7-Trifluoroacetamido-2,3,5,6,7,8-hexahydronaphtho[2,3-b]furan-8-one | 119004-43-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 萘并呋喃类
• 英文名称: 7-Trifluoroacetamido-2,3,5,6,7,8-hexahydronaphtho[2,3-b]furan-8-one
• 英文别名: 2,2,2-trifluoro-N-(8-oxo-3,5,6,7-tetrahydro-2H-benzo[f][1]benzofuran-7-yl)acetamide
• CAS: 119004-43-2
• 化学式: C₁₄H₁₂F₃NO₃
• 分子量: 299.249
• InChiKey: XPXNHUSSZTXAIY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  21
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 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：

  7-Trifluoroacetamido-2,3,5,6,7,8-hexahydronaphtho[2,3-b]furan-8-one 以55%的产率得到
  参考文献：
  名称：

  PEGLION, J. -L.;POIGNANT, J. -C.;VIAN, J.

  摘要：

  DOI：
• 作为产物：
  描述：

  2,3-二氢苯并呋喃 在 三乙基硅烷 、 三氯化铝 、 三氟乙酸 、 三氟乙酸酐 作用下， 以 二氯甲烷 、 三氟乙酸 为溶剂， 生成 7-Trifluoroacetamido-2,3,5,6,7,8-hexahydronaphtho[2,3-b]furan-8-one
  参考文献：
  名称：

  Tetracyclic analogues of [+]-S 14297: Synthesis and determination of affinity and selectivity at cloned human dopamine D3 vs D2 receptors

  摘要：

  Starting from the structure of the preferential D-3 antagonist S 14297 (1), we have prepared a series of cis and trans tetracyclic derivatives of general formula I in order to improve potency and selectivity for D-3 receptors. The trans oxazino derivative 2c, showed slightly increased affinity at D-3 receptors and double the selectivity for D-3 over D-2 receptors, in comparison to S 14297. Cis derivatives and compounds where R-1 is aralkyl were totally devoid of activity. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)00126-1

文献信息

• Pharmaceutically useful tricyclic amines derived from
  申请人：Adir et Cie

  公开号：US04851429A1

  公开（公告）日：1989-07-25

  Compound of general formula I ##STR1## in which R.sub.1 and R.sub.2, which may be identical or different, each denote a hydrogen atom, a benzyl radical, a cyclohexylmethyl radical or a linear or branched alkyl radical containing from 1 to 10 carbon atoms, optionally substituted with a hydroxy radical, with a carboxy radical or with an alkoxy radical having 1 to 5 carbon atoms, with an alkoxycarbonyl radical having 2 to 6 carbon atoms, with an alkylphenyl radical having 7 to 16 carbon atoms or with a 2-alkylthienyl radical having 5 to 14 carbon atoms, R.sub.3 denotes a hydrogen atom or a linear or branched alkyl radical containing from 1 to 4 carbon atoms, A denotes a single bond or a methylene radical, or a radical of formula ##STR2## in which R.sub.4 is a linear or branched alkyl radical containing from 1 to 4 carbon atoms. These products are useful in anti-depressant, anti-aggressive, or dopaminergic modulation therapy and the corresponding bicyclic compounds are useful as intermediates for ring closure and production of the tricyclic compounds having the foregoing formula.

  通式I的一般化合物##STR1##中，其中R.sub.1和R.sub.2，可以相同也可以不同，每个代表一个氢原子、苯甲基、环己甲基或含有1至10个碳原子的线性或支链烷基基团，可选地取代为一个羟基基团、一个羧基基团或一个含有1至5个碳原子的烷氧基基团、一个含有2至6个碳原子的烷氧羰基基团、一个含有7至16个碳原子的烷基苯基基团或一个含有5至14个碳原子的2-烷基噻吩基团，R.sub.3代表一个氢原子或含有1至4个碳原子的线性或支链烷基基团，A代表一个单键或一个亚甲基基团，或一个式子##STR2##中R.sub.4为含有1至4个碳原子的线性或支链烷基基团。这些产品在抗抑郁、抗攻击性或多巴胺调节疗法中有用，相应的双环化合物在环闭合和产生具有上述式子的三环化合物的中间体中有用。
• PEGLION, J. -L.;POIGNANT, J. -C.;VIAN, J.
  作者：PEGLION, J. -L.、POIGNANT, J. -C.、VIAN, J.

  DOI：——

  日期：——
• US4851429A
  申请人：——

  公开号：US4851429A

  公开（公告）日：1989-07-25
• US4874878A
  申请人：——

  公开号：US4874878A

  公开（公告）日：1989-10-17
• Tetracyclic analogues of [+]-S 14297: Synthesis and determination of affinity and selectivity at cloned human dopamine D3 vs D2 receptors
  作者：Jean-Louis Peglion、Joël Vian、Bertrand Goument、Nicole Despaux、Valérie Audinot、Mark J. Millan

  DOI：10.1016/s0960-894x(97)00126-1

  日期：1997.1

  Starting from the structure of the preferential D-3 antagonist S 14297 (1), we have prepared a series of cis and trans tetracyclic derivatives of general formula I in order to improve potency and selectivity for D-3 receptors. The trans oxazino derivative 2c, showed slightly increased affinity at D-3 receptors and double the selectivity for D-3 over D-2 receptors, in comparison to S 14297. Cis derivatives and compounds where R-1 is aralkyl were totally devoid of activity. (C) 1997 Elsevier Science Ltd.