1-(3'-methoxyphenyl)-5-methyl-2(1H)-pyridone

• 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: 1-(3'-methoxyphenyl)-5-methyl-2(1H)-pyridone
• 英文别名: (3'-methoxyphenyl)-5-methyl-2(1H)-pyridone；1-(3-Methoxyphenyl)-5-methylpyridin-2-one
• 化学式: C₁₃H₁₃NO₂
• 分子量: 215.252
• InChiKey: NUUFOILDYXVXLL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  3-碘苯甲醚 、 2-羟基-5-甲基嘧啶 在 copper(l) iodide potassium phosphate 、 N,N'-二甲基乙二胺 作用下， 以 1,4-二氧六环 为溶剂， 以78%的产率得到1-(3'-methoxyphenyl)-5-methyl-2(1H)-pyridone
  参考文献：
  名称：

  基于布赫瓦尔德规程的吡啶-2-酮与芳基和杂环卤化物的高效铜催化偶联反应

  摘要：

  已经建立了基于布赫瓦尔德协议的高效铜催化的偶联反应，用于吡啶-2-酮与芳基碘化物，芳基溴化物和杂环溴化物。

  DOI：

  10.1016/j.tetlet.2004.04.019

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。
• ANTI-FIBROTIC PYRIDINONES
  申请人：InterMune, Inc.

  公开号：US20140107110A1

  公开（公告）日：2014-04-17

  Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

  本发明涉及吡啶酮化合物、制备这些化合物的方法以及治疗纤维化疾病的方法。
• 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。
• 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.
• COMPOSITION AND METHOD FOR TREATING FIBROTIC DISEASES
  申请人：TAO Li Jian

  公开号：US20090258911A1

  公开（公告）日：2009-10-15

  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.