1-(3-aminopropyl)-4-[3-(phenoxy)propyl]piperazine | 145708-24-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 1-(3-aminopropyl)-4-[3-(phenoxy)propyl]piperazine
• 英文别名: 3-[4-(3-Phenoxypropyl)piperazin-1-yl]propan-1-amine
• CAS: 145708-24-3
• 化学式: C₁₆H₂₇N₃O
• 分子量: 277.41
• InChiKey: FXWDBGIZESYWLX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  20
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  41.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(3-aminopropyl)-4-[3-(phenoxy)propyl]piperazine 在 盐酸 作用下， 以 甲醇 为溶剂， 生成
  参考文献：
  名称：

  1-Phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl]piperazine derivatives as non-imidazole histamine H3-antagonists

  摘要：

  In this study, a series of 1-phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl]piperazine derivatives has been prepared and in vitro tested as H-3-receptor antagonists (electrically evoked contraction of the guinea pig jejunum). All compounds investigated show moderate in vitro affinities. The most potent antagonists in this series are the compounds 9b, 1b, 1f, and 1l, which exhibit, independently of the substituent at the end of -N- moiety, almost the same level of affinity (pA (2) = 7.18, pA (2) = 7.27, pA (2) = 7.13, pA (2) = 7.12, respectively). The histaminergic H-1 antagonism of the aforementioned four products was established on the isolated guinea pig ileum by conventional methods; the pA (2) values were compared with the potency of pyrilamine. None of them shows any H-1-antagonistic activity (pA (2) < 4; for pyrilamine pA (2) = 9.35).

  DOI：

  10.1007/s00044-012-0090-2
• 作为产物：
  描述：

  在 lithium aluminium tetrahydride 作用下， 以 乙醚 为溶剂， 反应 2.5h， 以98.6%的产率得到1-(3-aminopropyl)-4-[3-(phenoxy)propyl]piperazine
  参考文献：
  名称：

  1-Phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl]piperazine derivatives as non-imidazole histamine H3-antagonists

  摘要：

  In this study, a series of 1-phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl]piperazine derivatives has been prepared and in vitro tested as H-3-receptor antagonists (electrically evoked contraction of the guinea pig jejunum). All compounds investigated show moderate in vitro affinities. The most potent antagonists in this series are the compounds 9b, 1b, 1f, and 1l, which exhibit, independently of the substituent at the end of -N- moiety, almost the same level of affinity (pA (2) = 7.18, pA (2) = 7.27, pA (2) = 7.13, pA (2) = 7.12, respectively). The histaminergic H-1 antagonism of the aforementioned four products was established on the isolated guinea pig ileum by conventional methods; the pA (2) values were compared with the potency of pyrilamine. None of them shows any H-1-antagonistic activity (pA (2) < 4; for pyrilamine pA (2) = 9.35).

  DOI：

  10.1007/s00044-012-0090-2

文献信息

• SUBSTITUTED SULFONAMIDE DERIVATIVE OR PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0525203A1

  公开（公告）日：1993-02-03

  A substituted sulfonamide derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, both of which act on a bronchial smooth muscle of a mammal and are effective as an active ingredient of a pharmaceutical composition for preventing and treating respiratory organ diseases such as asthma. In formula (I) A represents hydrogen or alkyl; G represents methylene or alkylene; Q1 represents ethylene; Q2 represents ethylene or trimethylene; E represents alkyl or a group of formula (II-a) or (II-b): -G-J-Z (II-a), -G-Z (II- b) wherein G is as defined above, J represents oxygen, sulfur or nitrogen, and Z represents alkyl, alkoxy, aryl, or heterocycle; and X represents quinoline, isoquinoline, benzothiazole or quinazolin-4-one.

  一种由通式(I)代表的取代磺酰胺衍生物或其药学上可接受的盐，二者均作用于哺乳动物的支气管平滑肌，作为预防和治疗呼吸器官疾病如哮喘的药物组合物的有效成分。在式(I)中，A代表氢或烷基；G代表亚甲基或亚烷基；Q1代表乙烯；Q2代表乙烯或三亚甲基；E代表烷基或式(II-a)或(II-b)的基团：-G-J-Z（II-a），-G-Z（II- b） 其中 G 如上定义，J 代表氧、硫或氮，Z 代表烷基、烷氧基、芳基或杂环；X 代表喹啉、异喹啉、苯并噻唑或喹唑啉-4-酮。
• US5326870A
  申请人：——

  公开号：US5326870A

  公开（公告）日：1994-07-05