N-[1-(3,4-dichlorobenzyl)piperidin-4-yl]chloroacetamide | 328083-89-2

• 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: N-[1-(3,4-dichlorobenzyl)piperidin-4-yl]chloroacetamide
• 英文别名: 2-chloro-N-[1-(3,4-dichlorobenzyl)-4-piperidinyl]acetamide；2-chloro-N-[1-(3,4-dichlorobenzyl)-piperidin-4-yl]-acetamide；2-chloro-N-[1-[(3,4-dichlorophenyl)methyl]piperidin-4-yl]acetamide
• CAS: 328083-89-2
• 化学式: C₁₄H₁₇Cl₃N₂O
• 分子量: 335.661
• InChiKey: VRUJDFMWESUUOY-UHFFFAOYSA-N

物化性质

• 沸点：
  481.1±45.0 °C(Predicted)
• 密度：
  1.35±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  32.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-[1-(3,4-dichlorobenzyl)piperidin-4-yl]chloroacetamide 在 potassium tert-butylate 作用下， 以 N-甲基吡咯烷酮 为溶剂， 反应 17.25h， 生成 methyl [4-(2-{[1-(3,4-dichlorobenzyl)piperidin-4-yl]amino}-2-oxoethoxy)phenyl]acetate
  参考文献：
  名称：

  WO2007/102768

  摘要：

  公开号：
• 作为产物：
  描述：

  1-(3,4-dichlorobenzyl)piperidin-4-ylamine dihydrochloride 、 N,N-二异丙基乙胺 、 氯乙酰氯 以to give the subtitle compound (1.0 g)的产率得到N-[1-(3,4-dichlorobenzyl)piperidin-4-yl]chloroacetamide
  参考文献：
  名称：

  Substituted piperidine compounds useful as modulators of chemokine receptor activity

  摘要：

  本发明提供了公式(I)的化合物：其中R1，R2，R3，R6，Z，Q，m，n，X1，X2，X3，X4和T如规范中所定义，以及它们的制备方法，含有它们的药物组合物，并用于治疗，特别是用于治疗趋化因子受体相关疾病和病况。

  公开号：

  US20050250792A1

文献信息

• Novel benzylpiperidine compound
  申请人：——

  公开号：US20040158071A1

  公开（公告）日：2004-08-12

  The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. 1 wherein each symbol is as defined in the specification.

  本发明的目的是提供一种具有基于趋化因子抑制活性的治疗效果的化合物，作为口服药物而言，具有令人满意的药物品质。本发明人发现以下苯基哌啶衍生物（式（1））具有趋化因子抑制活性。进一步的深入研究成功增强了该化合物的趋化因子抑制活性和血液稳定性，从而完成了本发明。式中每个符号如说明书中所定义。
• Benzylpiperidine compound
  申请人：Mitsubishi Pharma Corporation

  公开号：US07115635B2

  公开（公告）日：2006-10-03

  The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.

  本发明的目的是提供一种具有基于趋化因子抑制活性的治疗效果的化合物，其作为口服药物的药品是令人满意的。本发明人发现以下苯基哌啶衍生物（式（1））具有趋化因子抑制活性。进一步的深入研究成功提高了该化合物的趋化因子抑制活性和血液稳定性，完成了本发明。 其中，每个符号如规范中所定义。
• Piperidine Derivatives, Their Process for Preparation, Their Use as Therapeutic Agents and Pharmaceutical Compositions Containing Them
  申请人：Cage Peter

  公开号：US20090197914A1

  公开（公告）日：2009-08-06

  The present invention provides a compound of a formula (I) wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.

  本发明提供了一个式(I)的化合物，其中变量在此定义；提供制备这种化合物的方法；以及使用这种化合物治疗趋化因子（如CCR3）介导的疾病状态。
• NOVEL BENZYLPIPERIDINE COMPOUND
  申请人：Mitsubishi Pharma Corporation

  公开号：EP1389616A1

  公开（公告）日：2004-02-18

  The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.

  本发明的目的是提供一种具有基于趋化因子抑制活性的治疗效果的化合物，该化合物作为口服药物是令人满意的。 本发明者发现以下苄基哌啶衍生物（式（1））具有趋化因子抑制活性。通过进一步深入研究，成功地提高了本化合物的趋化因子抑制活性和在血液中的稳定性，并完成了本发明。 其中各符号如说明书中所定义。
• 3,4-Dihalobenzylpiperidine derivatives and their medical use
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP1389616B1

  公开（公告）日：2011-07-27