2-<4-(chloropropoxy)phenyl>-7-methylimidazo<1,2-a>pyridine | 114604-72-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-<4-(chloropropoxy)phenyl>-7-methylimidazo<1,2-a>pyridine
• 英文别名: 2-(4-Chloropropoxyphenyl)-7-methylimidazo[1,2-a]pyridine；2-[4-(3-chloropropoxy)phenyl]-7-methylimidazo[1,2-a]pyridine
• CAS: 114604-72-7
• 化学式: C₁₇H₁₇ClN₂O
• 分子量: 300.788
• InChiKey: TYMLDQMTEMOVDX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  26.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-<4-(chloropropoxy)phenyl>-7-methylimidazo<1,2-a>pyridine 、 哌啶 在 乙酸乙酯 、 碳酸氢钠 、 magnesium sulfate 、 silica gel 、 methanol-dichloromethane 作用下， 反应 5.0h， 以to give the title compound (0.21 g)的产率得到JNJ-6379490
  参考文献：
  名称：

  Phenyl-substituted imidazopyridines

  摘要：

  本发明涉及一种具有药理活性的苯基取代的咪唑吡啶及其衍生物，制备方法和使用方法。

  公开号：

  US20050085501A1
• 作为产物：
  描述：

  1-[4-(3-chloropropoxy)phenyl]ethanone 在 溴 作用下， 以 乙醚 、 乙醇 为溶剂， 反应 20.0h， 生成 2-<4-(chloropropoxy)phenyl>-7-methylimidazo<1,2-a>pyridine
  参考文献：
  名称：

  Novel human histamine H3 receptor antagonists

  摘要：

  High throughput screening, using the recombinant human H-3 receptor, was used to identify novel histamine H-3 receptor antagonists. Evaluation of the lead compounds ultimately afforded potent, selective, orally bioavailable compounds (e.g., 38) with favorable blood-brain barrier penetration. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00738-2

文献信息

• Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity
  作者：Pauline J. Sanfilippo、Maud Urbanski、Jeffery B. Press、Barry Dubinsky、John B. Moore

  DOI：10.1021/jm00119a026

  日期：1988.11

  A series of imidazo-fused heterocycles substituted with an aryloxy)alkylamine side chain were prepared as modifications to butoprozine (I) and found to possess calcium channel blocking activity similar in potency to that of bepridil in trachea smooth muscle and similar to that of verapamil in nitrendipine binding affinity in rabbit cardiac muscle. Of the various imidazo-fused heterocycles prepared, the imidazo[1,2-a]pyridines were also found to be potent local anesthetic agents. While most compounds in this series were equipotent to lidocaine in our initial screen, compounds 2 and 35 showed local anesthetic activity approximately 100 times more potent than lidocaine in our preliminary assays. These compounds represent a novel structural class of local anesthetic agents, and compound 2 is under further investigation.
• PRESS, JEFFERY B.
  作者：PRESS, JEFFERY B.

  DOI：——

  日期：——
• SANFILIPPO, PAULINE J.;URBANSKI, MAUD;PRESS, JEFFERY B.;DUBINSKY, BARRY;M+, J. MED. CHEM., 31,(1988) N 11, C. 2201-2227
  作者：SANFILIPPO, PAULINE J.、URBANSKI, MAUD、PRESS, JEFFERY B.、DUBINSKY, BARRY、M+

  DOI：——

  日期：——
• PHENYL-SUBSTITUTED IMIDAZOPYRIDINES
  申请人：Ortho McNeil Pharmaceuticals, Inc.

  公开号：EP1268478A2

  公开（公告）日：2003-01-02
• US6908929B2
  申请人：——

  公开号：US6908929B2

  公开（公告）日：2005-06-21