[4-[4-(3-氯丙氧基)苯基]苯基]-吡咯烷-1-基甲酮 | 372514-08-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: [4-[4-(3-氯丙氧基)苯基]苯基]-吡咯烷-1-基甲酮
• 英文名称: [4'-(3-Chloropropoxy)[1,1'-biphenyl]-4-yl](pyrrolidin-1-yl)methanone
• 英文别名: [4-[4-(3-chloropropoxy)phenyl]phenyl]-pyrrolidin-1-ylmethanone
• CAS: 372514-08-4
• 化学式: C₂₀H₂₂ClNO₂
• 分子量: 343.853
• InChiKey: BUGAJOMIZYVOHJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2R,5R)-(-)-反-2,5-二甲基吡咯烷 、 [4-[4-(3-氯丙氧基)苯基]苯基]-吡咯烷-1-基甲酮 在 potassium carbonate 、 potassium iodide 作用下， 以 丁酮 为溶剂， 反应 72.0h， 生成 [4-[4-[3-[(2R,5R)-2,5-dimethylpyrrolidin-1-yl]propoxy]phenyl]phenyl]-pyrrolidin-1-ylmethanone
  参考文献：
  名称：

  Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists

  摘要：

  Novel 4'-[(NRIR2-1-yl)]-propoxy-biaryl-4-carboxamides were designed and synthesized. All compounds were tested for affinity at histamine H(3)receptors. Most compounds were highly potent and selective for human and rat H-3 receptors and selected examples such as A-349821 showed functional antagonism of H3 receptors in vitro and in a mouse dipsogenia model. (C) 2003 Published by Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(03)00118-5
• 作为产物：
  描述：

  4-羟基-[1,1-联苯]-4-羧酸甲酯 在 lithium hydroxide 、 氯化亚砜 、 potassium carbonate 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 、 丁酮 为溶剂， 反应 28.0h， 生成 [4-[4-(3-氯丙氧基)苯基]苯基]-吡咯烷-1-基甲酮
  参考文献：
  名称：

  Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists

  摘要：

  Novel 4'-[(NRIR2-1-yl)]-propoxy-biaryl-4-carboxamides were designed and synthesized. All compounds were tested for affinity at histamine H(3)receptors. Most compounds were highly potent and selective for human and rat H-3 receptors and selected examples such as A-349821 showed functional antagonism of H3 receptors in vitro and in a mouse dipsogenia model. (C) 2003 Published by Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(03)00118-5

文献信息

• 1,3-Disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
  申请人：——

  公开号：US20020035103A1

  公开（公告）日：2002-03-21

  Compounds of formula I 1 are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands. Also disclosed are histamine-3 receptor ligand compositions and methods of antagonizing or agonizing histamine-3 receptors.

  公式I1的化合物在治疗由组织胺-3受体配体防止或改善的疾病或病况中非常有用。还公开了组织胺-3受体配体组合物和拮抗或激动组织胺-3受体的方法。
• 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
  申请人：——

  公开号：US20020137931A1

  公开（公告）日：2002-09-26

  Compounds of formula I 1 are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands. Also disclosed are histamine-3 receptor ligand compositions and methods of antagonizing or agonizing histamine-3 receptors.

  公式I1的化合物在治疗由组胺-3受体配体防止或改善的疾病或症状中很有用。还披露了组胺-3受体配体组合物和拮抗或激动组胺-3受体的方法。
• Aminoalkoxybiphenylcarboxamides as histamine-3 receptor ligands and their therapeutic applications
  申请人：——

  公开号：US20020111340A1

  公开（公告）日：2002-08-15

  Compounds of formula (I) 1 are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands.

  化学式为(I)1的化合物可用于治疗由组胺-3受体配体预防或改善的疾病或症状。
• 1,3-DISUBSTITUTED AND 1,3,3-TRISUBSTITUTED PYRROLIDINES AS HISTAMINE-3 RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS
  申请人：ABBOTT LABORATORIES

  公开号：EP1301480B1

  公开（公告）日：2007-09-12
• US6316475B1
  申请人：——

  公开号：US6316475B1

  公开（公告）日：2001-11-13