3-碘-4-甲基吡啶-2-胺 | 1227509-37-6

• 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
• 中文名称: 3-碘-4-甲基吡啶-2-胺
• 英文名称: 3-Iodo-4-methylpyridin-2-amine
• CAS: 1227509-37-6
• 化学式: C₆H₇IN₂
• 分子量: 234.039
• InChiKey: NWASPRQQZYVWTO-UHFFFAOYSA-N

物化性质

• 沸点：
  298.4±40.0 °C(Predicted)
• 密度：
  1.898±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为产物：
  描述：

  2-氨基-4-甲基吡啶 在 N-碘代丁二酰亚胺 、 溶剂黄146 作用下， 以 苯 为溶剂， 反应 72.0h， 以13%的产率得到3-碘-4-甲基吡啶-2-胺
  参考文献：
  名称：

  N-碘代琥珀酰亚胺在苯胺碘化的区域化学中的显着变化：1,2-二氯-3,4-二碘苯的合成

  摘要：

  通过NIS在极性溶剂（例如DMSO）中直接对苯胺进行碘化，可得到对碘化的产品，其区域选择性高达> 99％。在AcOH存在下改用极性较小的溶剂（例如苯）会使该结果转向邻位异构体的急剧增加或优先生成，区域选择性也高达> 99％。该发现被用于合成1,2-二氯-3,4-二碘苯。 芳香胺-亲电取代-卤化-区域选择性-溶剂效应

  DOI：

  10.1055/s-0031-1290118

文献信息

• PYRIDONE DERIVATIVE HAVING TETRAHYDROPYRANYLMETHYL GROUP
  申请人：DAIICHI SANKYO COMPANY, LIMITED

  公开号：US20170183329A1

  公开（公告）日：2017-06-29

  The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl. The present disclosure provides pyridone derivatives having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or salts thereof, or crystals of the compounds or the salts, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, X, Y, and Z are each as defined in the specification:

  本公开提供了新颖的化合物或其盐，或者该化合物或盐的晶体，其抑制Axl并在治疗由Axl高功能引起的疾病、与Axl高功能相关的疾病的治疗和/或涉及Axl高功能的疾病的治疗中有用。本公开提供了具有以下式（I）所代表的四氢吡喃基甲基基团的吡啶酮衍生物，具有各种取代基，或其盐，或化合物或盐的晶体，其中R1、R2、R3、R4、R5、W、X、Y和Z均如规范中定义的。
• C-Ring Modified Tricyclic Benzonaphthiridinone Protein Kinase Inhibitors and Use Thereof
  申请人：Xiao Yufang

  公开号：US20110312951A1

  公开（公告）日：2011-12-22

  Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.

  本发明涉及C环修饰的三环苯并那敏酮化合物及其类似物、包含这些化合物的制药组合物和制备这些化合物的方法。这些化合物在治疗易受蛋白激酶信号转导抑制、调节和/或调控的疾病方面是有用的。
• PYRIDONE DERIVATIVE HAVING TETRAHYDROPYRANYL METHYL GROUP
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3168219A1

  公开（公告）日：2017-05-17

  It is intended to provide a novel compound or a salt thereof, or crystals of the compound or the salt, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl. [Solution] The present invention provides a pyridone derivative having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or a salt thereof, or crystals of the compound or the salt (wherein R1, R2, R3, R4, R5, W, X, Y, and Z are each as defined in the specification).

  本发明旨在提供一种新型化合物或其盐，或该化合物或其盐的结晶，该化合物或其盐可抑制 Axl，并可用于治疗由 Axl 功能亢进引起的疾病、治疗与 Axl 功能亢进相关的疾病和/或治疗涉及 Axl 功能亢进的疾病。 [解决方案］ 本发明提供一种吡啶酮衍生物，该衍生物具有下式（I）所代表的具有各种取代基的四氢吡喃甲基，或其盐，或该化合物或该盐的结晶（其中R1、R2、R3、R4、R5、W、X、Y和Z各自如说明书中所定义）。
• Pyridone derivatives having tetrahydropyranylmethyl groups
  申请人：DAIICHI SANKYO COMPANY, LIMITED

  公开号：US10442797B2

  公开（公告）日：2019-10-15

  The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl. The present disclosure provides pyridone derivatives having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or salts thereof, or crystals of the compounds or the salts, wherein R1, R2, R3, R4, R5, W, X, Y, and Z are each as defined in the specification:

  本公开提供了新型化合物或其盐，或化合物或其盐的结晶，它们抑制Axl，可用于治疗由Axl功能亢进引起的疾病、治疗与Axl功能亢进相关的疾病和/或治疗涉及Axl功能亢进的疾病。 本公开提供了具有下式(I)所代表的具有各种取代基的四氢吡喃甲基的吡啶酮衍生物，或其盐，或化合物或其盐的结晶，其中R1、R2、R3、R4、R5、W、X、Y和Z各自如说明书中所定义：
• PYRIDONE DERIVATIVES HAVING TETRAHYDROPYRANYLMETHYL GROUPS
  申请人：DAIICHI SANKYO COMPANY, LIMITED

  公开号：US20180148436A2

  公开（公告）日：2018-05-31

  The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl. The present disclosure provides pyridone derivatives having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or salts thereof, or crystals of the compounds or the salts, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, X, Y, and Z are each as defined in the specification: