1-(1,2,3,4-Tetrahydronaphthalen-1-yl)piperidin-4-one | 314081-20-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 1-(1,2,3,4-Tetrahydronaphthalen-1-yl)piperidin-4-one
• CAS: 314081-20-4
• 化学式: C₁₅H₁₉NO
• 分子量: 229.322
• InChiKey: KJLOTOQIHFQKIA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(1,2,3,4-Tetrahydronaphthalen-1-yl)piperidin-4-one 在 三乙酰氧基硼氢化钠 、 对甲苯磺酸 、 溶剂黄146 作用下， 以 1,2-二氯乙烷 、 甲苯 为溶剂， 反应 1.0h， 生成 1-(1-(1,2,3,4-tetrahydronaphthalen-1-yl)piperidin-4-yl)indolin-2-one
  参考文献：
  名称：

  A Novel Series of Piperidin-4-yl-1,3-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor

  摘要：

  A series of N-(4-piperidinyl)-2-indolinones were discovered as a new structural class of nociceptin receptor (NOP) ligands. Unlike other previously reported classes of NOP receptor ligands, modifications of the piperidine N substituents afforded both potent agonists and antagonists, with modest selectivities over other opioid receptors. The SAR revealed in this new series will provide important insights for the development of pharmacophores for agonist and antagonist actions at the NOP receptor.

  DOI：

  10.1021/jm034249d
• 作为产物：
  描述：

  N-乙基-4-哌啶酮 在 potassium carbonate 作用下， 以 乙醇 、 丙酮 为溶剂， 反应 19.0h， 生成 1-(1,2,3,4-Tetrahydronaphthalen-1-yl)piperidin-4-one
  参考文献：
  名称：

  A Novel Series of Piperidin-4-yl-1,3-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor

  摘要：

  A series of N-(4-piperidinyl)-2-indolinones were discovered as a new structural class of nociceptin receptor (NOP) ligands. Unlike other previously reported classes of NOP receptor ligands, modifications of the piperidine N substituents afforded both potent agonists and antagonists, with modest selectivities over other opioid receptors. The SAR revealed in this new series will provide important insights for the development of pharmacophores for agonist and antagonist actions at the NOP receptor.

  DOI：

  10.1021/jm034249d

文献信息

• Spiro(piperidine-4,1'-pyrrolo(3,4-c)pyrrole)
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP0963987A2

  公开（公告）日：1999-12-15

  The present invention relates to compounds of the general formula    wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na+ excretion, arterial blood pressure disorders and metabolic disorders such as obesity.

  本发明涉及通式为 其中的取代基见本申请所述，以及其药学上可接受的酸加成盐。 本发明的化合物可用于治疗与孤儿素 FQ（OFQ）受体有关的疾病，这些疾病包括精神、神经和生理疾病，如焦虑和应激障碍、抑郁症、创伤、阿尔茨海默病或其他痴呆症导致的记忆丧失、认知和精益功能障碍、癫痫和抽搐、急性和/或慢性疼痛病症、成瘾性药物戒断症状、水平衡控制、Na+排泄、动脉血压紊乱和代谢紊乱，如肥胖。
• BENZIMIDAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP2128154B1

  公开（公告）日：2015-04-08
• 4-AMINOPIPERIDINE DERIVATIVES OF TETRAHYDRONAPHTHALENE, CHROMANS AND THIOCHROMANS
  申请人：AstraZeneca UK Limited

  公开号：EP1204641A1

  公开（公告）日：2002-05-15
• US6075034A
  申请人：——

  公开号：US6075034A

  公开（公告）日：2000-06-13
• US8877779B2
  申请人：——

  公开号：US8877779B2

  公开（公告）日：2014-11-04