2-methyl-4-(oxiran-2-ylmethoxy)-1H-indole | 62119-47-5

• 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: 2-methyl-4-(oxiran-2-ylmethoxy)-1H-indole
• CAS: 62119-47-5
• 化学式: C₁₂H₁₃NO₂
• 分子量: 203.241
• InChiKey: GWRBPJXLXXKTEL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  37.6
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-methoxy-α,α,2-trimethyl-1H-indole-3-ethanamine 、 2-methyl-4-(oxiran-2-ylmethoxy)-1H-indole 以 乙醇 为溶剂， 反应 5.0h， 生成 1-[2-(5-Methoxy-1H-indol-3-yl)-1,1-dimethyl-ethylamino]-3-(2-methyl-1H-indol-4-yloxy)-propan-2-ol; hydrochloride
  参考文献：
  名称：

  Synthesis of indolyloxypropanolamines bearing the 2-(1H-indol-3yl)-1,1-dimethylethyl group: structure—activity studies and anti-hypertensive activity

  摘要：

  DOI：

  10.1016/0223-5234(88)90161-4

文献信息

• Indole derivatives for the treatment of depression and anxiety
  申请人：——

  公开号：US20040006229A1

  公开（公告）日：2004-01-08

  The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine. 1

  本发明提供了以下化合物的公式（I）：这些化合物对治疗抑郁症、焦虑症，并缓解因戒烟或部分戒烟引起的症状非常有用。
• Studies on Agents with Vasodilator and ,B-Blocking Activities. IV.
  作者：Toshimi SEKI、Tomio NAKAO、Takeshi MASUDA、Kohichi HASUMI、Kotaro GOTANDA、Tsutomu ISHIMORI、Seijiro HONMA、Nobuyoshi MINAMI、Kenyu SHIBATA、Kikuo YASUDA

  DOI：10.1248/cpb.44.2061

  日期：——

  A series of novel pyridazinone derivatives (II) having a phenoxypropanolamine moiety was synthesized. Their hypotensive and β-blocking activities were evaluated after intravenous administration of the compounds to anesthetized rats. Among them, the 5-chloro-2-cyanophenoxy derivative (29) showed the promising dual activities and was selected for further studies.

  合成了一系列具有苯氧基丙醇胺结构的新型哒嗪酮衍生物（II）。在静脉注射给麻醉大鼠后，评估了它们的降压和β-阻断活性。其中，5-氯-2-氰基苯氧基衍生物（29）显示出有前途的双重活性，并被选中进行进一步研究。
• BRIDGED ARYL PIPERAZINES DERIVATIVES USEFUL FOR THE TREATMENT OF CNS, GI-URINARY AND REPRODUCTIVE DISORDERS
  申请人：Creighton J. Christopher

  公开号：US20080070919A1

  公开（公告）日：2008-03-20

  The present invention is directed to bridged aryl piperazine derivatives, pharmaceutical compositions containing them and their use in the treatment of depression and related disorders. The compounds of the present invention are serotonin transport inhibitors and/or modulators of 5HT 1A .

  本发明涉及桥联芳基哌嗪衍生物，含有它们的药物组合物以及它们在治疗抑郁症和相关疾病中的用途。本发明的化合物是血清素转运抑制剂和/或5HT1A的调节剂。
• [EN] INDOLE DERIVATIVES FOR THE TREATMENT OF DEPRESSION AND ANXIETY<br/>[FR] DERIVES DE L'INDOLE DESTINES AU TRAITEMENT DE DEPRESSION ET D'ANXIETE
  申请人：LILLY CO ELI

  公开号：WO2001046181A1

  公开（公告）日：2001-06-28

  The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.

  本发明提供了式(I)的化合物，该化合物对于治疗抑郁症、焦虑症以及减轻戒烟或尼古丁部分戒断引起的症状是有用的。
• Basic substituted xanthine derivatives
  申请人：Deutsche Gold und Silber- Scheideanstalt vormals Roessler

  公开号：US04144340A1

  公开（公告）日：1979-03-13

  There are prepared compounds corresponding to the general formula T -- Alk -- NH -- CH.sub.2 -- CH(OH) -- CH.sub.2 -- O -- Ar I in which T represents a theophyllinyl-(7) or theobrominyl-(1) radical, Alk is a linear or branched alkylene group with 2 to 5 carbon atoms which may also be substituted by a hydroxy group and Ar represents an aromatic monocyclic or condensed bicyclic, carbocyclic or heterocyclic radical optionally substituted by one or more alkyl groups with 1 to 6 carbon atoms, alkenyl groups with 2 to 6 carbon atoms, alkinyl groups with 2 to 6 carbon atoms, hydroxy groups, acyloxy groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 6 carbon atoms, alkenoxy groups with 2 to 6 carbon atoms, phenyl radicals, halogen atoms, amino groups, acyl groups with 2 to 6 carbon atoms, aminocarbonyl groups, ureido groups, acyl amino groups with 1 to 6 carbon atoms, cycloalkyl groups with 3 to 8 carbon atoms or by one or more cycloalkenyl groups with 4 to 8 carbon atoms, the heterocyclic radical consisting of individual rings with 5 to 6 members and containing from 1 to 4 heteroatoms, and their pharmaceutically acceptable salts. The compounds have beta-adrenolytic activity.

  有准备好的化合物对应于一般式T-Alk-NH-CH.sub.2-CH(OH)-CH.sub.2-O-Ar I，在其中T代表茶碱基-(7)或可可碱基-(1)基团，Alk是具有2到5个碳原子的线性或支链烷基，也可以被一个羟基取代，Ar代表一个芳香单环或紧缩的双环、碳环或杂环基团，可选择地被一个或多个具有1到6个碳原子的烷基、具有2到6个碳原子的烯基、具有2到6个碳原子的炔基、羟基、具有1到6个碳原子的酰氧基、具有1到6个碳原子的烷氧基、具有2到6个碳原子的烯氧基、苯基基团、卤原子、氨基、具有2到6个碳原子的酰基、氨基甲酰基、脲基、具有1到6个碳原子的酰氨基基团、具有3到8个碳原子的环烷基或一个或多个具有4到8个碳原子的环烯基基团取代，杂环基团由5到6个成员的单独环组成，并含有1到4个杂原子，以及它们的药学上可接受的盐。这些化合物具有β-肾上腺素受体拮抗活性。