6-(2-Methyl-thiazol-4-yl)-4,5-dimethoxy-pyridine-2-carboxylic acid

• 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: 6-(2-Methyl-thiazol-4-yl)-4,5-dimethoxy-pyridine-2-carboxylic acid
• 英文别名: 4,5-Dimethoxy-6-(2-methyl-thiazol-4-yl)-pyridine-2-carboxylic acid；4,5-dimethoxy-6-(2-methyl-1,3-thiazol-4-yl)pyridine-2-carboxylic acid
• 化学式: C₁₂H₁₂N₂O₄S
• 分子量: 280.304
• InChiKey: DWFTZQBAKOCVDZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  110
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  Methyl 6-(2-bromoacetyl)-4,5-dimethoxypyridine-2-carboxylate 在 sodium hydroxide 作用下， 以 1,4-二氧六环 、 甲醇 为溶剂， 反应 2.0h， 生成 6-(2-Methyl-thiazol-4-yl)-4,5-dimethoxy-pyridine-2-carboxylic acid
  参考文献：
  名称：

  Synthesis of novel substituted pyridines as inhibitors of endothelin coverting enzyme-1 (ECE-1)

  摘要：

  A series of bi-aryl pyridine carboxylic acids has been prepared and evaluated as inhibitors of ECE-1. The analogs were prepared by Pd catalyzed cross couplings of halogenated pyridines with heteroaryl organo -boranes, -tinate or -zincate derivatives. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00375-8

文献信息

• Small molecule biaryl compounds as inhibitors of endothelin converting
  申请人：Warner-Lambert Company

  公开号：US05891892A1

  公开（公告）日：1999-04-06

  Novel small molecular biaryl compounds as inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.

  描述了作为内皮素转化酶抑制剂的新型小分子联苯化合物，以及其制备方法和药物组合物，这些对于治疗内皮素水平升高、急性和慢性肾衰竭、高血压、心肌梗死、心肌缺血、脑血管痉挛、脑缺血、脑梗死、肝硬化、脓毒性休克、充血性心力衰竭、内毒素休克、蛛网膜下出血、心律失常、哮喘、子痫前期、包括雷诺氏病和再狭窄症在内的动脉粥样硬化疾病、心绞痛、癌症、肺动脉高压、缺血性疾病、胃黏膜损伤、出血性休克、缺血性肠病、中风、良性前列腺增生（BPH）和糖尿病等方面是有用的。
• US5891892A
  申请人：——

  公开号：US5891892A

  公开（公告）日：1999-04-06
• Synthesis of novel substituted pyridines as inhibitors of endothelin coverting enzyme-1 (ECE-1)
  作者：Mark A. Massa、William C. Patt、Kyunghye Ahn、Andre M. Sisneros、Sarah B. Herman、Annette Doherty

  DOI：10.1016/s0960-894x(98)00375-8

  日期：1998.8

  A series of bi-aryl pyridine carboxylic acids has been prepared and evaluated as inhibitors of ECE-1. The analogs were prepared by Pd catalyzed cross couplings of halogenated pyridines with heteroaryl organo -boranes, -tinate or -zincate derivatives. (C) 1998 Elsevier Science Ltd. All rights reserved.