4-pyridyl tert-butyl sulfoxide | 142075-47-6

• 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
• 英文名称: 4-pyridyl tert-butyl sulfoxide
• 英文别名: 4-Tert-butylsulfinylpyridine
• CAS: 142075-47-6
• 化学式: C₉H₁₃NOS
• 分子量: 183.274
• InChiKey: VCHBNCBRPVXHKN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  49.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-pyridyl tert-butyl sulfoxide 、 碘甲烷 在 lithium diisopropyl amide 作用下， 生成 3-Methyl-4-(2-methyl-propane-2-sulfinyl)-pyridine
  参考文献：
  名称：

  叔丁基丁基亚砜定向的邻金属化基团。取代的芳族化合物和吡啶的新合成方法以及与其他金属化导向剂的比较

  摘要：

  叔丁基苯基亚砜（的邻位定向金属化反应的细节1和2-和4-叔丁基吡啶基亚砜（3A，3B与既定的金属化主管（CONR比较沿着描述2，OCONR 2，OMOM，SO 2吨-Bu）通过分子间和分子内竞争实验。

  DOI：

  10.1016/s0040-4039(00)79042-3

文献信息

• Amino Compounds for Treatment of Complement Mediated Disorders
  申请人：Achillion Pharmaceuticals, Inc.

  公开号：US20150239894A1

  公开（公告）日：2015-08-27

  Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R 12 or R 13 on the A group is an amino substituent (R 32 ) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

  本文提供了公式I或其药学上可接受的盐或组合物所组成的抑制补体因子D的化合物、使用方法和制备过程，其中A组上的R12或R13是氨基取代基（R32）。所述抑制剂靶向因子D并在替代性补体途径的早期和关键点上抑制或调节补体级联反应，并减少因子D调节经典和凝集素补体途径的能力。本文所述的因子D抑制剂能够减少过度激活补体，这与某些自身免疫性、炎症性和神经退行性疾病以及缺血再灌注损伤和癌症有关。
• Amino compounds for treatment of complement mediated disorders
  申请人：Achillion Pharmaceuticals, Inc.

  公开号：US10689409B2

  公开（公告）日：2020-06-23

  Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

  本研究提供了由式 I 或其药学上可接受的盐或组合物组成的补体因子 D 抑制剂的化合物、使用方法和制造工艺，其中 A 基上的 R12 或 R13 是氨基取代基 (R32)。本文所述的抑制剂以因子 D 为靶点，在替代补体途径的早期和关键点抑制或调节补体级联，并降低因子 D 调节经典和凝集素补体途径的能力。本文所述的因子 D 抑制剂能够减少补体的过度活化，而补体的过度活化与某些自身免疫性、炎症性和神经退行性疾病以及缺血再灌注损伤和癌症有关。
• AMINO COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS
  申请人：Achillion Pharmaceuticals, Inc.

  公开号：US20190144473A1

  公开（公告）日：2019-05-16

  Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R 12 or R 13 on the A group is an amino substituent (R 32 ) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
• US9598446B2
  申请人：——

  公开号：US9598446B2

  公开（公告）日：2017-03-21