5-Amino-6-methyl-2,3-dihydro-[1,3]thiazolo[3,2-a]pyrimidin-7-one | 149221-61-4

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 英文名称: 5-Amino-6-methyl-2,3-dihydro-[1,3]thiazolo[3,2-a]pyrimidin-7-one
• CAS: 149221-61-4
• 化学式: C₇H₉N₃OS
• 分子量: 183.234
• InChiKey: ABAWYKJEPOEZMB-UHFFFAOYSA-N

物化性质

• 沸点：
  317.8±45.0 °C(predicted)
• 密度：
  1.64±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  84
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-Amino-6-methyl-2,3-dihydro-[1,3]thiazolo[3,2-a]pyrimidin-7-one 在 硫酸 作用下， 以 水 为溶剂， 反应 19.0h， 以81%的产率得到8-methyl-2,3-dihydrothiazolo[3,2-c]pyrimidine-5,7-dione
  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-氨基-2-噻唑啉 、 2-氰基丙酸甲酯 在 potassium carbonate 作用下， 以 甲醇 为溶剂， 反应 8.0h， 以53.3%的产率得到5-Amino-6-methyl-2,3-dihydro-[1,3]thiazolo[3,2-a]pyrimidin-7-one
  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.