5-fluoro-8-methoxy-1-tetralone | 881190-26-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 5-fluoro-8-methoxy-1-tetralone
• 英文别名: 5-fluoro-8-methoxy-3,4-dihydro-2H-naphthalen-1-one
• CAS: 881190-26-7
• 化学式: C₁₁H₁₁FO₂
• mdl: MFCD18648029
• 分子量: 194.206
• InChiKey: FMLPACUQSAKYAG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.363
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-fluoro-8-methoxy-1-tetralone 、 碳酸二甲酯 在 sodium hydride 作用下， 以 四氢呋喃 、 mineral oil 为溶剂， 反应 3.0h， 生成 methyl 5-fluoro-8-methoxy-1-oxo-1,2,3,4-tetrahydronaphthalene-2-carboxylate
  参考文献：
  名称：

  EP2394987

  摘要：

  公开号：

文献信息

• Cyclic amine derivative or salt thereof
  申请人：Hayashibe Satoshi

  公开号：US20070197594A1

  公开（公告）日：2007-08-23

  Provided are compounds which are an NMDA antagonist having a broad safety margin and are useful as a treating agent or a preventing agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, pain, etc. Concretely provided are an amine derivative or its salt characterized in that the amine-containing structure A therein bonds to a 2- or 3-cyclic condensed ring (e.g., indane, tetralone, 4,5,6,7-tetrahydrobenzothiophene, 4,5,6,7-tetrahydrobenzofuran, 7,8-dihydro-6H-indeno[4,5-b]furan, 2,3-dihydro- 1 H-cyclopenta[1]naphthalene) via X 1 (bond or lower alkylene); and an NMDA antagonist containing it as an active ingredient thereof.

  提供的化合物是NMDA受体拮抗剂，具有广泛的安全边界，并可用作治疗或预防阿尔茨海默病、脑血管性痴呆、帕金森病、缺血性卒中、疼痛等药物。具体提供的是胺衍生物或其盐，其特点在于其中含有胺基结构A，通过X1（键或低碳烷基）与2-或3-环状紧缩环（例如茚烷、四氢萘酮、4,5,6,7-四氢苯并噻吩、4,5,6,7-四氢苯并呋喃、7,8-二氢-6H-茚并[4,5-b]呋喃、2,3-二氢-1H-环戊[1]萘烷）结合；以及含有它作为有效成分的NMDA受体拮抗剂。
• ACYLGUANIDINE DERIVATIVES
  申请人：Kinoyama Isao

  公开号：US20110306621A1

  公开（公告）日：2011-12-15

  An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT 5A receptor modulating action. It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT 5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.

  本发明的目的是提供一种基于5-羟色胺5-HT5A受体调节作用的治疗或预防痴呆症、精神分裂症的优良药剂。经确认，酰基胍衍生物具有特征结构，其中胍基通过羰基和环状基团与萘的一个环结合，另一个环上结合环状基团，表现出强效的5-HT5A受体调节作用和优良的药理作用。本发明可用作治疗或预防痴呆症、精神分裂症、双相障碍或注意力缺陷多动障碍的优良药剂。
• CYCLIC AMINE DERIVATIVE OR SALT THEREOF
  申请人：Astellas Pharma Inc.

  公开号：EP1795524A1

  公开（公告）日：2007-06-13

  Provided are compounds which are an NMDA antagonist having a broad safety margin and are useful as a treating agent or a preventing agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, pain, etc. Concretely provided are an amine derivative or its salt characterized in that the amine-containing structure A therein bonds to a 2- or 3-cyclic condensed ring (e.g., indane, tetralone, 4,5,6,7-tetrahydrobenzothiophene, 4,5,6,7-tetrahydrobenzofuran, 7,8-dihydro-6H-indeno[4,5-b]furan, 2,3-dihydro-1H-cyclopenta[1]naphthalene) via X1 (bond or lower alkylene); and an NMDA antagonist containing it as an active ingredient thereof.

  本发明提供的化合物是一种具有广泛安全范围的 NMDA 拮抗剂，可作为阿尔茨海默病、脑血管痴呆症、帕金森病、缺血性脑中风、疼痛等的治疗剂或预防剂。具体而言，提供了一种胺衍生物或其盐，其特征在于其中的含胺结构 A 与 2-或 3-环缩合环（如茚满、四烯酮、4-环缩合环、5-环缩合环、6-环缩合环、7-环缩合环、8-环缩合环、9-环缩合环）结合、茚、四酮、4,5,6,7-四氢苯并噻吩、4,5,6,7-四氢苯并呋喃、7,8-二氢-6H-茚并[4,5-b]呋喃、2,3-二氢-1H-环戊并[1]萘）通过 X1（键或低级亚烷基）结合；以及含有它作为其活性成分的 NMDA 拮抗剂。
• ACYLGUANIDINE DERIVATIVE
  申请人：Astellas Pharma Inc.

  公开号：EP2394987A1

  公开（公告）日：2011-12-14

  An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT5A receptor modulating action. It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.

  本发明的目的是提供一种基于5-羟色胺5-HT5A受体调节作用的治疗或预防痴呆症、精神分裂症的优良药物。 经证实，酰基胍衍生物具有胍基通过羰基与萘的一个环键合、环基与萘的另一个环键合的特征结构，具有强效的 5-HT5A 受体调节作用和基于该作用的优异药理作用。本发明可作为治疗或预防痴呆症、精神分裂症、双相情感障碍或注意缺陷多动障碍的优良药物。