2-chloro-1-(4-methoxy-phenyl)-1H-benzoimidazole | 875004-76-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: 2-chloro-1-(4-methoxy-phenyl)-1H-benzoimidazole
• 英文别名: 2-chloro-1-(4-methoxyphenyl)benzimidazole
• CAS: 875004-76-5
• 化学式: C₁₄H₁₁ClN₂O
• 分子量: 258.707
• InChiKey: GYTZUJVHGGGXKX-UHFFFAOYSA-N

物化性质

• 沸点：
  435.7±47.0 °C(Predicted)
• 密度：
  1.27±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  27
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-{3-[1-(3-aminopropyl)piperidin-4-yl]phenyl}acetamide 、 2-chloro-1-(4-methoxy-phenyl)-1H-benzoimidazole 以giving 60 mg (30%) of the title compound Example 8的产率得到N-[3-(1-{3-[1-(4-methoxyphenyl)-1H-benzimidazol-2-ylamino]propyl}piperidin-4-yl)phenyl]acetamide
  参考文献：
  名称：

  MEDICINAL USE OF RECEPTOR LIGANDS

  摘要：

  式(I)的化合物是黑素浓集激素-1受体(MCH-1R)的配体，可用于治疗对黑素浓集激素(MCH)活性调节敏感的疾病，例如进食障碍和肥胖是危险因素的疾病（式(I)）：其中环B选自规定的特定取代苯基或苯并5元杂环；R附着在环B的环碳上，表示氢，F，Cl或—OCH3；X为═CH—或═N—；L为—CH2—或—CH2CH2—；L2为键，—CH2—或—CO—；R2为H或C，—C3烷基，或—N(R2)L，—选自规定的特定环状氨基连接基团。环A选自规定的特定含氮杂环。

  公开号：

  US20090062317A1
• 作为产物：
  描述：

  1-(p-Methoxyphenyl)benzimidazolon 在 三氯氧磷 作用下， 生成 2-chloro-1-(4-methoxy-phenyl)-1H-benzoimidazole
  参考文献：
  名称：

  Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists

  摘要：

  Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays role in several disorders such as obesity, stress, depression and anxiety. The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified. (c) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.07.086

文献信息

• Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：US10174052B2

  公开（公告）日：2019-01-08

  There are disclosed a series of quinuclidines having the Formula (I), which bind to the nicotinic α7 receptor and may be useful for the treatment of disorders of the central nervous system.

  本研究公开了一系列具有式（I）的喹烯酮类化合物，它们与烟碱α7 受体结合，可用于治疗中枢神经系统疾病。
• QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：US20170305929A1

  公开（公告）日：2017-10-26

  There are disclosed a series of quinuclidines having the Formula (I), which bind to the nicotinic α7 receptor and may be useful for the treatment of disorders of the central nervous system.
• [EN] MEDICINAL USE OF RECEPTOR LIGANDS<br/>[FR] UTILISATION MEDICALE DE LIGANDS RECEPTEURS
  申请人：7TM PHARMA AS

  公开号：WO2006010446A2

  公开（公告）日：2006-02-02

  Compounds of formula (I) are ligands of the melanin concentrating hormone-1 receptor (MCH-1 R), useful in the treatment of diseases responsive to modulation of melanin concentrating hormone (MCH) activity, for example feeding disorders and diseases for which obesity is a risk factor (I): wherein ring B is selected from specific substituted phenyl or benz-fused 5­membered N-containing heterocycles defined in the specification; R, is attached to a ring carbon of ring B, and represents hydrogen, F, Cl, or -OCH3; X is =CH- or =N-; L, is -CH2- or -CH2CH2- ; L2 is a bond, -CH2- or -CO-; R2 is H or C,-C3 alkyl, or -N(R2) L,- is selected from specific cyclic amino linker radicals as defined in the specification; ring A is selected from specific N- containing heterocyclic rings as defined in the specification.