INTEPIRDINE中间体 | 607743-10-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: INTEPIRDINE中间体
• 英文名称: tert-butyl 4-[3-(phenylsulfonyl)quinolin-8-yl]piperazine-1-carboxylate
• 英文别名: 8-(4-t-butoxycarbonyl)piperazin-1-yl-3-phenylsulfonylquinoline；tert-butyl 4-[3-(benzenesulfonyl)quinolin-8-yl]piperazine-1-carboxylate
• CAS: 607743-10-2
• 化学式: C₂₄H₂₇N₃O₄S
• 分子量: 453.562
• InChiKey: KPUWJBDXKICJTB-UHFFFAOYSA-N

物化性质

• 沸点：
  646.3±55.0 °C(Predicted)
• 密度：
  1.275±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  32
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  88.2
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  INTEPIRDINE中间体 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 3-苯磺酰基-8-(哌嗪-1-基)喹啉
  参考文献：
  名称：

  Syntheses, Radiolabelings, and in Vitro Evaluations of Fluorinated PET Radioligands of 5-HT₆ Serotoninergic Receptors

  摘要：

  The 5-HT6 receptors are potent therapeutic targets for psychiatric and neurological diseases (schizophrenia, Alzheimer's disease, etc.). However, with lack of specific radiopharmaceuticals, their pharmacology is still incomplete and their exploration is limited to animal models. In this context, we have designed a fluorinated PET radiotracer, [F-18]2FNQ1P, that possesses a high affinity and selectivity for 5-HT6. In vitro PET autoradiographies in rat brain sections with this radiotracer were in accordance with the 5-HT6 distribution pattern.

  DOI：

  10.1021/jm500372e
• 作为产物：
  描述：

  8-chloro-3-iodoquinoline 在 tris-(dibenzylideneacetone)dipalladium(0) 、 copper(l) iodide 、 caesium carbonate 、 sodium t-butanolate 、 2-二环己膦基-2'-(N,N-二甲胺)-联苯 、 N,N'-二甲基乙二胺 作用下， 以 二甲基亚砜 、 甲苯 为溶剂， 反应 4.0h， 生成 INTEPIRDINE中间体
  参考文献：
  名称：

  Syntheses, Radiolabelings, and in Vitro Evaluations of Fluorinated PET Radioligands of 5-HT₆ Serotoninergic Receptors

  摘要：

  The 5-HT6 receptors are potent therapeutic targets for psychiatric and neurological diseases (schizophrenia, Alzheimer's disease, etc.). However, with lack of specific radiopharmaceuticals, their pharmacology is still incomplete and their exploration is limited to animal models. In this context, we have designed a fluorinated PET radiotracer, [F-18]2FNQ1P, that possesses a high affinity and selectivity for 5-HT6. In vitro PET autoradiographies in rat brain sections with this radiotracer were in accordance with the 5-HT6 distribution pattern.

  DOI：

  10.1021/jm500372e

文献信息

• [EN] QUINOLINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] COMPOSES DE QUINOLEINE ET COMPOSITIONS PHARMACEUTIQUES CONTENANT CEUX-CI
  申请人：GLAXO GROUP LTD

  公开号：WO2005026125A1

  公开（公告）日：2005-03-24

  This application relates to quinoline compounds of formula (I) having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.

  本申请涉及具有药理活性的公式（I）的喹啉化合物，以及其制备过程，包含它们的组合物和在治疗中枢神经系统和其他疾病中的使用。
• QUINOLINE DERIVATIVES AND THEIR USE AS 5-HT6 LIGANDS
  申请人：AHMED Mahmood

  公开号：US20100305107A1

  公开（公告）日：2010-12-02

  Disclosed are quinoline compounds having affinity for the 5-HT 6 receptor and having the formula: where R 1 , R 2 , R 3 , R 4 , R 5 , n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.

  揭示了亲和力对于5-HT6受体的喹啉化合物，其化学式为：其中R1，R2，R3，R4，R5，n，m，p和A在此定义，并且包括其盐，含有这些化合物和盐的组合物以及制备和使用它们的方法。
• Novel compounds
  申请人：Ahmend Mahood

  公开号：US20050124628A1

  公开（公告）日：2005-06-09

  The present invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.

  本发明涉及一种具有药理活性的新型喹啉化合物，其制备过程、含有它们的组合物以及它们在中枢神经系统和其他疾病的治疗中的应用。
• Quinoline Derivatives and Their Use as 5-HT6 Ligands
  申请人：AHMED Mahmood

  公开号：US20090036682A1

  公开（公告）日：2009-02-05

  The present invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.

  本发明涉及具有药理活性的新奎诺啉化合物，以及它们的制备方法、含有它们的组合物和在治疗中枢神经系统和其他疾病方面的应用。
• Quinoline compounds and pharmeceutical compositions containing them
  申请人：Johnson Norbert Christopher

  公开号：US20060287334A1

  公开（公告）日：2006-12-21

  This invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.

  本发明涉及具有药理活性的新奎诺林化合物，以及制备它们的方法、含有它们的组合物和它们在治疗中枢神经系统和其他疾病中的应用。