5,7-dioxo-3,5,6,7-tetrahydro-2H-thiazolo<3,2-c>pyrimidine-8-carboxylic acid chlorosulfonylamide | 1026969-58-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 5,7-dioxo-3,5,6,7-tetrahydro-2H-thiazolo<3,2-c>pyrimidine-8-carboxylic acid chlorosulfonylamide
• 英文别名: 5,7-dioxo-3,5,6,7-tetrahydro-2H-thiazolo[3,2-c]pyrimidine-8-carboxylic acid chlorosulfonylamide；N-(5,7-dioxo-2,3-dihydro-[1,3]thiazolo[3,2-c]pyrimidine-8-carbonyl)sulfamoyl chloride
• CAS: 1026969-58-3
• 化学式: C₇H₆ClN₃O₅S₂
• 分子量: 311.727
• InChiKey: UIIQPKCAGPDVCQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  146
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  5,7-dioxo-3,5,6,7-tetrahydro-2H-thiazolo<3,2-c>pyrimidine-8-carboxylic acid chlorosulfonylamide 在 N,N-二甲基甲酰胺 作用下， 反应 2.0h， 以46.6%的产率得到5,7-dioxo-3,5,6,7-tetrahydro-2H-thiazolo<3,2-c>pyrimidine-8-carbonitrile
  参考文献：
  名称：

  A new class of potent hypolipemic agents raising high-density lipoproteins. Synthesis, reactions and pharmacological properties

  摘要：

  A series of thiazolo[3,2-c]pyrimidin-5,7-diones has been synthesized. Results from in vivo evaluations in rats have shown that many of these compounds produce a pronounced increase of HDL cholesterol and a marked decrease of LDL and VLDL cholesterol. The most potent compound 17 (30 mg/kg/d per os over 7 d in male rats) led to the following changes: HDL cholesterol + 101%, LDL cholesterol -40%, and VLDL cholesterol -98%. These effects may result in antiatherosclerotic properties in these compounds. The preparation of 7-amino-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-ones and 5-amino-2,3-dihydrothiazolo[3,2-a] pyrimidin-7-ones is described.

  DOI：

  10.1016/0223-5234(94)90105-8
• 作为产物：
  描述：

  2,3-dihydro-thiazolo[3,2-a]pyrimidine-5,7-dione 在 硫酸 、 溶剂黄146 作用下， 以 水 为溶剂， 反应 6.0h， 生成 5,7-dioxo-3,5,6,7-tetrahydro-2H-thiazolo<3,2-c>pyrimidine-8-carboxylic acid chlorosulfonylamide
  参考文献：
  名称：

  A new class of potent hypolipemic agents raising high-density lipoproteins. Synthesis, reactions and pharmacological properties

  摘要：

  A series of thiazolo[3,2-c]pyrimidin-5,7-diones has been synthesized. Results from in vivo evaluations in rats have shown that many of these compounds produce a pronounced increase of HDL cholesterol and a marked decrease of LDL and VLDL cholesterol. The most potent compound 17 (30 mg/kg/d per os over 7 d in male rats) led to the following changes: HDL cholesterol + 101%, LDL cholesterol -40%, and VLDL cholesterol -98%. These effects may result in antiatherosclerotic properties in these compounds. The preparation of 7-amino-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-ones and 5-amino-2,3-dihydrothiazolo[3,2-a] pyrimidin-7-ones is described.

  DOI：

  10.1016/0223-5234(94)90105-8

文献信息

• A new class of potent hypolipemic agents raising high-density lipoproteins. Synthesis, reactions and pharmacological properties
  作者：H FURRER、E GRANZER、R WAGNER

  DOI：10.1016/0223-5234(94)90105-8

  日期：——

  A series of thiazolo[3,2-c]pyrimidin-5,7-diones has been synthesized. Results from in vivo evaluations in rats have shown that many of these compounds produce a pronounced increase of HDL cholesterol and a marked decrease of LDL and VLDL cholesterol. The most potent compound 17 (30 mg/kg/d per os over 7 d in male rats) led to the following changes: HDL cholesterol + 101%, LDL cholesterol -40%, and VLDL cholesterol -98%. These effects may result in antiatherosclerotic properties in these compounds. The preparation of 7-amino-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-ones and 5-amino-2,3-dihydrothiazolo[3,2-a] pyrimidin-7-ones is described.