7-Methoxy-1-(piperazin-1-yl)-1,2,3,4-tetrahydronaphthalene | 128226-38-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 7-Methoxy-1-(piperazin-1-yl)-1,2,3,4-tetrahydronaphthalene
• 英文别名: 1-(7-methoxy-1,2,3,4-tetrahydro-1-naphthalenyl)piperazine；1-(7-methoxy-1,2,3,4-tetrahydro-1-naphthyl)piperazine；(7-methoxytetralin-1-yl)piperazine；1-(7-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)piperazine
• CAS: 128226-38-0
• 化学式: C₁₅H₂₂N₂O
• mdl: MFCD11901040
• 分子量: 246.352
• InChiKey: KXEROXFYRWYIGF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  24.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-溴-4'-氟苯乙酮 、 7-Methoxy-1-(piperazin-1-yl)-1,2,3,4-tetrahydronaphthalene 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 1-{4-[2-(4-fluorophenyl)-2-oxoethyl]piperazin-1-yl}-7-methoxy-1,2,3,4-tetrahydronaphthalene hydrochloride
  参考文献：
  名称：

  Indoles

  摘要：

  一种由以下公式表示的1,4-取代的环胺衍生物或其药理学上可接受的盐： 其中A、B、C、D、T、Y和Z分别表示亚甲基或氮键合物；R1、R2、R3、R4和R5分别表示取代基；n表示0或1至3的整数；m表示0或1至6的整数；p表示1至3的整数。这些化合物具有5-羟色胺拮抗作用。因此，在临床上作为药物特别有用，用于治疗、改善和预防痉挛性瘫痪。它们还可用作中枢肌肉松弛剂，改善肌张力过高。

  公开号：

  US20020019531A1
• 作为产物：
  描述：

  7-甲氧基-1-萘满酮 在 titanium(IV) isopropylate 、 sodium tetrahydroborate 作用下， 以 乙醇 为溶剂， 生成 7-Methoxy-1-(piperazin-1-yl)-1,2,3,4-tetrahydronaphthalene
  参考文献：
  名称：

  Indanyl piperazines as melatonergic MT2 selective agents

  摘要：

  Optimization of a benzyl piperazine pharmacophore produced N-acyl-4-indanyl-piperazines that bind with high affinity to melatonergic MT2 receptors. (R)-4-(2,3-dihydro-6-methoxy-1H-inden-1-yl)-N-ethyl-1-piperazine-carboxamide fumarate (13) is a water soluble, selective MT2 agonist, which produces advances in circadian phase in rats at doses of 1-56 mg/kg that are no different from those of melatonin at 1 mg/kg. Unlike melatonin, 13 produced only weak contractile effects in rat tail artery. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00090-8

文献信息

• Indolone derivatives, their preparation and their application in therapy
  申请人：Synthelabo

  公开号：US05010079A1

  公开（公告）日：1991-04-23

  An indolone derivative is useful for the treatment of anxiety, depression and schizophrenia and is a 5HT.sub.1A agonist and 5HT.sub.2 antagonist, which is a compound of formula (I): ##STR1## in which R.sub.1 is a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical, R.sub.2 is a hydrogen atom or a (C.sub.1-4)alkyl radical, R.sub.3 is a hydrogen atom, a (C.sub.1-4)alkyl radical or an S-(C.sub.1-4) alkyl radical; and R.sub.4 is a phenyl, chlorophenyl, naphthyl, 7-methoxy-1-naphthyl, 6-methoxy-1-indanyl, 2-methoxy-6-pyridyl, 3-methoxy-2-pyridyl, isoquinolyl, 7-methoxy-1-isoquinolyl, 7-methoxy-1,2,3,4-tetrahydro-1-naphthyl or 7-fluoro-1-naphthyl radical; or a pharmaceutically acceptable acid addition salt thereof.

  一种吲哚酮衍生物对焦虑、抑郁和精神分裂症的治疗具有用处，是一种5HT.sub.1A激动剂和5HT.sub.2拮抗剂，其化学式为(I)：##STR1## 其中R.sub.1是氢原子或卤素原子或(C.sub.1-4)烷基基团，R.sub.2是氢原子或(C.sub.1-4)烷基基团，R.sub.3是氢原子、(C.sub.1-4)烷基基团或S-(C.sub.1-4)烷基基团；R.sub.4是苯基、氯苯基、萘基、7-甲氧基-1-萘基、6-甲氧基-1-茚基、2-甲氧基-6-吡啶基、3-甲氧基-2-吡啶基、异喹啉基、7-甲氧基-1-异喹啉基、7-甲氧基-1,2,3,4-四氢-1-萘基或7-氟-1-萘基基团；或其药学上可接受的酸盐。
• Melatonergic indanyl piperazines
  申请人：Bristol-Myers Squibb Company

  公开号：US05780470A1

  公开（公告）日：1998-07-14

  Certain indanyl piperazines are useful as melatonergic agents and can treat various CNS disorders. They are use useful in treating sleep disorders and other conditions related to circadian rhythms.

  某些吲哚基哌嗪可作为褪黑素受体激动剂，可用于治疗各种中枢神经系统疾病。它们在治疗睡眠障碍和与昼夜节律相关的其他疾病方面非常有用。
• Quinoline derivatives
  申请人：Eisai Co., Ltd.

  公开号：US07071201B2

  公开（公告）日：2006-07-04

  A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

  一种新型化合物的公式：其中A、B、C、D、T、Y和Z分别代表亚甲基或氮；R1、R2、R3、R4和R5分别代表取代基；n代表0或1至3的整数；m代表0或1至6的整数；p代表1至3的整数；以及其药理学上可接受的盐。该化合物具有5-羟色胺拮抗作用，临床上可作为药物使用，特别是用于治疗、改善和预防痉挛性瘫痪或中枢肌肉松弛剂以改善肌强直症状。
• Novel melatonergic indanyl piperazines or homopiperazines
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：EP0745597A2

  公开（公告）日：1996-12-04

  Certain indanyl piperazines are useful as melatonergic agents and can treat various CNS disorders. They are use useful in treating sleep disorders and other conditions related to circadian rhythms.

  某些茚并苝类化合物可用作褪黑激素能药物，治疗各种中枢神经系统疾病。它们可用于治疗睡眠障碍和其他与昼夜节律有关的疾病。
• 1,4-SUBSTITUTED CYCLIC AMINE DERIVATIVES
  申请人：Eisai Co., Ltd.

  公开号：EP0976732A1

  公开（公告）日：2000-02-02

  A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, R4 and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3.) The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

  由下式代表的新型 1，4-取代环胺衍生物或其药理学上可接受的盐： (其中 A、B、C、D、T、Y 和 Z 分别代表甲烷或氮；R1、R2、R3、R4 和 R5 分别代表取代基；n 代表 0 或 1 至 3 的整数；m 代表 0 或 1 至 6 的整数；p 代表 1 至 3 的整数）。 该化合物具有血清素拮抗作用，在临床上可用作药物，特别是用于治疗、改善和预防痉挛性瘫痪或用于改善肌张力的中枢性肌肉松弛剂。