1-(2,3-二甲氧基丙基)-哌嗪 | 329217-27-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 1-(2,3-二甲氧基丙基)-哌嗪
• 英文名称: 1-(2,3-dimethoxypropyl)piperazine
• CAS: 329217-27-8
• 化学式: C₉H₂₀N₂O₂
• 分子量: 188.27
• InChiKey: VXSDCSNXIDVDPO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  13
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  33.7
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933599090

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-(2,3-二甲氧基丙基)-哌嗪 以 xylene 为溶剂， 反应 8.0h， 生成 11-[4-(2,3-Dimethoxy-propyl)-piperazin-1-yl]-dibenzo[b,f][1,4]thiazepine
  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+
• 作为产物：
  描述：

  1-(2,3-二甲氧基丙基)-4-苯基甲基哌嗪 在 10percent Pd/C 氢气 作用下， 以 乙醇 为溶剂， 50.0 ℃ 、344.75 kPa 条件下， 反应 1.5h， 以72%的产率得到1-(2,3-二甲氧基丙基)-哌嗪
  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

• COMPOSITION FOR CARBON DIOXIDE SEPARATION AND METHOD FOR SEPARATING CARBON DIOXIDE
  申请人：Tosoh Corporation

  公开号：EP4098348A1

  公开（公告）日：2022-12-07

  To provide a carbon dioxide separation composition which is excellent in carbon dioxide desorption efficiency (desorption amount/absorption amount) and durability to nitrogen oxides, and a method for separating carbon dioxide. A carbon dioxide separation composition, containing at least one amine compound selected from the group consisting of an amine compound represented by the following formula (1): wherein R1 to R3 each independently represent a hydrogen atom or a C1-4 alkyl group, and an amine compound represented by the following formula (2): wherein R10, R11, R12, R13 and R14 each independently represent a hydrogen atom, a C1-4 alkyl group, a hydroxy group, a hydroxymethyl group, a 2-hydroxyethyl group or a C1-4 alkoxy group, a and b are each independently 0 or 1 and satisfy the relation a+b=1, and R15 is a hydrogen atom, a C1-4 alkyl group, a methoxymethyl group, a methoxyethoxymethyl group or a 2-hydroxyethyl group.

  提供一种在二氧化碳解吸效率（解吸量/吸附量）和对氮氧化物的耐久性方面性能优异的二氧化碳分离组合物，以及一种分离二氧化碳的方法。 一种二氧化碳分离组合物，含有至少一种选自由下式（1）表示的胺化合物组成的组中的胺化合物： 其中R1至R3各自独立地代表氢原子或C1-4烷基，以及由下式(2)代表的胺化合物： 其中 R10、R11、R12、R13 和 R14 各自独立地代表氢原子、C1-4 烷基、羟基、羟甲基、2-羟乙基或 C1-4 烷氧基、 a 和 b 各自独立地为 0 或 1，并满足 a+b=1 的关系式，以及 R15 是氢原子、C1-4 烷基、甲氧基甲基、甲氧基乙氧基甲基或 2-羟乙基。
• [EN] COMPOSITION FOR CARBON DIOXIDE SEPARATION AND METHOD FOR SEPARATING CARBON DIOXIDE<br/>[FR] COMPOSITION POUR LA SÉPARATION DE DIOXYDE DE CARBONE ET PROCÉDÉ POUR SÉPARER DU DIOXYDE DE CARBONE<br/>[JA] 二酸化炭素分離用組成物、及び二酸化炭素の分離方法
  申请人：TOSOH CORP

  公开号：WO2021153650A1

  公开（公告）日：2021-08-05

  二酸化炭素の放散効率（放散量／吸収量）と窒素酸化物耐久性に優れた二酸化炭素分離用組成物、及び二酸化炭素の分離方法の提供。　下記一般式（１）［上記一般式（１）中、Ｒ１～Ｒ３は、各々独立して、水素原子、又は炭素数１～４のアルキル基を表す。］で示されるアミン化合物、及び下記一般式（２）［上記一般式（２）中、Ｒ１０、Ｒ１１、Ｒ１２、Ｒ１３及びＲ１４は、各々独立して、水素原子、炭素数１～４のアルキル基、水酸基、ヒドロキシメチル基、２－ヒドロキシエチル基、又は炭素数１～４のアルコキシ基を表す。 ａ及びｂは、それぞれ独立に、０又は１であり、ａ＋ｂ＝１の関係を満たす。 Ｒ１５は、水素原子、炭素数１～４のアルキル基、メトキシメチル基、メトキシエトキシメチル基、又は２－ヒドロキシエチル基を表す。］ で示されるアミン化合物からなる群より選ばれる少なくとも一つのアミン化合物を含むことを特徴とする二酸化炭素分離用組成物を用いる。
• Behavioral Approach to Nondyskinetic Dopamine Antagonists:  Identification of Seroquel
  作者：Edward J. Warawa、Bernard M. Migler、Cyrus J. Ohnmacht、Ann L. Needles、George C. Gatos、Frances M. McLaren、Cynthia L. Nelson、Karen M. Kirkland

  DOI：10.1021/jm000242+

  日期：2001.2.1

  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.