tert-butyl (3R,5S)-7-(5-(benzylcarbamoyl)-1-(4-fluorophenyl)-4-isopropyl-1H-pyrazol-3-yl)-3,5-dihydroxyhept-6-enoate | 1005476-32-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: tert-butyl (3R,5S)-7-(5-(benzylcarbamoyl)-1-(4-fluorophenyl)-4-isopropyl-1H-pyrazol-3-yl)-3,5-dihydroxyhept-6-enoate
• CAS: 1005476-32-3
• 化学式: C₃₁H₃₈FN₃O₅
• 分子量: 551.658
• InChiKey: RPYBBWREWONORO-JWQCQUIFSA-N

反应信息

• 作为产物：
  描述：

  在 盐酸 作用下， 以 甲醇 为溶剂， 反应 1.5h， 以93%的产率得到tert-butyl (3R,5S)-7-(5-(benzylcarbamoyl)-1-(4-fluorophenyl)-4-isopropyl-1H-pyrazol-3-yl)-3,5-dihydroxyhept-6-enoate
  参考文献：
  名称：

  Substituted Pyrazoles as Hepatoselective HMG-CoA Reductase Inhibitors: Discovery of (3R,5R)-7-[2-(4-Fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic Acid (PF-3052334) as a Candidate for the Treatment of Hypercholesterolemia

  摘要：

  In light of accumulating evidence that aggressive LDL-lowering therapy may offer increased protection against coronary heart disease, we undertook the design and synthesis of a novel series of HMG-CoA reductase inhibitors based upon a substituted pyrazole template. Optimizing this series using both structure-based design and molecular property considerations afforded a class of highly efficacious and hepatoselective inhibitors resulting in the identification of (3 R,5 R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2 H-pyrazol-3-yl]-3,5-dihydroxy-heptanoic (PF-3052334) as a candidate for the treatment of hypercholesterolemia.

  DOI：

  10.1021/jm070849r