2-chloro-N-(2-hydroxy-4-trifluoromethoxy-benzyl)-acetamide | 562080-94-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-chloro-N-(2-hydroxy-4-trifluoromethoxy-benzyl)-acetamide
• 英文别名: 2-Chloro-N-(2-hydroxy-4-(trifluoromethoxy)benzyl)acetamide；2-chloro-N-[[2-hydroxy-4-(trifluoromethoxy)phenyl]methyl]acetamide
• CAS: 562080-94-8
• 化学式: C₁₀H₉ClF₃NO₃
• 分子量: 283.635
• InChiKey: VJRZBEXEJLOKMF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  58.6
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-chloro-N-(2-hydroxy-4-trifluoromethoxy-benzyl)-acetamide 在 乙酸乙酯 作用下， 以 乙醇 、 盐酸 为溶剂， 反应 22.0h， 生成 2-Aminomethyl-5-trifluoromethoxy-phenol
  参考文献：
  名称：

  Phosphate transport inhibitors

  摘要：

  本发明涉及已被鉴定为磷酸盐转运抑制剂的化合物。其中许多化合物由结构式（I）表示：Ar1—W—X—Y—Ar2；或其药学上可接受的盐。其中，Ar1和Ar2独立地表示取代或未取代的芳基或可选取代的融合到可选取代的单环芳基上的五元或六元非芳杂环基。W和Y独立地表示共价键或C1-C3取代或未取代的烷基。X表示含杂原子的功能基团、芳基杂环基团、取代的芳基杂环基团、非芳杂环基团、取代的非芳杂环基团、烯基或取代的烯基。本发明还涉及用于治疗与高磷血症相关的疾病以及由磷酸盐转运功能介导的疾病的方法。该方法包括给予上述化合物之一的有效量。

  公开号：

  US07119120B2
• 作为产物：
  描述：

  氯乙酰胺-N-甲醇 、 3-三氟甲氧基苯酚 以 concentrated sulfuric acid 、 溶剂黄146 为溶剂， 以33.8%的产率得到2-chloro-N-(2-hydroxy-4-trifluoromethoxy-benzyl)-acetamide
  参考文献：
  名称：

  Phosphate transport inhibitors

  摘要：

  本文披露了被识别为磷酸盐转运抑制剂的化合物。许多化合物由结构式(I)表示：Ar1—W—X—Y—Ar2；或其药用可接受的盐。Ar1和Ar2独立地是取代或未取代的芳基或可取代的五元或六元非芳香杂环基与可取代的单环芳基融合。W和Y独立地是共价键或C1-C3取代或未取代的烷基基团。X是含杂原子的官能团、芳香杂环基、取代芳香杂环基、非芳香杂环基、取代非芳香杂环基、烯烃基或取代烯烃基。还披露了治疗与高磷血症相关疾病以及磷酸盐转运功能介导的疾病的方法。该方法包括给予上述化合物之一的有效量。

  公开号：

  US20040019113A1

文献信息

• PHOSPHATE TRANSPORT INHIBITORS
  申请人：GENZYME CORPORATION

  公开号：EP1465638A2

  公开（公告）日：2004-10-13
• US7119120B2
  申请人：——

  公开号：US7119120B2

  公开（公告）日：2006-10-10
• [EN] PHOSPHATE TRANSPORT INHIBITORS<br/>[FR] INHIBITEURS DE TRANSPORT DU PHOSPHATE
  申请人：GENZYME CORP

  公开号：WO2003057225A2

  公开（公告）日：2003-07-17

  Disclosed are compounds, which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar1-W-X-Y-Ar2; or a pharmaceutically acceptable salt thereof. Ar1 and Ar2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C 1-C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function. The methods comprise the step of administering an effective amount of the one of the compounds described above.
• Phosphate transport inhibitors
  申请人：GelTex Pharmaceuticals, Inc.

  公开号：US20040019113A1

  公开（公告）日：2004-01-29

  Disclosed are compounds which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar 1 —W—X—Y—Ar 2 ; or a pharmaceutically acceptable salt thereof. Ar 1 and Ar 2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C1-C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function. The methods comprise the step of administering an effective amount of the one of the compounds described above.

  本文披露了被识别为磷酸盐转运抑制剂的化合物。许多化合物由结构式(I)表示：Ar1—W—X—Y—Ar2；或其药用可接受的盐。Ar1和Ar2独立地是取代或未取代的芳基或可取代的五元或六元非芳香杂环基与可取代的单环芳基融合。W和Y独立地是共价键或C1-C3取代或未取代的烷基基团。X是含杂原子的官能团、芳香杂环基、取代芳香杂环基、非芳香杂环基、取代非芳香杂环基、烯烃基或取代烯烃基。还披露了治疗与高磷血症相关疾病以及磷酸盐转运功能介导的疾病的方法。该方法包括给予上述化合物之一的有效量。