5-fluoro-6-(trifluoromethyl)picolinic acid | 1256802-73-9

• 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: 5-fluoro-6-(trifluoromethyl)picolinic acid
• 英文别名: 5-Fluoro-6-(trifluoromethyl)pyridine-2-carboxylic acid
• CAS: 1256802-73-9
• 化学式: C₇H₃F₄NO₂
• 分子量: 209.1
• InChiKey: ZVEWDUKKJBNCSN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  50.2
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  5-fluoro-6-(trifluoromethyl)picolinic acid 、 (2S,5r)-1-boc-2,5-二甲基哌嗪 在 N,N-二异丙基乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 乙腈 为溶剂， 以84 %的产率得到tert-butyl (2S,5R)-4-(5-fluoro-6-(trifluoromethyl)picolinoyl)-2,5-dimethylpiperazine-1-carboxylate
  参考文献：
  名称：

  [EN] TRICYCLIC TRIAZOLO COMPOUNDS AS DGK INHIBITORS
  [FR] COMPOSÉS TRIAZOLO TRICYCLIQUES UTILISÉS COMME INHIBITEURS DE DGK

  摘要：

  本申请提供了调节二酰甘油激酶（DGK）活性的三环三唑化合物 I，可用于治疗包括癌症在内的各种疾病。

  公开号：

  WO2023239768A1

文献信息

• IMIDAZOLYL PYRIMIDINYLAMINE COMPOUNDS AS CDK2 INHIBITORS
  申请人：Incyte Corporation

  公开号：US20210047294A1

  公开（公告）日：2021-02-18

  The present application provides imidazolyl pyrimidinylamine inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

  本申请提供了嘧啶基咪唑基胺类细胞周期蛋白依赖性激酶2（CDK2）抑制剂，以及其药物组合物和使用这些物质治疗癌症的方法。
• IMIDAZO[1,2-A]PYRIDINYL DERIVATIVES AS IRAK4 INHIBITORS
  申请人：BIOGEN MA INC.

  公开号：US20220089592A1

  公开（公告）日：2022-03-24

  This invention relates to Imidazo[1,2-a]pyridinyl Derivatives of formula (I′), or pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, capable of modulating the activity of IRAK4. The invention further provides a method of manufacturing compounds of the invention, and methods for their therapeutic use. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including inflammatory disease, autoimmune disease, cancer, cardiovascular disease, a disease of the central nervous system, disease of the skin, an ophthalmic disease and condition, and a bone disease.

  这项发明涉及Imidazo[1,2-a]pyridinyl Derivatives的化合物（I′）或其药学上可接受的盐，其中所有变量如规范中所定义，能够调节IRAK4的活性。该发明进一步提供了一种制造该发明化合物的方法，以及它们在治疗中的方法。该发明还提供了它们的制备方法，医学用途，特别是在治疗和管理炎症性疾病、自身免疫疾病、癌症、心血管疾病、中枢神经系统疾病、皮肤疾病、眼科疾病和骨骼疾病等疾病或疾病的用途。
• [EN] IMIDAZO[1,2-A]PYRIDINYL DERIVATIVES AS IRAK4 INHIBITORS<br/>[FR] DÉRIVÉS D'IMIDAZO[1,2-A]PYRIDINYLE SERVANT D'INHIBITEURS D'IRAK4
  申请人：BIOGEN MA INC

  公开号：WO2020150626A1

  公开（公告）日：2020-07-23

  This invention relates to Imidazo[1,2-a]pyridinyl Derivatives of formula (I'), or pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, capable of modulating the activity of IRAK4. The invention further provides a method of manufacturing compounds of the invention, and methods for their therapeutic use. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including inflammatory disease, autoimmune disease, cancer, cardiovascular disease, a disease of the central nervous system, disease of the skin, an ophthalmic disease and condition, and a bone disease.
• [EN] IMIDAZOLYL PYRIMIDINYLAMINE COMPOUNDS AS CDK2 INHIBITORS<br/>[FR] COMPOSÉS IMIDAZOLYL-PYRIMIDINYLAMINES UTILISÉS COMME INHIBITEURS DE LA CDK2
  申请人：INCYTE CORP

  公开号：WO2021030537A1

  公开（公告）日：2021-02-18

  The present application provides imidazolyl pyrimidinylamine inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.