4-(4-chloro-2-fluorobenzyloxy)pyridin-2(1H)-one | 1260240-58-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 4-(4-chloro-2-fluorobenzyloxy)pyridin-2(1H)-one
• 英文别名: 4-[(4-chloro-2-fluorophenyl)methoxy]-1H-pyridin-2-one
• CAS: 1260240-58-1
• 化学式: C₁₂H₉ClFNO₂
• 分子量: 253.66
• InChiKey: WRVGVKWLGDDEJC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(4-chloro-2-fluorobenzyloxy)pyridin-2(1H)-one 、 tert-butyl 8-bromo-6-methyl-1,2,4,5-tetrahydroazepino[4,5-b]indole-3(6H)-carboxylate 在 copper(l) iodide 8-羟基喹啉 、 caesium carbonate 、 盐酸 作用下， 以 二甲基亚砜 、 乙醚 、 二氯甲烷 为溶剂， 反应 44.0h， 以29%的产率得到4-(4-Chloro-2-fluorobenzyloxy)-1-(6-methyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indol-8-yl)pyridin-2(1H)-one hydrochloride
  参考文献：
  名称：

  AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF

  摘要：

  揭示了新型MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖、焦虑、抑郁、非酒精性脂肪肝病和精神疾病。本发明还描述了制备这些化合物的方法。

  公开号：

  US20110003793A1
• 作为产物：
  描述：

  2-氯-4-碘吡啶 、 4-氯-2-氟苄醇 在 copper(l) iodide 甲酸 、 1,10-菲罗啉 、 caesium carbonate 、 ammonium acetate 作用下， 以 甲苯 、 水 为溶剂， 反应 114.0h， 以28%的产率得到4-(4-chloro-2-fluorobenzyloxy)pyridin-2(1H)-one
  参考文献：
  名称：

  AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF

  摘要：

  揭示了新型MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖、焦虑、抑郁、非酒精性脂肪肝病和精神疾病。本发明还描述了制备这些化合物的方法。

  公开号：

  US20110003793A1

文献信息

• AZABICYCLOALKANE-INDOLE AND AZABICYCLOALKANE-PYRROLO-PYRIDINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
  申请人：GUZZO Peter R.

  公开号：US20110003737A1

  公开（公告）日：2011-01-06

  Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

  揭示了新型MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖、焦虑、抑郁、非酒精性脂肪肝病和精神障碍。本发明还描述了制备这些化合物的方法。
• AZINONE-SUBSTITUTED AZAPOLYCYCLE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
  申请人：GUZZO Peter R.

  公开号：US20110003738A1

  公开（公告）日：2011-01-06

  Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

  揭示了新型MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖、焦虑、抑郁、非酒精性脂肪肝病和精神疾病。本发明还描述了制备这些化合物的方法。
• Azinone-substituted azapolycycle MCH-1 antagonists, methods of making, and use thereof
  申请人：Guzzo Peter R.

  公开号：US08618299B2

  公开（公告）日：2013-12-31

  MCH-1 receptor antagonists are disclosed having the general formula These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

  本发明揭示了具有通式的MCH-1受体拮抗剂，这些化合物可用于治疗各种疾病，包括肥胖症、焦虑症、抑郁症、非酒精性脂肪肝病和精神障碍。本发明还描述了制备这些化合物的方法。
• Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof
  申请人：Guzzo Peter R.

  公开号：US08629158B2

  公开（公告）日：2014-01-14

  Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

  本发明揭示了新型的MCH-1受体拮抗剂。这些化合物可用于治疗各种疾病，包括肥胖症、焦虑症、抑郁症、非酒精性脂肪肝病和精神障碍。本发明还描述了制备这些化合物的方法。
• Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine MCH-1 antagonists, methods of making, and use thereof
  申请人：Guzzo Peter R.

  公开号：US08637501B2

  公开（公告）日：2014-01-28

  Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

  本发明揭示了新型MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖症、焦虑、抑郁、非酒精性脂肪肝病和精神障碍。本发明还描述了制备这些化合物的方法。