(RS)-2-三氟乙酰氨基-1-(4-甲氧基苯基)-1-丙酮 | 742095-36-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: (RS)-2-三氟乙酰氨基-1-(4-甲氧基苯基)-1-丙酮
• 英文名称: (RS)-2-trifluoroacetamido-1-(4-methoxyphenyl)-1-propanone
• 英文别名: 2,2,2-trifluoro-N-[1-(4-methoxyphenyl)-1-oxopropan-2-yl]acetamide
• CAS: 742095-36-9
• 化学式: C₁₂H₁₂F₃NO₃
• 分子量: 275.227
• InChiKey: RTKXLACASKOKSX-UHFFFAOYSA-N

物化性质

• 熔点：
  93-95 °C
• 沸点：
  399.8±42.0 °C(Predicted)
• 密度：
  1.267±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  55.4
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (RS)-2-三氟乙酰氨基-1-(4-甲氧基苯基)-1-丙酮 在 盐酸 作用下， 以 乙醇 为溶剂， 生成 4'-methoxy-2-aminopropiophenone hydrochloride
  参考文献：
  名称：

  5-Aryl-imidazolin-2-ones as a scaffold for potent antioxidant and memory-improving activity

  摘要：

  A series of 5-phenyl-substituted-N-alkyl-imidazolin-2-ones with potent radical-scavenging activity and lipid peroxidation inhibitory activity was synthesized. Many of the compounds showed memory-improving effect in animal models independent of the inhibitory activity on lipid peroxidation. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.12.064
• 作为产物：
  描述：

  2,2,2-三氟乙酰胺 、 2-溴-1-(4-甲氧苯基)丙酮 在 potassium carbonate 作用下， 以 丙酮 为溶剂， 生成 (RS)-2-三氟乙酰氨基-1-(4-甲氧基苯基)-1-丙酮
  参考文献：
  名称：

  5-Aryl-imidazolin-2-ones as a scaffold for potent antioxidant and memory-improving activity

  摘要：

  A series of 5-phenyl-substituted-N-alkyl-imidazolin-2-ones with potent radical-scavenging activity and lipid peroxidation inhibitory activity was synthesized. Many of the compounds showed memory-improving effect in animal models independent of the inhibitory activity on lipid peroxidation. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.12.064

文献信息

• [EN] SYNTHESIS OF OPTICALLY PURE (R)-5-(2-AMINOPROPYL)-2-METHOXYBENZENESULPHONAMIDE<br/>[FR] SYNTHESE DE (R)-5-(2-AMINOPROPYL)-2-METHOXYBENZENOSULFONAMIDE OPTIQUEMENT PUR
  申请人：LEK PHARMACEUTICALS

  公开号：WO2005063701A1

  公开（公告）日：2005-07-14

  The present invention relates to a new process for the preparation of optically pure (R)-5-(2-aminopropyl)-2-methoxybenzenesulphonamide, which is an intermediate in the synthesis of tamsulosin.

  本发明涉及一种制备光学纯(R)-5-(2-氨丙基)-2-甲氧基苯磺胺的新工艺，该化合物是特拉唑嗪合成中的中间体。
• Synthesis of optically pure(r)-5-(2-amynopropyl)-2-methoxybenzenesulphonamide
  申请人：Mohar Barbara

  公开号：US20070155989A1

  公开（公告）日：2007-07-05

  The present invention relates to a new process for the preparation of optically pure (R)-5-(2-aminopropyl)-2-methoxybenzenesulphonamide, which is an intermediate in the synthesis of tamsulosin.

  本发明涉及一种新的制备光学纯(R)-5-(2-氨基丙基)-2-甲氧基苯磺酰胺的方法，该化合物是替唑嗪合成过程中的中间体。
• MAO inhibition by arylisopropylamines: the effect of oxygen substituents at the β-position
  作者：Mauricio Osorio-Olivares、Marcos Caroli Rezende、Silvia Sepúlveda-Boza、Bruce K Cassels、Angélica Fierro

  DOI：10.1016/j.bmc.2004.05.033

  日期：2004.8.1

  Twenty-nine arylisopropylamines, substituted at the beta-position of their side chain by an oxo, hydroxy, or methoxy group, were evaluated in vitro as MAO-A and MAO-B inhibitors. The oxo derivatives ('cathinones') were in general less active as MAO-A inhibitors than the corresponding arylisopropylamines, but exhibited an interesting MAO-13 inhibiting activity, which was absent in the hydroxy, methoxy, and beta-unsubstituted analogues. These results suggest that selective affinity for the two MAO isoforms in this family of compounds is modulated not only by the aryl substitution pattern but also by the side-chain substituents on the aryl-alkylamine scaffold. (C) 2004 Elsevier Ltd. All rights reserved.
• SYNTHESIS OF OPTICALLY PURE (R)-5-(2-AMINOPROPYL)-2-METHOXYBENZENESULPHONAMIDE
  申请人：LEK Pharmaceuticals d.d.

  公开号：EP1704140A1

  公开（公告）日：2006-09-27
• US7538246B2
  申请人：——

  公开号：US7538246B2

  公开（公告）日：2009-05-26