3-Furan-2-yl-4-morpholin-4-yl-benzaldehyde | 263349-25-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 3-Furan-2-yl-4-morpholin-4-yl-benzaldehyde
• 英文别名: 3-(2-Furanyl)4-(4-morpholinyl)benzaldehyde；3-(furan-2-yl)-4-morpholin-4-ylbenzaldehyde
• CAS: 263349-25-3
• 化学式: C₁₅H₁₅NO₃
• 分子量: 257.289
• InChiKey: OQKJVHMEILQLQJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  42.7
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-Furan-2-yl-4-morpholin-4-yl-benzaldehyde 在 Yb(CF₃CO₃)3 、 三乙酰氧基硼氢化钠 、 溶剂黄146 作用下， 以 1,2-二氯乙烷 、 乙腈 为溶剂， 反应 2.0h， 生成 3-[(3-phenoxyphenyl)[[3-(2-furanyl)-4-(4-morpholinyl)phenyl]methyl]amino]-1,1,1-trifluoro-2-propanol
  参考文献：
  名称：

  Novel heteroaryl replacements of aromatic 3-tetrafluoroethoxy substituents in trifluoro-3-(tertiaryamino)-2-propanols as potent inhibitors of cholesteryl ester transfer protein

  摘要：

  A series of novel N,N-desubstituted trifluoro-3-amino-2-propanols has been prepared as potent inhibitors of cholesteryl ester transfer protein (CETP). Modifying the aromatic 3-tetrafluoroethoxy group in the lead molecule la with various heteroaryl moieties produced new 2-furyl analogues 2a.b with submicromolar potency in vitro. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(01)00244-x
• 作为产物：
  描述：

  2-(三丁基锡烷基)呋喃 、 3-溴-4-(4-吗啉基)苯甲醛 在 bis-triphenylphosphine-palladium(II) chloride 作用下， 以 1,4-二氧六环 为溶剂， 反应 18.0h， 生成 3-Furan-2-yl-4-morpholin-4-yl-benzaldehyde
  参考文献：
  名称：

  Novel heteroaryl replacements of aromatic 3-tetrafluoroethoxy substituents in trifluoro-3-(tertiaryamino)-2-propanols as potent inhibitors of cholesteryl ester transfer protein

  摘要：

  A series of novel N,N-desubstituted trifluoro-3-amino-2-propanols has been prepared as potent inhibitors of cholesteryl ester transfer protein (CETP). Modifying the aromatic 3-tetrafluoroethoxy group in the lead molecule la with various heteroaryl moieties produced new 2-furyl analogues 2a.b with submicromolar potency in vitro. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(01)00244-x

文献信息

• Substituted N, N-disubstituted diamino compounds useful for inhibiting cholesteryl ester transfer protein activity
  申请人：——

  公开号：US20020120011A1

  公开（公告）日：2002-08-29

  The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted diamines. A preferred specific N,N-disubstituted diamine is the compound: 1

  这项发明涉及替代多环芳基和杂环芳基的三级杂烷基胺化合物，可用作胆固醇酯转移蛋白（CETP；血浆脂质转移蛋白-I）的抑制剂，以及用于治疗动脉粥样硬化和其他冠状动脉疾病的化合物、组合物和方法。首选的三级杂烷基胺化合物是取代的N,N-二取代二胺。首选的具体N,N-二取代二胺化合物是：1
• Substituted N, N-disubstituted cycloalkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
  申请人：——

  公开号：US20020165232A1

  公开（公告）日：2002-11-07

  The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.

  本发明涉及取代的多环芳基和杂环芳基三级-杂基烷胺化合物，用于作为胆固醇酯转移蛋白（CETP; 血浆脂质转移蛋白-I）的抑制剂，并涉及用于治疗动脉粥样硬化和其他冠状动脉疾病的化合物、组合物和方法。
• Substituted n-phenyl-n-fused-benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
  申请人：——

  公开号：US20020183397A1

  公开（公告）日：2002-12-05

  The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-fused-benzyl aminoalcohols. A preferred specific N-phenyl-N-fused-benzyl aminoalcohol is the compound: 1

  本发明涉及取代的多环芳基和杂环芳基三级-杂代烷基胺化合物，可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-I）抑制剂，以及用于治疗动脉粥样硬化和其他冠状动脉疾病的化合物、组合物和方法。优选的三级-杂代烷基胺化合物是取代的N-苯基-N-融合苄基氨基醇。一种优选的特定N-苯基-N-融合苄基氨基醇化合物是化合物：1。
• Substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity
  申请人：G.D. Searle & Co.

  公开号：US20030083331A1

  公开（公告）日：2003-05-01

  The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.

  本发明涉及取代的多环芳基和杂环芳基三级杂-脂肪基胺化合物，用作胆固醇酯转移蛋白（CETP; 血浆脂质转移蛋白-I）的抑制剂以及用于治疗动脉粥样硬化和其他冠状动脉疾病的化合物、组合物和方法。
• Use of substituted N, N-disubstituted reverse aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
  申请人：Pfizer, Inc.

  公开号：US06765023B2

  公开（公告）日：2004-07-20

  The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols. A preferred specific N,N-disubstituted reverse aminoalcohols is the compound:

  本发明涉及替代多环芳基和杂环芳基三级杂-杂烷基胺化合物，其作为胆固醇酯转移蛋白（CETP；血浆脂质转移蛋白-I）的抑制剂，以及用于治疗动脉粥样硬化和其他冠状动脉疾病的化合物、组合物和方法。首选的三级杂-杂烷基胺化合物是取代的N，N-二取代反式氨基醇。一种首选的特定N，N-二取代反式氨基醇是该化合物：