4-[[3-(3-Cyclopentyloxy-4-methoxyphenyl)pyrrolidin-3-yl]methyl]pyridine | 203441-47-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 4-[[3-(3-Cyclopentyloxy-4-methoxyphenyl)pyrrolidin-3-yl]methyl]pyridine
• CAS: 203441-47-8
• 化学式: C₂₂H₂₈N₂O₂
• 分子量: 352.477
• InChiKey: CFUCXSYPCKTBQA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  43.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  二碳酸二叔丁酯 、 4-[[3-(3-Cyclopentyloxy-4-methoxyphenyl)pyrrolidin-3-yl]methyl]pyridine 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 生成 Tert-butyl 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-(pyridin-4-ylmethyl)pyrrolidine-1-carboxylate
  参考文献：
  名称：

  Quaternary substituted PDE IV inhibitors II: The synthesis and in vitro evaluation of a novel series of γ-lactams

  摘要：

  This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE TV) inhibitors. Several of the quaternary substituted lactams presented possess low nanomolar IC50's for PDE IV inhibition. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00036-5
• 作为产物：
  描述：

  3-(3-Cyclopentyloxy-4-methoxy-phenyl)-3-pyridin-4-ylmethyl-pyrrolidin-2-one 在 红铝 作用下， 以 甲苯 为溶剂， 反应 2.0h， 生成 4-[[3-(3-Cyclopentyloxy-4-methoxyphenyl)pyrrolidin-3-yl]methyl]pyridine
  参考文献：
  名称：

  Quaternary substituted PDE IV inhibitors II: The synthesis and in vitro evaluation of a novel series of γ-lactams

  摘要：

  This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE TV) inhibitors. Several of the quaternary substituted lactams presented possess low nanomolar IC50's for PDE IV inhibition. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00036-5

文献信息

• [EN] SUBSTITUTED AROMATIC COMPOUNDS<br/>[FR] COMPOSES AROMATIQUES SUBSTITUES
  申请人：RHONE-POULENC RORER PHARMACEUTICALS INC.

  公开号：WO1998005327A1

  公开（公告）日：1998-02-12

  (EN) This invention is directed to compound of formula (I) or hydrate thereof, solvate thereof, N-oxide thereof, prodrug thereof or a pharmaceutically acceptable salt thereof, which possess useful pharmaceutical properties. They are especially useful for inhibiting the production or physiological effects of TNF and inhibit cyclic AMP. The present invention is also directed to their pharmaceutical use, pharmaceutical compositions containing the compounds, and methods of their preparation.(FR) La présente invention concerne un composé de la formule (I) ou un hydrate, un solvate, un N-oxyde, un promédicament ou un sel pharmaceutiquement acceptable dudit composé possédant des propriétés pharmaceutiques efficaces. Ils peuvent servir en particulier pour l'inhibition de la production ou des effets physiologiques du facteur de nécrose tumorale (TNF) et pour l'inhibition de l'AMP cyclique. La présente invention concerne également leur usage pharmaceutique, les compositions pharmaceutiques contenant de tels composés et leurs procédés de préparation.
• Quaternary substituted PDE IV inhibitors II: The synthesis and in vitro evaluation of a novel series of γ-lactams
  作者：Christopher Hulme、Kevin Moriarty、Fu-Chih Huang、Jonathon Mason、Dan McGarry、Richard Labaudiniere、John Souness、Stevan Djuric

  DOI：10.1016/s0960-894x(98)00036-5

  日期：1998.2

  This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE TV) inhibitors. Several of the quaternary substituted lactams presented possess low nanomolar IC50's for PDE IV inhibition. (C) 1998 Elsevier Science Ltd. All rights reserved.