4-[2-(三氟甲氧基)苯氧基]哌啶 | 902836-49-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: 4-[2-(三氟甲氧基)苯氧基]哌啶
• 英文名称: 4-[2-trifluoromethoxyphenoxy]piperidine
• 英文别名: 4-(2-(Trifluoromethoxy)phenoxy)piperidine；4-[2-(trifluoromethoxy)phenoxy]piperidine
• CAS: 902836-49-1
• 化学式: C₁₂H₁₄F₃NO₂
• mdl: MFCD08061004
• 分子量: 261.244
• InChiKey: UXSFSVYZILNPEV-UHFFFAOYSA-N

物化性质

• 沸点：
  275℃
• 密度：
  1.230
• 闪点：
  120℃

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  30.5
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-[2-(三氟甲氧基)苯氧基]哌啶 在 palladium diacetate 、 4-甲基苯磺酸吡啶 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 乙醇 、 caesium carbonate 作用下， 以 甲苯 为溶剂， 反应 24.5h， 生成 4-[4-[3-(三氟甲氧基)苯氧基]哌啶-1-基]苯酚
  参考文献：
  名称：

  Synthesis and Antituberculosis Activity of a Novel Series of Optically Active 6-Nitro-2,3-dihydroimidazo[2,1-b]oxazoles

  摘要：

  In an effort to develop potent new antituberculosis agents that would be effective against both drug-susceptible and drug-resistant strains of Mycobacterium tuberculosis, we prepared a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles substituted at the 2-position with various phenoxymethyl groups and a methyl group and investigated the in vitro and in vivo activity of these compounds. Several of these derivatives showed potent in vitro and in vivo activity, and compound 19 (OPC-67683) in particular displayed excellent in vitro activity against both drug-susceptible and drug-resistant strains of M. tuberculosis H(37)Rv (MIC = 0.006 mu g/mL) and dose-dependent and significant in vivo efficacy at lower oral doses than rifampicin in mouse models infected with M. tuberculosis Kurono. The synthesis and structure-activity relationships of these new compounds are presented.

  DOI：

  10.1021/jm060957y

文献信息

• [EN] ARYL CARBOXAMIDE DERIVATIVES AS SODIUM CHANNEL INHIBITORS FOR TREATMENT OF PAIN<br/>[FR] DÉRIVÉS D'ARYLCARBOXAMIDE EN TANT QU'INHIBITEURS DE CANAL SODIQUE POUR LE TRAITEMENT DE LA DOULEUR
  申请人：AMGEN INC

  公开号：WO2011103196A1

  公开（公告）日：2011-08-25

  The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

  本发明提供了一种抑制电压门控钠通道（Nav）的化合物，特别是Nav 1.7，因此适用于治疗通过抑制这些通道可治疗的疾病，特别是慢性疼痛疾病。还提供了含有这种化合物的药物组合物以及制备这种化合物的方法。
• PREPARATION OF (N-HETEROCYCLYL) ARYL ETHERS
  申请人：Kreis Michael

  公开号：US20100152454A1

  公开（公告）日：2010-06-17

  The present invention relates to a process for the preparation of optionally substituted (N-heterocyclyl) aryl ethers.

  本发明涉及一种制备可选取代的（N-杂环基）芳基醚的方法。
• Novel Phenyl Imidazoles and Phenyl Triazoles As Gamma-Secretase Modulators
  申请人：Allen Martin Patrick

  公开号：US20120053165A1

  公开（公告）日：2012-03-01

  Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  本发明公开了具有式（I）所定义的结构的化合物及其药学上可接受的盐，同时公开了相应的制药组合物、治疗方法、合成方法和中间体。
• CARBOXAMIDES AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS
  申请人：Bregman Howard

  公开号：US20130131035A1

  公开（公告）日：2013-05-23

  The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

  本发明提供了一种抑制电压门控钠通道（Nav）的化合物，特别是Nav 1.7，因此可用于治疗可通过抑制这些通道治疗的疾病，特别是慢性疼痛疾病。还提供了含有这种化合物的药物组合物以及制备这种化合物的方法。
• Herstellung von (N-Heterozyklyl)-Arylethern
  申请人：Saltigo GmbH

  公开号：EP2179988A1

  公开（公告）日：2010-04-28

  Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung von gegebenenfalls substituierten (N-Heterozyklyl)-Arylethem.

  本发明涉及一种制备任选取代的（N-杂环基）芳基莱姆的工艺。