6-(2-chloro-6-methylphenyl)-2-methylpyrido[2,3-d]-pyrimidin-7-amine | 76574-82-8

• 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-chloro-6-methylphenyl)-2-methylpyrido[2,3-d]-pyrimidin-7-amine
• 英文别名: 6-(2-chloro-6-methylphenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine
• CAS: 76574-82-8
• 化学式: C₁₅H₁₃ClN₄
• 分子量: 284.748
• InChiKey: BCAXDBAUNQCLBL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  64.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-氯-6-甲基苯甲醛 在 sodium tetrahydroborate 、 氯化亚砜 、 sodium ethanolate 作用下， 以 甲醇 、 乙醇 、 水 、 苯 为溶剂， 反应 24.0h， 生成 6-(2-chloro-6-methylphenyl)-2-methylpyrido[2,3-d]-pyrimidin-7-amine
  参考文献：
  名称：

  Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives

  摘要：

  A series of 51 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat. A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg. Normalized blood pressure levels could then be maintained by single daily oral doses. The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.

  DOI：

  10.1021/jm00136a006

文献信息

• 6-Substituted-arylpyrido[2,3-d]pyrimidin-7-amines and derivatives
  申请人：Warner-Lambert Company

  公开号：US04271164A1

  公开（公告）日：1981-06-02

  6-Substituted-arylpyrido[2,3-d]pyrimidin-7-amines and derivatives and their pharmaceutically acceptable acid addition salts are useful in the treatment of hypertension.

  6-取代基芳基吡啶[2,3-d]嘧啶-7-胺及其衍生物和其药学上可接受的酸加盐在高血压治疗中有用。
• 6-Substituted-arylpyrido(2,3-d)pyrimidin-7-amines, derivatives and salts thereof, pharmaceutical compositions containing any of the foregoing, and processes for producing any of the foregoing
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0018151B1

  公开（公告）日：1984-01-25
• US4271164A
  申请人：——

  公开号：US4271164A

  公开（公告）日：1981-06-02
• Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives
  作者：Lawrence R. Bennett、C. John Blankley、Robert W. Fleming、Ronald D. Smith、Deirdre K. Tessman

  DOI：10.1021/jm00136a006

  日期：1981.4

  A series of 51 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat. A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg. Normalized blood pressure levels could then be maintained by single daily oral doses. The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.