4-氨基-1-(2-吲哚-3-基乙基)哌啶 | 35633-77-3

• 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
• 中文名称: 4-氨基-1-(2-吲哚-3-基乙基)哌啶
• 英文名称: 3-<2-(4-aminopiperidyl)ethyl>indole
• 英文别名: 3-<2-(4-Aminopiperid-1-yl)-ethyl>indol；4-amino-1-[2-(indol-3-yl)ethyl]piperidine；1-[2-(3-indolyl)ethyl]-4-aminopiperidine；3-[2-(4-aminopiperidyl)-ethyl]indole；1-(2-indol-3-yl-ethyl)-piperidin-4-ylamine；3-[2-(4-amino-1-piperidyl)ethyl]indole；1-(2-(1H-Indol-3-yl)ethyl)piperidin-4-amine；1-[2-(1H-indol-3-yl)ethyl]piperidin-4-amine
• CAS: 35633-77-3
• 化学式: C₁₅H₂₁N₃
• 分子量: 243.352
• InChiKey: OYRXLTLEMXGPPF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  45
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  4-氨基-1-(2-吲哚-3-基乙基)哌啶 生成 N-[1-[2-(1H-indol-3-yl)ethyl]piperidin-4-yl]-5-methyl-1H-imidazole-4-carboxamide
  参考文献：
  名称：

  ARCHIBALD, JOHN LEHEUP;WARD, TERENCE JAMES

  摘要：

  DOI：

文献信息

• Antihypertensive ureidopiperidines
  作者：J. L. Archibald、D. R. Beardsley、G. M. F. Bisset、P. Fairbrother、J. L. Jackson、A. Opalko、T. J. Ward

  DOI：10.1021/jm00182a009

  日期：1980.8

  These compounds are related to the benzamidopiperidines exemplified by indoramin. Some of the ureidopiperidines are more potent antihypertensive agents than their benzamidopiperidine counterparts. Two examples, 1-(2-thenoyl)-3-[1-[2-(3-indolyl)ethyl]piperid-4-yl]urea and 1-(2-thenoyl)-3-[1-[4-(4-fluorophenyl)-4-oxobutyl]piperid-4-yl]urea (19 and 58), emerged as the most potent antihypertensive agents

  报道了一系列1-芳烷基-4-脲基哌啶的合成。这些化合物与吲哚胺为例的苯甲酰氨基哌啶有关。一些脲基哌啶比其苯甲酰氨基哌啶具有更强的抗高血压药。两个例子，1-（2-thenoyl）-3- [1- [2-（3-吲哚基）乙基]哌啶-4-基]脲和1-（2-thenoyl）-3- [1- [4- （4-氟苯基）-4-氧代丁基]哌啶-4-基]脲（19和58）成为本系列中最有效的降压药。
• Indole derivatives
  申请人：John Wyeth & Brother Limited

  公开号：US04772617A1

  公开（公告）日：1988-09-20

  The invention concerns indole derivatives of formula I ##STR1## in which R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy, R.sub.2, R.sub.3 and R.sub.4 independently represent hydrogen or lower alkyl, A represents an alkylene, oxoalkylene or hydroxyalkylene chain each having 2 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity while exhibiting reduced CNS depressant properties. Also disclosed are methods for preparing the compounds of formula I and pharmaceutical compositions containing them.

  该发明涉及式I的吲哌啶衍生物##STR1##其中R.sub.1是氢、较低烷基、卤素、较低烷氧基或羟基，R.sub.2、R.sub.3和R.sub.4独立地代表氢或较低烷基，A代表具有2到6个碳原子的烷基、氧代烷基或羟基烷基链，或其药学上可接受的盐，这些化合物具有降低中枢神经系统抑制作用的抗高血压活性。还公开了制备式I化合物的方法和含有它们的药物组合物。
• N-[2-[[1-[1H-Indolylalkyl- or
  申请人：John Wyeth & Brother Limited

  公开号：US04443461A1

  公开（公告）日：1984-04-17

  The invention concerns compounds of formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Ar represents an optionally substituted indolyl group; A represents a straight or branched chain alkylene or oxoalkylene group, each having 2-4 carbon atoms and R represents an optionally substituted aryl (including heteroaryl) group, which possess anti-hypertensive and psychotropic activity, and are useful in the treatment of high blood pressure or as anti-depressants.

  这项发明涉及公式##STR1##的化合物或其药用盐，其中Ar代表可选择取代的吲哩基团；A代表直链或支链烷基或氧代烷基团，每个团含有2-4个碳原子；R代表可选择取代的芳基（包括杂环芳基）团，这些化合物具有抗高血压和精神药效，并可用于治疗高血压或作为抗抑郁药。
• Ureidopiperidino-ketoalkyl indoles
  申请人：John Wyeth & Brother Limited

  公开号：US04061641A1

  公开（公告）日：1977-12-06

  The invention provides compounds of general formula I ##STR1## and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein R represents hydrogen or lower alkyl, R.sup.1 represents hydrogen or lower alkyl, R.sup.2 represents hydrogen or lower alkyl, R.sup.3 represents hydrogen, halogen, lower alkoxy, hydroxy, or lower alkyl, R.sup.4 represents hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, thienyl, furyl, phenyl; phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy or trifluoromethyl; or benzoyl, halobenzoyl, lower alkanoyl, cycloalkanoyl of 6 to 8 carbon atoms, or thienoyl, A represents an alkylene, mono- or diketo- or hydroxy-alkylene radical having from 1 to 5 carbon atoms and X is oxygen or sulphur. The compounds exhibit action on the cardiovascular system particularly hypotensive and/or anti-hypertensive activity.

  本发明提供一般式I的化合物及其药学上可接受的酸加合物和季铵盐，其中R代表氢或较低的烷基，R.sup.1代表氢或较低的烷基，R.sup.2代表氢或较低的烷基，R.sup.3代表氢、卤素、较低的烷氧基、羟基或较低的烷基，R.sup.4代表氢、较低的烷基、5至7个碳原子的环烷基、噻吩基、呋喃基、苯基；苯基单取代或双取代的卤素、较低的烷基、较低的烷氧基、羟基或三氟甲基；或苯甲酰基、卤代苯甲酰基、较低的烷酰基、6至8个碳原子的环烷酰基或噻吩酰基，A代表含有1至5个碳原子的烷基、单或双酮基或羟基烷基基团，X为氧或硫。这些化合物表现出对心血管系统的作用，特别是降低血压和/或抗高血压活性。
• 1-[(3-Indolyl)-alkyl]-piperidyl ureas and hypotensive compositions
  申请人：John Wyeth & Brother Ltd.

  公开号：US04177279A1

  公开（公告）日：1979-12-04

  The invention provides compounds of general formula I ##STR1## and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein R represents hydrogen or lower alkyl, R.sup.1 represents hydrogen or lower alkyl, R.sup.2 represents hydrogen or lower alkyl, R.sup.3 represents hydrogen, halogen, lower alkoxy, hydroxy, or lower alkyl, R.sup.4 represents hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, thienyl, furyl, phenyl; phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy or trifluoromethyl; or benzoyl, halobenzoyl, lower alkanoyl, cycloalkanoyl of 6 to 8 carbon atoms, or thienoyl, A represents an alkylene, mono- or diketo- or hydroxy-alkylene radical having from 1 to 5 carbon atoms and X is oxygen or sulphur. The compounds exhibit action on the cardiovascular system particularly hypotensive and/or anti-hypertensive activity.

  本发明提供了通式I的化合物及其药学上可接受的酸加合物和季铵盐，其中R代表氢或低碳基，R1代表氢或低碳基，R2代表氢或低碳基，R3代表氢、卤素、低烷氧基、羟基或低碳基，R4代表氢、低碳基、5至7个碳原子的环烷基、噻吩基、呋喃基、苯基；苯基单取代或双取代卤素、低烷基、低烷氧基、羟基或三氟甲基；或苯甲酰基、卤代苯甲酰基、6至8个碳原子的低烷酰基、环烷酰基或噻吩酰基，A代表1至5个碳原子的烷基、单酮基或双酮基或羟基烷基，X为氧或硫。这些化合物表现出对心血管系统的作用，特别是降低血压和/或抗高血压活性。