5-methyl-1-[4-(trifluoromethyl)phenyl]pyridin-2-one

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-methyl-1-[4-(trifluoromethyl)phenyl]pyridin-2-one
• 英文别名: 5-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one；5-methyl-1-(4'-trifluoromethylphenyl)-2(1H)-pyridone
• 化学式: C₁₃H₁₀F₃NO
• 分子量: 253.224
• InChiKey: IKTCWTVJVXLKRU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-methyl-1-[4-(trifluoromethyl)phenyl]pyridin-2-one 在 N-溴代丁二酰亚胺(NBS) 、 偶氮二异丁腈 作用下， 以 四氯化碳 为溶剂， 以84%的产率得到5-(bromomethyl)-1-[4-(trifluoromethyl)phenyl] pyridin-2-one
  参考文献：
  名称：

  HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE CONTAINING SAME

  摘要：

  公开号：

  EP3412664B1
• 作为产物：
  描述：

  4-碘三氟甲苯 、 2-羟基-5-甲基嘧啶 在 potassium phosphate 、 copper(l) iodide 、 N,N'-二甲基乙二胺 作用下， 以 1,4-二氧六环 为溶剂， 以91%的产率得到5-methyl-1-[4-(trifluoromethyl)phenyl]pyridin-2-one
  参考文献：
  名称：

  HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE CONTAINING SAME

  摘要：

  公开号：

  EP3412664B1

文献信息

• COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS
  申请人：Kossen Karl

  公开号：US20090318455A1

  公开（公告）日：2009-12-24

  Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

  公开了用于治疗炎症和纤维化疾病的化合物和方法，包括用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物对p38 MAPK的抑制效力较低；并且其中接触是在SAPK调节浓度下进行的，该浓度对化合物抑制p38 MAPK的抑制浓度百分比较低。还公开了吡非尼酮的衍生物和类似物，它们可用于调节应激活化蛋白激酶（SAPK）系统。
• Ni‐Catalyzed Photochemical C−N Coupling of Amides with (Hetero)aryl Chlorides
  作者：Geyang Song、Qi Li、Ding‐Zhan Nong、Jiameng Song、Gang Li、Chao Wang、Jianliang Xiao、Dong Xue

  DOI：10.1002/chem.202300458

  日期：2023.7.3

  A photochemical C−N coupling reaction of (hetero)aryl halides with amides using NiCl2-bipyridine complex as a pre-catalyst in the absence of an external photocatalyst is reported, allowing a broad array of aryl chlorides to be converted into the corresponding (hetero)arylamides.

  据报道，在没有外部光催化剂的情况下，使用 NiCl 2 -联吡啶复合物作为预催化剂，（杂）芳基卤化物与酰胺发生光化学 CN 偶联反应，使多种芳基氯化物转化为相应的（杂）芳基酰胺。
• 1-(SUBSTITUTED PHENYL)-5- METHYL- 2 - (1H) PYRIDONE IN THE MANUFACTURE OF MEDICAMENTS FOR TREATING FIBROSIS IN ORGANS OR TISSUES
  申请人：Xiangya Hospital of Central South University

  公开号：EP1878428A1

  公开（公告）日：2008-01-16

  The use of 1-(substituted phenyl)-5-methyl-2-(1H) pyridone in the manufacture of medicaments for treating fibrosis in organs or tissues. It indicates that 1-(substituted phenyl)-5-methyl-2-(1H) pyridone can inhibit the cells produced by various ECM, and their effect is higher than pirfenidone. Therefore, this tpye of compounds can be used as active ingredient for preparing the antifibrotic agent in organs and tissues.

  将 1-(取代苯基)-5-甲基-2-(1H)吡啶酮用于制造治疗器官或组织纤维化的药物。研究表明，1-（取代苯基）-5-甲基-2-（1H）吡啶酮能抑制由各种 ECM 产生的细胞，其效果高于吡非尼酮。因此，这类化合物可作为制备器官和组织抗纤维化剂的活性成分。
• Heterocyclic sulfonamide derivative and medicine containing same
  申请人：EA Pharma Co., Ltd.

  公开号：US10584116B2

  公开（公告）日：2020-03-10

  Compounds of represented by formula (I): wherein each symbol is defined herein and pharmaceutically acceptable salts thereof exhibit TRPA1 antagonist activity and are useful as TRPA1 antagonists and the prophylaxis or treatment of diseases involving TRPA1.

  式 (I) 所代表的化合物： 其中各符号在此定义，其药学上可接受的盐类具有 TRPA1 拮抗剂活性，可用作 TRPA1 拮抗剂，预防或治疗涉及 TRPA1 的疾病。
• Composition and Method for Treating Fibrotic Diseases
  申请人：Tao Jian Li

  公开号：US20070203203A1

  公开（公告）日：2007-08-30

  The present invention discloses 5-methyl-1-(substituted phenyl)-2(1H)-pyridones have enhanced anti-fibrotic activities than 5-methyl-1-(non-substituted phenyl)-2(1H)-pyridones. An representative example of 5-methyl-(1-substituted phenyl)-2(1H)-pyridones is 1-(3′-fluorophenyl)-5-methyl-2(1H)-pyridone. Accordingly, there are provided compositions comprising one or more compounds selected from the group consisting of 5-methyl-1-(substituted phenyl)-2(1H)-pyridones and methods of using the same to treat or prevent fibrosis diseases.