1-(2-hydroxyphenyl)piperazine dihydrobromide | 58260-69-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(2-hydroxyphenyl)piperazine dihydrobromide
• 英文别名: 2-(1-piperazinyl)phenol dihydrobromide；2-piperazino-phenol; dihydrobromide；2-Piperazino-phenol; Dihydrobromid；o-(1-piperazinyl)phenol dihydrobromide；2-hydroxyphenylpiperazine dihydrobromide salt；2-(Piperazin-1-yl)phenol hydrobromide；2-piperazin-1-ylphenol;hydrobromide
• CAS: 58260-69-8
• 化学式: 2BrH*C₁₀H₁₄N₂O
• 分子量: 340.058
• InChiKey: KOLZUNYLPQYZQD-UHFFFAOYSA-N

物化性质

• 熔点：
  260°C (dec.)

计算性质

• 辛醇/水分配系数(LogP)：
  1.38
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  35.5
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xi
• 安全说明：
  S26,S36/37/39
• 危险类别码：
  R36/37/38
• 海关编码：
  2933599090

反应信息

• 作为反应物：
  描述：

  1-(2-hydroxyphenyl)piperazine dihydrobromide 在 potassium carbonate 作用下， 以 水 为溶剂， 生成 1-(2-羟基苯基)哌嗪
  参考文献：
  名称：

  WO2006/50048

  摘要：

  公开号：
• 作为产物：
  描述：

  1-(2-甲氧苯基)哌嗪 在 氢溴酸 作用下， 生成 1-(2-hydroxyphenyl)piperazine dihydrobromide
  参考文献：
  名称：

  苯基和苯甲酰基哌嗪作为潜在的血清素能药物的合成与评价。

  摘要：

  研究了一系列苯基哌嗪（3）和苯甲酰基哌嗪（4）与5-羟色胺中心部位的结合。3的几种衍生物显示出对5-HT1位点的纳摩尔亲和力，而4的衍生物在5-HT1和5-HT2位点上基本上没有活性。发现1-（2-甲氧基苯基）哌嗪（2-MPP，3a）对5-HT1位点具有亲和力（Ki = 35 nM）与公认的5-HT激动剂1- [3-（三氟甲基）苯基]哌嗪（TFMPP）（Ki = 20 nM）；图3a还显示了对5-HT1位点的100倍选择性（相比于TFMPP的8倍）。在使用训练以从盐水中区分TFMPP（ED50 = 0.17 mg / kg）的大鼠进行的刺激泛化测试中，发现3a与训练药物几乎等效（ED50 = 0.22 mg / kg）。

  DOI：

  10.1021/jm00155a008

文献信息

• Pyrimidinylpyrazole derivatives
  申请人：Daiichi Pharmaceutical Co., Ltd.

  公开号：US05852019A1

  公开（公告）日：1998-12-22

  The present invention provides a novel compound which is represented by formula (I): ##STR1## wherein preferable examples of R.sup.1 to R.sup.6 are as follows; R.sup.1 and R.sup.2 are each an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a hydrogen atom, a halogen atom or an alkoxyl group; R.sup.3 is a hydrogen atom; R.sup.4 is a methyl group; R.sup.5 is a hydrogen atom or an alkyl group; and R.sup.6 is a group of the formula: ##STR2## wherein Z is a phenyl group; and has an antitumor effect.

  本发明提供了一种新型化合物，其由式(I)表示：##STR1##其中R.sup.1至R.sup.6的优选示例如下；R.sup.1和R.sup.2分别是可选择地由卤原子、氨基、羟基、烷氧基或硫醇基取代的烷基基团，氢原子，卤原子或烷氧基；R.sup.3是氢原子；R.sup.4是甲基基团；R.sup.5是氢原子或烷基基团；R.sup.6是下式的基团：##STR2##其中Z是苯基；并具有抗肿瘤作用。
• Method of treating anxiety with 5-[(4-aryl or
  申请人：A. H. Robbins Company, Incorporated

  公开号：US05162322A1

  公开（公告）日：1992-11-10

  This invention discloses the antianxiety properties of compounds of the formula: ##STR1## wherein n is 3 or 4, R is C.sub.1 -C.sub.4 alkyl or phenyl, and Ar is ##STR2## where Z is selected from H, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyloxy or hydroxy.

  这项发明揭示了以下式化合物的抗焦虑特性：##STR1## 其中n为3或4，R为C.sub.1 -C.sub.4烷基或苯基，Ar为##STR2## 其中Z选自H，C.sub.1 -C.sub.4烷氧基，C.sub.2 -C.sub.4烯氧基或羟基。
• Certain aryl-aliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
  申请人：Biovitrum AB

  公开号：US06465467B1

  公开（公告）日：2002-10-15

  Compounds of the general formula (I): wherein the variables are as defined in the specification are useful for the prophylaxis or treatment of serotonin-related, especially 5-HT2 receptor-related, diseases in human beings or animals, particularly diseases related to the 5-HT2c receptor, especially diseases such as eating disorders, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctionions, and urinary disorders.

  通式（I）的化合物： 其中变量如规范中定义的那样，对于预防或治疗人类或动物中与血清素相关，特别是5-HT2受体相关的疾病是有用的，特别是与5-HT2c受体相关的疾病，尤其是与进食障碍、记忆障碍、精神分裂症、情绪障碍、焦虑障碍、疼痛、性功能障碍和尿液障碍等疾病相关的疾病。
• Benzopyranones, a method for producing them and uses therefor
  申请人：Dr. Willmar Schwabe GmbH & Co.

  公开号：US05428038A1

  公开（公告）日：1995-06-27

  Novel 2H-1-benzopyran-2-ones (coumarin derivatives) of the general formula (I) are provided: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and Y are defined as in the specification, and the addition compounds thereof with physiologically compatible acids, intermediates and methods for the preparation thereof. The coumarin compounds possess a neuroprotective and anti-allergic action.

  提供一般式(I)的新型2H-1-苯并吡喃-2-酮（香豆素衍生物）：##STR1## 其中R.sup.1、R.sup.2、R.sup.3、R.sup.4、X和Y的定义如规范中所述，并与生理兼容酸的加合物、中间体及其制备方法。香豆素化合物具有神经保护和抗过敏作用。
• Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy
  作者：Gregory E. Martin、Robert J. Elgin、Joanne R. Mathiasen、Coralie B. Davis、James M. Kesslick、William J. Baldy、Richard P. Shank、Deena L. DiStefano、Cynthia L. Fedde、Malcom K. Scott

  DOI：10.1021/jm00125a020

  日期：1989.5

  Generally, antipsychotic agents are dopamine receptor blocking agents that also block conditioned avoidance responding (CAR) in the rat. Recently, however, both (Q-methoxyphenyl)piperazine (OMPP, 1h) and (m-chlorophenyl)piperazine (MCPP, 1o) have been reported to block conditioned avoidance responding in the rat although neither has dopamine receptor blocking properties. The present paper examines the behavioral and biochemical profile of a number of additional substituted phenylpiperazines. None of the phenylpiperazines tested demonstrated high affinity for either dopamine D-1 or D-2 receptor sites, yet many were effective in blocking CAR. The results suggest that the phenylpiperazines may be effective antipsychotic agents without blocking dopamine receptors. Moreover, the active compounds did demonstrate activity in displacing ligand binding to serotonin receptors. Receptor binding profiles were determined for 5-HT-1A and 5-HT-1B binding sites as well as for 5-HT-2 sites. The data from this preclinical test suggest these phenylpiperazines might be effective antipsychotic agents acting via a nondopaminergic mechanism of action.