4-(2-{[(9H-Fluoren-9-ylmethoxycarbonyl)-(2-methoxy-1-methyl-ethyl)-amino]-methyl}-phenyl)-piperazine-1-carboxylic acid tert-butyl ester | 865303-24-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: 4-(2-{[(9H-Fluoren-9-ylmethoxycarbonyl)-(2-methoxy-1-methyl-ethyl)-amino]-methyl}-phenyl)-piperazine-1-carboxylic acid tert-butyl ester
• CAS: 865303-24-8
• 化学式: C₃₅H₄₃N₃O₅
• 分子量: 585.744
• InChiKey: OPPGHJPLDMJSIJ-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  4-(2-{[(9H-Fluoren-9-ylmethoxycarbonyl)-(2-methoxy-1-methyl-ethyl)-amino]-methyl}-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 在 1-羟基苯并三唑 、 1-(3-二甲基氨基丙基)-3-乙基碳二亚胺 、 二乙胺 、 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 Thiophene-2-carboxylic acid [(R)-1-(2,4-dichloro-benzyl)-2-(4-{2-[(2-methoxy-1-methyl-ethylamino)-methyl]-phenyl}-piperazin-1-yl)-2-oxo-ethyl]-amide
  参考文献：
  名称：

  Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor

  摘要：

  Piperazinebenzylamines bearing a small N-(1-methoxy-2-propyl) side chain were found to be potent and selective antagonists of the human melanocortin-4 (MC4) receptor. Compound 7b, having K-i values of 6.9 and 2800 nM at the human MC4 and MC3 receptors, respectively, has moderate oral bioavailability in mice, which is improved relative to the arylethyl analogues. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.06.058
• 作为产物：
  描述：

  4-{2-[(2-Methoxy-1-methyl-ethylamino)-methyl]-phenyl}-piperazine-1-carboxylic acid tert-butyl ester 、 氯甲酸-9-芴基甲酯 以82%的产率得到4-(2-{[(9H-Fluoren-9-ylmethoxycarbonyl)-(2-methoxy-1-methyl-ethyl)-amino]-methyl}-phenyl)-piperazine-1-carboxylic acid tert-butyl ester
  参考文献：
  名称：

  Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor

  摘要：

  Piperazinebenzylamines bearing a small N-(1-methoxy-2-propyl) side chain were found to be potent and selective antagonists of the human melanocortin-4 (MC4) receptor. Compound 7b, having K-i values of 6.9 and 2800 nM at the human MC4 and MC3 receptors, respectively, has moderate oral bioavailability in mice, which is improved relative to the arylethyl analogues. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.06.058