1-(2-<2-(2-Hydroxy-ethoxy)-ethoxy>-ethyl)-piperazin | 68465-68-9

• 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-<2-(2-Hydroxy-ethoxy)-ethoxy>-ethyl)-piperazin
• 英文别名: 2-[2-(2-Piperazin-1-ylethoxy)ethoxy]ethanol
• CAS: 68465-68-9
• 化学式: C₁₀H₂₂N₂O₃
• 分子量: 218.296
• InChiKey: GYCLKODXTAIUAY-UHFFFAOYSA-N

物化性质

• 沸点：
  155 °C(Press: 1 Torr)
• 密度：
  1.052±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  15
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  54
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  11-氯-二苯并[b,f][1,4]硫氮杂卓 、 1-(2-<2-(2-Hydroxy-ethoxy)-ethoxy>-ethyl)-piperazin 以 xylene 为溶剂， 生成 喹硫平杂质DHCl
  参考文献：
  名称：

  Behavioral Approach to Nondyskinetic Dopamine Antagonists:  Identification of Seroquel

  摘要：

  A great need exists for antipsychotic drugs which will not induce extrapyramidal symptoms (EPS) and tardive dyskinesias (TDs). These side effects are deemed to be a consequence of nonselective blockade of nigrostriatal and mesolimbic dopamine D2 receptors. Nondyskinetic clozapine (1) is a low-potency D2 dopamine receptor antagonist which appears to act selectively in the mesolimbic area. In this work dopamine antagonism was assessed in two mouse behavioral assays: antagonism of apomorphine-induced climbing and antagonism of apomorphine-induced disruption of swimming. The potential for the liability of dyskinesias was determined in haloperidol-sensitized Cebus monkeys. Initial examination of a few close cogeners of 1 enhanced confidence in the Cebus model as a predictor of dyskinetic potential. Considering dibenzazepines, 2 was not dyskinetic whereas 2a was dyskinetic. Among dibenzodiazepines, 1 did not induce dyskinesias where as its N-2-(2-hydroxyethoxy)ethyl analogue 3 was dyskinetic. The emergence of such distinctions presented an opportunity. Thus, aromatic and N-substituted analogues of 6-(piperazin-1-yl)-11H-dibenz[b,e]azepines and 11-(piperazin-1-yl)dibenzo[b,f][1,4]thiazepines and -oxazepines were prepared and evaluated. 11-(4-[2-(2-Hydroxyethoxy)ethyl]piperazin-1-yl)dibenzo[b,f][1,4]thiazepine (23) was found to be an apomorphine antagonist comparable to clozapine. It was essentially nondyskinetic in the Cebus model. With 23 as a platform, a number of N-substituted analogues were found to be good apomorphine antagonists but all were dyskinetic.

  DOI：

  10.1021/jm000242+

文献信息

• Polymethoxybenzyl piperazine derivatives, processes for their preparation and pharmaceutical compositions containing said derivatives
  申请人：WAKO PURE CHEMICAL INDUSTRIES, LTD.

  公开号：EP0144991A2

  公开（公告）日：1985-06-19

  A compound of the formula: (R = H, CH30; n = 2 to 5) is effective for improving blood circulation system.

  式中：（R = H，CH30；n = 2 至 5）的化合物可有效改善血液循环系统。
• [EN] EGFR PROTEOLYSIS TARGETING CHIMERIC MOLECULES AND ASSOCIATED METHODS OF USE<br/>[FR] MOLÉCULES CHIMÉRIQUES CIBLANT LA PROTÉOLYSE DE L'EGFR ET PROCÉDÉS D'UTILISATION ASSOCIÉS
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2018119441A9

  公开（公告）日：2019-10-10
• US4097597A
  申请人：——

  公开号：US4097597A

  公开（公告）日：1978-06-27
• US4574156A
  申请人：——

  公开号：US4574156A

  公开（公告）日：1986-03-04
• [DE] VERFAHREN ZUR HOMOGEN-KATALYSIERTEN HERSTELLUNG VON MONO-N-SUBSTITUIERTEN-PIPERAZINEN<br/>[EN] METHOD FOR THE HOMOGENEOUSLY CATALYZED PRODUCTION OF MONO-N-SUBSTITUTED PIPERAZINES<br/>[FR] PROCÉDÉ DE PRODUCTION À CATALYSE HOMOGÈNE DE PIPÉRAZINES MONO-N-SUBSTITUÉES
  申请人：BASF SE

  公开号：WO2017125358A1

  公开（公告）日：2017-07-27

  Verfahren zur Herstellung von Mono-N-substituierten-piperazinen der allgemeinen Formel (I) durch homogen-katalysierte Alkoholaminierung von Alkoholen der allgemeinen Formel (II) mit Piperazin (III) in Gegenwart eines Komplexkatalysators (IV), der Iridium enthält.