methyl 7-fluoro-8-oxo-5,6,7,8-tetrahydronaphthalene-2-carboxylate | 1116093-71-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: methyl 7-fluoro-8-oxo-5,6,7,8-tetrahydronaphthalene-2-carboxylate
• 英文别名: methyl 7-fluoro-8-oxo-6,7-dihydro-5H-naphthalene-2-carboxylate
• CAS: 1116093-71-0
• 化学式: C₁₂H₁₁FO₃
• 分子量: 222.216
• InChiKey: FDPJNRUAKLWAQG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  43.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  methyl 7-fluoro-8-oxo-5,6,7,8-tetrahydronaphthalene-2-carboxylate 在 pyridinium hydrobromide perbromide 、 lithium bromide 、 copper(ll) bromide 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 155.0h， 生成 methyl 5-bromo-7-fluoro-8-hydroxy-2-naphthalene carboxylate
  参考文献：
  名称：

  EP2394988

  摘要：

  公开号：
• 作为产物：
  描述：

  8-氧代-5,6,7,8-四氢萘-2-羧酸甲酯 在 1-fluoro-4-hydroxy-1,4-diazoniabicyclo[2,2,2]octane-1,4-bis(tetrafluoroborate) 作用下， 以 甲醇 为溶剂， 反应 3.0h， 生成 methyl 7-fluoro-8-oxo-5,6,7,8-tetrahydronaphthalene-2-carboxylate
  参考文献：
  名称：

  EP2394988

  摘要：

  公开号：

文献信息

• SUBSTITUTED ACYLGUANIDINE DERIVATIVES (AS AMENDED)
  申请人：Kinoyama Isao

  公开号：US20120041036A1

  公开（公告）日：2012-02-16

  An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT 5A receptor modulating action. It was discovered that acylguanidine derivatives, 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 the 5-HT 5A receptor modulating action and excellent pharmacological actions 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血清素5-HT5A受体调节作用的用于治疗或预防痴呆症、精神分裂症的优良药剂。发现酰基胍衍生物，其中胍基通过一个羰基与萘的一个环相结合，另一个环上结合有一个环状基团，表现出强效的5-HT5A受体调节作用和基于该作用的优良药理作用。本发明可用作治疗或预防痴呆症、精神分裂症、躁郁症或注意力缺陷多动障碍的优良药剂。
• BICYCLIC ACYLGUANIDINE DERIVATIVE
  申请人：Kinoyama Isao

  公开号：US20110207729A1

  公开（公告）日：2011-08-25

  An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia, and the like, based on the serotonin 5-HT 5A receptor modulating action. It was confirmed that a bicyclic acylguanidine derivative which has a characteristic structure that guanidine is bonded to one ring of a bicyclic structure such as chromene and dihydronaphthalene through a carbonyl group and a cyclic group is bonded on the other ring, has a potent 5-HT 5A receptor modulating action and an excellent pharmacological action based on this mechanism. 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血清素5-HT5A受体调节作用的新型优良药剂，用于治疗或预防痴呆症、精神分裂症等疾病。经确认，一种具有特征结构的双环酰基胍衍生物，其中胍基通过羰基和环状基团与类似香豆素和二氢萘的双环结构的一个环相结合，另一个环上结合有一个环状基团，具有强效的5-HT5A受体调节作用和基于该机制的优良药理作用。本发明可用作治疗或预防痴呆症、精神分裂症、双相情感障碍或注意力缺陷多动障碍的优良药剂。
• 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。
• 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。
• SUBSTITUTED ACYLGUANIDINE DERIVATIVE
  申请人：Astellas Pharma Inc.

  公开号：EP2394988A1

  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 serotonin 5-HT5A receptor modulating action. It was discovered that acylguanidine derivatives, 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 the 5-HT5A receptor modulating action and excellent pharmacological actions 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。 研究发现，酰基胍衍生物（其中胍通过羰基键合在萘的一个环上，环基键合在其另一个环上）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。