1-(3,5-Difluorophenyl)piperidin-4-amine | 483366-42-3

• 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: 1-(3,5-Difluorophenyl)piperidin-4-amine
• CAS: 483366-42-3
• 化学式: C₁₁H₁₄F₂N₂
• 分子量: 212.242
• InChiKey: CDXUIVYVYXNIOC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N,N'-二琥珀酰亚胺基碳酸酯 、 1-(3,5-Difluorophenyl)piperidin-4-amine 在 吡啶 作用下， 以 四氢呋喃 为溶剂， 生成
  参考文献：
  名称：

  Discovery of novel orally active ureido NPY Y5 receptor antagonists

  摘要：

  We have derived a novel series of neuropeptide Y (NPY) Y5 receptor antagonists from the biphenylurea 3. Cyclohexylurea 21c, a member of the series, is a potent NPY Y5 receptor antagonist that exhibits excellent pharmacokinetic parameters in rats and dogs. On chronic oral administration to diet-induced obese rats, 21c displayed an anti-obesity profile, causing a modest reduction in food intake, a significant decrease in body weight gain, a decrease in adipose mass, and an increase in lean tissue mass. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.11.132
• 作为产物：
  描述：

  在 palladium on activated charcoal 甲酸 作用下， 以 甲醇 为溶剂， 以83%的产率得到1-(3,5-Difluorophenyl)piperidin-4-amine
  参考文献：
  名称：

  Discovery of novel orally active ureido NPY Y5 receptor antagonists

  摘要：

  We have derived a novel series of neuropeptide Y (NPY) Y5 receptor antagonists from the biphenylurea 3. Cyclohexylurea 21c, a member of the series, is a potent NPY Y5 receptor antagonist that exhibits excellent pharmacokinetic parameters in rats and dogs. On chronic oral administration to diet-induced obese rats, 21c displayed an anti-obesity profile, causing a modest reduction in food intake, a significant decrease in body weight gain, a decrease in adipose mass, and an increase in lean tissue mass. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.11.132

文献信息

• Fluoropyrrolidines as dipeptidyl peptidase inhibitors
  申请人：——

  公开号：US20040242636A1

  公开（公告）日：2004-12-02

  The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV), and to methods for their production and their therapeutic utility.

  本发明涉及新颖化合物，其用于抑制后脯氨酸/苯丙氨酸剪切蛋白酶，例如丝氨酸蛋白酶，例如二肽基肽酶，例如二肽基肽酶IV（DPP-IV），以及其生产方法和治疗效用。
• FLUOROPYRROLIDINES AS DIPEPTIDYL PEPTIDASE INHIBITORS
  申请人：SMITHKLINE BEECHAM CORPORATION

  公开号：EP1399433A2

  公开（公告）日：2004-03-24
• US7183290B2
  申请人：——

  公开号：US7183290B2

  公开（公告）日：2007-02-27
• US7304076B2
  申请人：——

  公开号：US7304076B2

  公开（公告）日：2007-12-04
• [EN] FLUOROPYRROLIDINES AS DIPEPTIDYL PEPTIDASE INHIBITORS<br/>[FR] FLUOROPYRROLIDINES INHIBITRICES DE LA DIPEPTIDYL PEPTIDASE
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2003002553A2

  公开（公告）日：2003-01-09

  The present invention relates to novel compounds of following formulae (I)-(VI) their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV), and to methods for their production and their therapeutic utility.