4-Piperidin-4-yl-heptan-4-ol | 160809-31-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-Piperidin-4-yl-heptan-4-ol
• 英文别名: 4-Piperidin-4-ylheptan-4-ol
• CAS: 160809-31-4
• 化学式: C₁₂H₂₅NO
• 分子量: 199.337
• InChiKey: WBMMKSMFXKAVAU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-Piperidin-4-yl-heptan-4-ol 、 N-[2-(3,4-dichlorophenyl)-3-formylpropyl]-N-methylbenzamide 在 sodium cyanoborohydride 作用下， 以 甲醇 为溶剂， 生成 N-{2-(3,4-Dichloro-phenyl)-4-[4-(1-hydroxy-1-propyl-butyl)-piperidin-1-yl]-butyl}-N-methyl-benzamide
  参考文献：
  名称：

  4-Alkylpiperidines related to SR-48968: Potent antagonists of the neurokinin-2 (NK2) receptor

  摘要：

  A series of 4-alkylpiperidine derivatives related to the potent neurokinin-2 (NK2) receptor antagonist SR-48968 (1) is described. Simple aliphatic derivatives were found to be poorly active, but appropriate placement of an alcohol functional group afforded compounds that were of similar activity to 1. Several representatives in this series, such as the 4-(1-hydroxy-1-ethylpropyl)piperidine (14), were found to exhibit oral activity in a model of labored abdominal breathing in guinea pigs. These results expand the latitude of substituents available in this region of this series of NK2 receptor antagonists. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00037-7
• 作为产物：
  描述：

  哌啶-4-甲酸乙酯 在 palladium on activated charcoal 氢气 、 三乙胺 作用下， 以 四氢呋喃 、 乙醇 、 氯仿 为溶剂， 生成 4-Piperidin-4-yl-heptan-4-ol
  参考文献：
  名称：

  4-Alkylpiperidines related to SR-48968: Potent antagonists of the neurokinin-2 (NK2) receptor

  摘要：

  A series of 4-alkylpiperidine derivatives related to the potent neurokinin-2 (NK2) receptor antagonist SR-48968 (1) is described. Simple aliphatic derivatives were found to be poorly active, but appropriate placement of an alcohol functional group afforded compounds that were of similar activity to 1. Several representatives in this series, such as the 4-(1-hydroxy-1-ethylpropyl)piperidine (14), were found to exhibit oral activity in a model of labored abdominal breathing in guinea pigs. These results expand the latitude of substituents available in this region of this series of NK2 receptor antagonists. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00037-7

文献信息

• N-alkyl substituted piperidine-derivatives with neurokinin receptor antagonist activity
  申请人：ZENECA LIMITED

  公开号：EP0625509A1

  公开（公告）日：1994-11-23

  The present invention concerns the novel alkyl substituted heterocycles of formula I, set out below, wherein Q, Q¹, Q² and R have the values defined herein, which antagonize the pharmacological actions of one of the endogenous neuropeptide tachykinins at the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the alkyl substituted heterocycles for use in such treatment, methods for their use, and processes and novel intermediates for their manufacture.

  本发明涉及下式 I 的新型烷基取代杂环，其中 Q、Q¹、Q² 和 R 具有本文所定义的值，该杂环可拮抗内源性神经肽之一速激肽在神经激肽 2 (NK2) 受体上的药理作用，使其在需要这种拮抗作用时非常有用，例如在治疗哮喘和相关疾病时。本发明还提供了用于此类治疗的含有烷基取代杂环的药物组合物、使用方法以及生产工艺和新型中间体。
• Heterocyclic compounds
  申请人：ZENECA LIMITED

  公开号：EP0680962A2

  公开（公告）日：1995-11-08

  Compounds of formula I wherein Q1, Q2, Q3, Q4, Q5 and T have any of the meanings given in the specification, their N-oxides, their quaternary ammonium salts, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

  式 I 的化合物 其中 Q1、Q2、Q3、Q4、Q5 和 T 具有说明书中给出的任何含义，它们的 N-氧化物、季铵盐和它们的药学上可接受的盐是神经激肽 A 的非肽拮抗剂，可用于治疗哮喘等。还公开了药物组合物、制备式 I 化合物的工艺和中间体。
• Substituted heterocycles
  申请人：ZENECA LIMITED

  公开号：EP0739891A2

  公开（公告）日：1996-10-30

  Compounds of formula I wherein Q1, Q2, Q3, Q4 and Q5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

  式 I 的化合物 其中 Q1、Q2、Q3、Q4 和 Q5 具有说明书中给出的任何含义，它们的 N-氧化物和它们的药学上可接受的盐是非肽拮抗剂 NKA，可用于治疗哮喘等。还公开了药物组合物、制备式 I 化合物的工艺和中间体。
• CYCLIC AMIDE DERIVATIVES AS NEUROKININ A ANTAGONISTS
  申请人：AstraZeneca AB

  公开号：EP0734383B1

  公开（公告）日：2002-07-24
• US5521199A
  申请人：——

  公开号：US5521199A

  公开（公告）日：1996-05-28