺部、鼻部、颊部或局部给药，但最好用于肺部吸入。
• Treatment of Addiction and Impulse-Control Disorders Using PDE7 Inhibitors
  申请人：OMEROS CORPORATION

  公开号：US20130267502A1

  公开（公告）日：2013-10-10

  This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.

  本公开涉及使用磷酸二酯酶7（PDE7）抑制剂，单独或与其他治疗药物联合治疗成瘾和原发性冲动控制障碍。
• TAURINE COMPOSITIONS SUITABLE FOR INHALATION
  申请人：VECTURA LIMITED

  公开号：US20160051473A1

  公开（公告）日：2016-02-25

  The invention discloses spray-dried compositions for inhalation and methods for preparing such powder compositions. The compositions of the invention are produced by spray-drying taurine under conditions that (i) retain the physical and chemical stability of the composition during spray drying and upon storage, (ii) protect the powder composition from aggregation and (iii) provide particles suitable for aerosolisation.

  本发明公开了用于吸入的喷雾干燥组合物以及制备这种粉末组合物的方法。本发明的组合物是通过在保持组合物在喷雾干燥和储存期间的物理和化学稳定性，保护粉末组合物免受聚集，并为气溶胶化提供适当的颗粒的条件下，喷雾干燥牛磺酸而制成的。
• Inhaler
  申请人：Vectura Delivery Devices Limited

  公开号：EP2082767A1

  公开（公告）日：2009-07-29

  An inhaler (1) is disclosed. It comprises a housing (2) to receive a strip (3) having a surface (3a) and a plurality of blister pockets (5) depending from said surface. Each blister pocket contains a dose of medicament for inhalation by a user. The inhaler has a blister strip drive mechanism (7) including a blister strip drive member (27) shaped to contact the strip along a line defined by the crease (30) between a blister pocket and said surface, to drive said strip.

  本发明公开了一种吸入器（1）。它包括一个外壳（2），用于容纳一个具有表面（3a）的条状物（3）和多个与所述表面相连的水泡袋（5）。每个水泡袋中装有一定剂量的药物，供使用者吸入。吸入器有一个泡罩条驱动机构（7），包括一个泡罩条驱动部件（27），其形状是沿着泡罩袋和所述表面之间的折痕（30）所确定的线接触泡罩条，以驱动所述泡罩条。