2-bromo-5-(fluoromethyl)pyridine | 1346533-43-4

• 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: 2-bromo-5-(fluoromethyl)pyridine
• 英文别名: 2-Bromo-5-(fluoromethyl)pyridine
• CAS: 1346533-43-4
• 化学式: C₆H₅BrFN
• 分子量: 190.015
• InChiKey: WXSAPSVNMVRIJB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  12.9
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-bromo-5-(fluoromethyl)pyridine 、 乙烯三氟硼酸钾 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 caesium carbonate 作用下， 以 水 为溶剂， 反应 1.5h， 以67%的产率得到5-(fluoromethyl)-2-vinylpyridine
  参考文献：
  名称：

  [EN] PYRIMIDINE PDE10 INHIBITORS
  [FR] INHIBITEURS PYRIMIDINES DE PDE10

  摘要：

  本发明涉及嘧啶化合物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及利用这些化合物治疗神经系统和精神疾病，如精神分裂症、精神病或亨廷顿病，以及与纹状体功能不足或基底神经节功能障碍相关的疾病。

  公开号：

  WO2013028590A1
• 作为产物：
  描述：

  6-溴-3-羟甲基吡啶 在 二乙胺基三氟化硫 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 以37%的产率得到2-bromo-5-(fluoromethyl)pyridine
  参考文献：
  名称：

  [EN] PYRIMIDINE PDE10 INHIBITORS
  [FR] INHIBITEURS PYRIMIDINES DE PDE10

  摘要：

  本发明涉及嘧啶化合物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及利用这些化合物治疗神经系统和精神疾病，如精神分裂症、精神病或亨廷顿病，以及与纹状体功能不足或基底神经节功能障碍相关的疾病。

  公开号：

  WO2013028590A1

文献信息

• Pyrimidine PDE10 inhibitors
  申请人：Cox Christopher D.

  公开号：US09062059B2

  公开（公告）日：2015-06-23

  The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及嘧啶类化合物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及使用这些化合物治疗神经系统和精神障碍，例如精神分裂症、精神病或亨廷顿病，以及与纹状体低功能或基底节功能障碍相关的疾病。
• Aryloxmethyl cyclopropane derivatives as PDE10 inhibitors
  申请人：Breslin Michael J.

  公开号：US08975261B2

  公开（公告）日：2015-03-10

  The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及芳基氧甲基环丙烷衍生物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及使用这些化合物治疗神经和精神障碍，如精神分裂症、精神病或亨廷顿病，以及与纹状体功能不足或基底节功能障碍有关的疾病。
• ARYLOXMETHYL CYCLOPROPANE DERIVATIVES AS PDE10 INHIBITORS
  申请人：Breslin Michael J.

  公开号：US20140336195A1

  公开（公告）日：2014-11-13

  The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及芳氧甲基环丙烷衍生物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及使用这些化合物治疗神经系统和精神疾病，如精神分裂症、精神病或亨廷顿病等与纹状体低功能或基底节功能障碍有关的疾病。
• PYRIMIDINE PDE10 INHIBITORS
  申请人：Cox Christopher D.

  公开号：US20140228368A1

  公开（公告）日：2014-08-14

  The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及嘧啶化合物，其作为治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及使用这些化合物治疗神经系统和精神疾病，例如精神分裂症、精神病或亨廷顿病以及与纹状体功能减退或基底节功能障碍相关的疾病。
• Process for producing substituted methylamine compound and triazine derivative
  申请人：NIPPON SODA CO., LTD.

  公开号：EP2650283A1

  公开（公告）日：2013-10-16

  The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid. (wherein A represents an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, R represents a hydrogen atom, an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, L represents a halogen atom and the like, and n represents an integer of 2 to 20)

  本发明提供了一种工艺，该工艺可使作为生产农药和医药中间体的取代甲胺化合物的生产变得简单、收率高且成本低，同时还提供了其生产中间体。该工艺包括以下步骤：将式（I）代表的六亚甲基四铵盐化合物与碱反应，得到式（II）代表的 N-亚甲基取代甲胺低聚物或两种或两种以上低聚物的混合物；在酸存在下水解式（II）代表的 N-亚甲基取代甲胺低聚物或两种或两种以上低聚物的混合物。 (其中 A 代表烃基或杂环基的有机基团，或具有取代基的有机基团，R 代表氢原子、烃基或杂环基的有机基团，或具有取代基的有机基团，L 代表卤素原子等，n 代表 2 至 20 的整数）。