1-(2-nitro-4-trifluoromethyl-phenyl)-2,3-dihydro-indole | 71971-46-5

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1-(2-nitro-4-trifluoromethyl-phenyl)-2,3-dihydro-indole
• 英文别名: 1-(2-nitro-4-(trifluoromethyl)phenyl)indoline；1-(2-nitro-4-trifluoromethylphenyl)indoline；1-(2-Nitro-4-trifluormethylphenyl)-indolin；[2-Nitro-4-(trifluoromethyl)phenyl]indoline；1-[2-nitro-4-(trifluoromethyl)phenyl]-2,3-dihydroindole
• CAS: 71971-46-5
• 化学式: C₁₅H₁₁F₃N₂O₂
• mdl: MFCD01442183
• 分子量: 308.26
• InChiKey: HTYOJGBBZYEJPX-UHFFFAOYSA-N

物化性质

• 熔点：
  90-92 °C(Solv: hexane (110-54-3))
• 沸点：
  401.2±45.0 °C(Predicted)
• 密度：
  1.406±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  49.1
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  1-(2-nitro-4-trifluoromethyl-phenyl)-2,3-dihydro-indole 在 盐酸 、 tin(ll) chloride 、 水 、 碳酸氢钠 作用下， 以 甲醇 为溶剂， 反应 8.0h， 以93.9%的产率得到1-[2-amino-4-(trifluoromethyl)phenyl]indoline
  参考文献：
  名称：

  METHOD OF REGULATING PHOSPHORYLATION OF SR PROTEIN AND ANTIVIRAL AGENTS COMPRISING SR PROTEIN ACTIVITY REGULATOR AS THE ACTIVE INGREDIENT

  摘要：

  公开号：

  EP1712242B1
• 作为产物：
  描述：

  吲哚啉 、 4-氟-3-硝基三氟甲苯 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 6.5h， 以99.4%的产率得到1-(2-nitro-4-trifluoromethyl-phenyl)-2,3-dihydro-indole
  参考文献：
  名称：

  METHOD OF REGULATING PHOSPHORYLATION OF SR PROTEIN AND ANTIVIRAL AGENTS COMPRISING SR PROTEIN ACTIVITY REGULATOR AS THE ACTIVE INGREDIENT

  摘要：

  公开号：

  EP1712242B1

文献信息

• Indolo-,1,2-dihydroindolo-, and 1,2,6,7-tetrahydroindolo [1,7-ab][1,5]
  申请人：American Hoechst Corporation

  公开号：US04186199A1

  公开（公告）日：1980-01-29

  What is disclosed are ##STR1## wherein X is hydrogen, halogen or trifluoromethyl; Y is hydrogen, halogen or trifluoromethyl; R is hydrogen, loweralkyl, cycloalkyl, phenyl, halophenyl, furyl, pyridinyl, 4-methylpiperazin-1-ylethyl or phenylloweralkyl; R.sup.1 is hydrogen; n and m are independently 0 or 1, but n is not 0 when m is 1, and the bonds between ring positions 1 and 2 and between positions 6 and 7 are respectively saturated when n and m are 1 and are unsaturated when n and m are 0; pharmaceutically acceptable acid addition salts thereof; methods of preparing said compounds; pharmaceutical compositions including said compounds; methods of treatment using the compounds; and intermediates therefor. These compounds are useful as analgesic and anti-inflammatory agents, as well as intermediates for the preparation of other pharmaceutically active compounds.

  所披露的是##STR1##，其中X为氢、卤素或三氟甲基；Y为氢、卤素或三氟甲基；R为氢、较低烷基、环烷基、苯基、卤苯基、呋喃基、吡啶基、4-甲基哌嗪-1-乙基或苯基较低烷基；R.sup.1为氢；n和m独立地为0或1，但当m为1时，n不为0，并且当n和m为1时，环位置1和2之间的键和位置6和7之间的键分别饱和，当n和m为0时，键是不饱和的；其药学上可接受的酸盐；制备所述化合物的方法；包括所述化合物的药物组合物；使用这些化合物的治疗方法；以及其中间体。这些化合物可用作镇痛和抗炎药物，以及其他药用活性化合物的制备中间体。
• Method for controlling sr protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control sr protein activity
  申请人：Hagiwara Masatoshi

  公开号：US20070135367A1

  公开（公告）日：2007-06-14

  The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.

  本发明提供了：（1）通过减少或抑制SR蛋白活性作用的抗病毒剂，更具体地，（i）通过增强SR蛋白的去磷酸化作用的抗病毒剂，和（ii）通过抑制磷酸化SR蛋白的蛋白质的抗病毒剂；（2）通过抑制SR蛋白表达的抗病毒剂，和（3）通过激活拮抗SR蛋白的蛋白质的抗病毒剂。本发明还提供了抑制磷酸化SR蛋白的SRPKs的化合物。这些化合物抑制SR蛋白的活性并具有抗病毒活性。各种新病毒，包括SARS，已经出现，因此本发明提供了适用于新病毒的持久的广谱抗病毒剂。
• METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY
  申请人：Hagiwara Masatoshi

  公开号：US20100016359A1

  公开（公告）日：2010-01-21

  The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.

  本发明提供：（1）抗病毒剂，通过减少或抑制SR蛋白的活性发挥作用，更具体地，（i）通过增强SR蛋白的去磷酸化作用发挥作用的抗病毒剂，以及（ii）通过抑制磷酸化SR蛋白的蛋白质发挥作用的抗病毒剂；（2）通过抑制SR蛋白的表达发挥作用的抗病毒剂，以及（3）通过激活对抗SR蛋白的蛋白质发挥作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPKs的化合物。这些化合物抑制SR蛋白的活性，并具有抗病毒活性。各种新的病毒，包括SARS，已经出现，因此本发明提供适用于新病毒的持久广谱抗病毒剂。
• Method for controlling SR protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control SR protein activity
  申请人：——

  公开号：US07569536B2

  公开（公告）日：2009-08-04

  The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.

  本发明提供以下内容：（1）抗病毒剂，通过减少或抑制SR蛋白的活性来发挥作用，更具体地，（i）通过增强SR蛋白的去磷酸化作用来发挥作用的抗病毒剂，以及（ii）通过抑制SR蛋白磷酸化的蛋白质来发挥作用的抗病毒剂；（2）通过抑制SR蛋白的表达来发挥作用的抗病毒剂，以及（3）通过激活对抗SR蛋白的蛋白质来发挥作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPKs的化合物。这些化合物抑制SR蛋白的活性，并具有抗病毒活性。各种新的病毒，包括SARS，已经出现，因此本发明提供了适用于新病毒的持久的广谱抗病毒剂。
• Methods for controlling SR protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control SR protein activity
  申请人：Masatoshi Hagiwara

  公开号：US08338362B2

  公开（公告）日：2012-12-25

  The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.

  本发明提供了以下内容：（1）抗病毒剂，通过降低或抑制SR蛋白活性来发挥作用，更具体地说，（i）通过增强SR蛋白去磷酸化的抗病毒剂，和（ii）通过抑制SR蛋白磷酸化的蛋白质的抗病毒剂；（2）通过抑制SR蛋白表达的抗病毒剂，和（3）通过激活对抗SR蛋白的蛋白质的抗病毒剂。本发明还提供了抑制SR蛋白激酶（SRPKs）的化合物，这些化合物抑制SR蛋白的活性，并具有抗病毒活性。各种新的病毒，包括SARS，已经出现，因此本发明提供了适用于新病毒的长效广谱抗病毒剂。