5-methyl-1-p-tolyl-2-(1H) pyridone

• 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-methyl-1-p-tolyl-2-(1H) pyridone
• 英文别名: 5-Methyl-1-p-tolyl-2-(1H)-pyridone；5-methyl-1-(4-methylphenyl)pyridin-2-one
• 化学式: C₁₃H₁₃NO
• 分子量: 199.252
• InChiKey: ZVEJTXODUXFIAO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  15
• 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：
  1

反应信息

• 作为产物：
  描述：

  4-碘甲苯 、 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94%的产率得到5-methyl-1-p-tolyl-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

• Macrocyclic compounds as inhibitors of viral replication
  申请人：Blatt M. Lawrence

  公开号：US20050267018A1

  公开（公告）日：2005-12-01

  The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

  该实施例提供了一般式I-XIX的化合物，以及包括药物组合在内的组合物，其中包括一种主体化合物。该实施例还提供了治疗方法，包括治疗黄病毒感染的方法，包括丙型肝炎病毒感染的方法和治疗肝纤维化的方法，这些方法通常涉及向需要的个体施用一种主体化合物或组合物的有效量。
• 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。
• 5-Methyl-1-phenyl-2-(1H)-pyridone compositions and methods of use
  申请人：Affiliated Medical Research, Inc.

  公开号：US03974281A1

  公开（公告）日：1976-08-10

  Novel analgesic, anti-pyretic, anti-inflammatory compositions containing as the active ingredient the compound, 5-methyl-1-phenyl-2-(1H)-pyridone are described. Such compositions have also been found to cause significant lowering of serum uric acid and glucose levels and to be effective in the treatment of a number of upper respiratory ailments in humans and other mammals. Skin conditions such as dermatitis and poison ivy are also alleviated by this agent. The compositions containing 5-methyl-1-phenyl-2-(1H)-pyridone caused no irritation on oral administration or when applied to specific target tissues showed no significant irritation or other sequelae.

  描述了一种含有活性成分5-甲基-1-苯基-2-(1H)-吡啶酮的新型镇痛、退烧、抗炎组合物。这种组合物还被发现能显著降低血清尿酸和葡萄糖水平，并对人类和其他哺乳动物的多种上呼吸道疾病治疗有效。皮肤状况如皮炎和毒葛也可以通过这种药物缓解。含有5-甲基-1-苯基-2-(1H)-吡啶酮的组合物在口服时不引起刺激，在应用于特定靶组织时也没有显著的刺激或其他后遗症。
• Method for reducing serum glucose levels
  申请人：Affiliated Medical Research, Inc.

  公开号：US04042699A1

  公开（公告）日：1977-08-16

  Novel pharmaceutical compositions containing as the active ingredient the compound 5-methyl-1-phenyl-2-(1H)-pyridone are described. Such compositions have been found to have a metabolic property which causes significant lowering of serum glucose levels in humans and other mammals. The compositions containing 5-methyl-1-phenyl-2-(1H)-pyridone caused no irritation on oral administration or when applied to specific target tissues showed no significant irritation or other sequelae.

  本发明涉及一种含有化合物5-甲基-1-苯基-2-(1H)-吡啶酮作为活性成分的新型药物组合物。发现这种组合物具有代谢特性，可以显著降低人类和其他哺乳动物的血清葡萄糖水平。含有5-甲基-1-苯基-2-(1H)-吡啶酮的组合物在口服时不引起刺激，在应用于特定目标组织时也没有显著的刺激或其他后遗症。
• Method for reducing serum uric acid levels
  申请人：Affiliated Medical Research, Inc.

  公开号：US04052509A1

  公开（公告）日：1977-10-04

  Novel pharmaceutical compositions containing as the active ingredient the compound 5-methyl-1-phenyl-2-(1H)-pyridone are described. Such compositions have been found to have a metabolic property which causes significant lowering of serum uric acid levels in humans and other mammals. The compositions containing 5-methyl-1-phenyl-2-(1H)-pyridone caused no irritation on oral administration or when applied to specific target tissues showed no significant irritation or other sequelae.

  本发明涉及一种新型药物组合物，其活性成分为5-甲基-1-苯基-2-(1H)-吡啶酮化合物。已发现这种组合物具有代谢特性，能显著降低人类和其他哺乳动物的血清尿酸水平。含有5-甲基-1-苯基-2-(1H)-吡啶酮的组合物在口服时不会引起刺激，应用于特定目标组织时也不会出现明显的刺激或其他后遗症。