4-bromo-1-isopentylpyridin-2(1H)-one | 1127499-10-8

• 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-bromo-1-isopentylpyridin-2(1H)-one
• 英文别名: 4-bromo-1-(3-methylbutyl)pyridin-2-one
• CAS: 1127499-10-8
• 化学式: C₁₀H₁₄BrNO
• 分子量: 244.131
• InChiKey: DFEPEYKJYRODLN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  4-bromo-1-isopentylpyridin-2(1H)-one 在 bis-triphenylphosphine-palladium(II) chloride 、 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 、 potassium acetate 、 potassium carbonate 、 联硼酸频那醇酯 作用下， 以 水 、 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 0.25h， 生成 4-(3-acetylimidazo[1,2-b]pyridazin-6-yl)-1-isopentylpyridin-2(1H)-one
  参考文献：
  名称：

  [EN] IMIDAZO[1,2-b]PYRIDAZINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE
  [FR] COMPOSÉS À BASE D'IMIDAZO[1,2-B]PYRIMIDINE, COMPOSITIONS LES COMPRENANT ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  本文披露了基于咪唑并[1,2-b]吡啶嗪的化合物的公式：其中R1、R2和R3在此处定义。还披露了包含这些化合物的组合物以及它们用于治疗、管理和/或预防由适配器相关激酶1活性介导的疾病和疾病的方法。

  公开号：

  WO2015035167A1
• 作为产物：
  描述：

  1-溴代异戊烷 、 4-溴-2-羟基吡啶 在 sodium hydride 、 lithium bromide 作用下， 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 1.5h， 生成 4-bromo-1-isopentylpyridin-2(1H)-one
  参考文献：
  名称：

  [EN] PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE
  [FR] COMPOSÉS À BASE DE PYRAZOLO[1,5-A] PYRIMIDINE, COMPOSITIONS LES COMPRENANT ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  公开了以式(I)为基础的吡唑并[1,5-a]嘧啶化合物，其中R1、R2和R3在此处定义。还公开了包含这些化合物的组合物以及它们用于治疗、管理和/或预防由适配器相关激酶1活性介导的疾病和疾病的方法。

  公开号：

  WO2015035117A1

文献信息

• [EN] 1,3-DISUBSTITUTED-4-PHENYL-1 H-PYRIDIN-2-ONES<br/>[FR] 4-PHÉNYLE-1H-PYRIDINE-2-ONES 1,3-DISUBSTITUÉES
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2009033703A1

  公开（公告）日：2009-03-19

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新颖化合物，特别是根据式（I）的新型吡啶酮衍生物，其中所有基团如申请和权利要求中所定义。根据本发明的化合物是代谢型受体-亚型2（'mGluR2'）的阳性变构调节剂，用于治疗或预防与谷氨酸功能障碍相关的神经和精神疾病以及涉及代谢型受体mGluR2亚型的疾病。具体来说，这些疾病是中枢神经系统疾病，包括焦虑、精神分裂症、偏头痛、抑郁症和癫痫等。该发明还涉及制备这种化合物和组合物的药物组合物和过程，以及利用这种化合物预防和治疗涉及mGluR2的疾病。
• [EN] 1',3'-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H, 1'H-[1, 4'] BIPYRIDINYL-2'-ONES<br/>[FR] 4-PHÉNYL-3,4,5,6-TÉTRAHYDRO-2H,1'H-[1, 4'] BIPYRIDINYL-2'-ONES 1', 3'-DISUSBSTITUÉES
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2009033704A1

  公开（公告）日：2009-03-19

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新型化合物，特别是根据式（I）中定义的新型吡啶酮衍生物，其中所有基团均如申请和权利要求中所定义。根据本发明的化合物是代谢型受体亚型2（'mGluR2'）的阳性变构调节剂，用于治疗或预防与谷氨酸功能障碍相关的神经系统和精神疾病，以及mGluR2代谢型受体亚型涉及的疾病。具体来说，这些疾病是来自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病的选择性疾病。本发明还涉及制备这种化合物和组合物的药物组合物和方法，以及利用这种化合物预防和治疗mGluR2涉及的疾病。
• [EN] PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE<br/>[FR] COMPOSÉS À BASE DE PYRAZOLO[1,5-A] PYRIMIDINE, COMPOSITIONS LES COMPRENANT ET LEURS PROCÉDÉS D'UTILISATION
  申请人：LEXICON PHARMACEUTICALS INC

  公开号：WO2015035117A1

  公开（公告）日：2015-03-12

  Pyrazolo[1,5-a]pyrimidine-based compounds of the formula (I) are disclosed, wherein R1, R2 and R3 are defined herein. Compositions comprising the compounds and methods of their use to treat, manage and/or prevent diseases and disorders mediated by mediated by adaptor associated kinase 1 activity are also disclosed.

  公开了以式(I)为基础的吡唑并[1,5-a]嘧啶化合物，其中R1、R2和R3在此处定义。还公开了包含这些化合物的组合物以及它们用于治疗、管理和/或预防由适配器相关激酶1活性介导的疾病和疾病的方法。
• 1,3-DISUBSTITUTED-4-PHENYL-1H-PYRIDIN-2-ONES
  申请人：Cid-Nunez Jose Maria

  公开号：US20100240706A1

  公开（公告）日：2010-09-23

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新型化合物，特别是根据公式(I)定义的新型吡啶酮衍生物，其中所有基团均如本申请和权利要求中所定义。本发明的化合物是代谢型受体亚型2（“mGluR2”）的阳性变构调节剂，可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及代谢型受体亚型mGluR2的疾病。特别地，这些疾病是选择自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病的一组。本发明还涉及制备此类化合物和组合物的制药组合和过程，以及使用此类化合物预防和治疗涉及mGluR2的上述疾病。
• 1,3-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H,1 H-1,4 BIPYRIDINYL-2-ONES
  申请人：Cid-Nunez Jose Maria

  公开号：US20100240688A1

  公开（公告）日：2010-09-23

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及一种新型化合物，特别是公式（I）中所示的新型吡啶酮衍生物，其中所有基团均如申请和权利要求中所定义。本发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体mGluR2亚型的疾病。特别是，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病中选择的。本发明还涉及制备这种化合物和组合物的制药组合物和制备过程，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病的用途。