4-(2-吡啶基)-1-哌嗪乙醇 | 40004-68-0

• 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: 4-(2-吡啶基)-1-哌嗪乙醇
• 英文名称: 2-<4-(pyridin-2-yl)piperazin-1-yl>ethanol
• 英文别名: 2-(4-[2]pyridyl-piperazino)-ethanol；2-(4-[2]Pyridyl-piperazino)-aethanol；4-(2-pyridyl)-1-piperazineethanol；4-(pyridin-2-yl)-1-piperazineethanol；1-(2-hydroxyethyl)-4-(2-pyridyl)piperazine；2-(4-pyridin-2-yl-piperazin-1-yl)ethanol；2-[4-(Pyridin-2-yl)piperazin-1-yl]ethan-1-ol；2-(4-pyridin-2-ylpiperazin-1-yl)ethanol
• CAS: 40004-68-0
• 化学式: C₁₁H₁₇N₃O
• mdl: MFCD06620199
• 分子量: 207.275
• InChiKey: JADLXZSDPDFNLC-UHFFFAOYSA-N

物化性质

• 沸点：
  377.8±37.0 °C(Predicted)
• 密度：
  1.144±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.545
• 拓扑面积：
  39.6
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  4-(2-吡啶基)-1-哌嗪乙醇 在 哌啶 、 sodium hydride 、 苯甲酸 作用下， 以 甲苯 为溶剂， 反应 6.5h， 生成 5-[4-[2-[4-(2-Pyridyl)-1-piperazinyl]ethoxy]phenylmethylene]thiazolidine-2,4-dione
  参考文献：
  名称：

  Novel Euglycemic and Hypolipidemic Agents. 4. Pyridyl- and Quinolinyl-Containing Thiazolidinediones

  摘要：

  A series of substituted pyridyl- and quinolinyl-containing 2,4-thiazolidinediones having interesting cyclic amine as a linker have been synthesized. Both unsaturated thiazolidinediones 5 and saturated thiazolidinediones 6 and their various salts were evaluated in db/db mice for euglycemic and hypolipidemic effects and compared with BRL compound 11 and BRL-49653, respectively. Some of the potent compounds were converted to various salts in order to obtain improved activities. Among all the salts evaluated, the maleate salt of unsaturated TZD 5a was found to be a very potent euglycemic and hypolipidemic compound. Some of the more interesting compounds have also been evaluated in ob/ob mice and compared with rosiglitazone (maleate salt of BRL-49653). Oral glucose tolerance tests were performed in both db/db and ob/ob mice. Pharmacokinetic studies of 5a maleate are also reported. Receptor binding studies of PPAR gamma by 5a/5a maleate did not show any significant transactivation of PPAR alpha or PPAR gamma.

  DOI：

  10.1021/jm980622j
• 作为产物：
  描述：

  2-氯吡啶 在 potassium carbonate 作用下， 以 二甲基亚砜 为溶剂， 反应 16.0h， 生成 4-(2-吡啶基)-1-哌嗪乙醇
  参考文献：
  名称：

  Novel Euglycemic and Hypolipidemic Agents. 4. Pyridyl- and Quinolinyl-Containing Thiazolidinediones

  摘要：

  A series of substituted pyridyl- and quinolinyl-containing 2,4-thiazolidinediones having interesting cyclic amine as a linker have been synthesized. Both unsaturated thiazolidinediones 5 and saturated thiazolidinediones 6 and their various salts were evaluated in db/db mice for euglycemic and hypolipidemic effects and compared with BRL compound 11 and BRL-49653, respectively. Some of the potent compounds were converted to various salts in order to obtain improved activities. Among all the salts evaluated, the maleate salt of unsaturated TZD 5a was found to be a very potent euglycemic and hypolipidemic compound. Some of the more interesting compounds have also been evaluated in ob/ob mice and compared with rosiglitazone (maleate salt of BRL-49653). Oral glucose tolerance tests were performed in both db/db and ob/ob mice. Pharmacokinetic studies of 5a maleate are also reported. Receptor binding studies of PPAR gamma by 5a/5a maleate did not show any significant transactivation of PPAR alpha or PPAR gamma.

  DOI：

  10.1021/jm980622j

文献信息

• Substituted heterocyclylalkyl esters of
  申请人：Takeda Chemical Industries, Ltd.

  公开号：US04892875A1

  公开（公告）日：1990-01-09

  Dihydropyridine derivatives and acid addition salts thereof which are of use as prophylactic or/and therapeutic drugs for cardiovascular diseases, said dihydropyridine derivatives having the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is alkyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; R.sup.4 and R.sup.5 are the same or different and each is hydrogen, halogen, nitro, trifluoromethyl, alkyl, cycloalkyl, alkoxy, cyano, alkoxycarbonyl or alkylthio; R.sup.6 is hydrogen, alkyl, cycloalkyl, aralkyl, aryl or a pyridyl; X is oxygen, sulfur, vinylene, azomethine or a group of the formula ##STR2## A is alkylene; Ar is aryl or a pyridyl; m is an integer of 1 to 3; n is an integer of 0 to 2.

  二氢吡啶衍生物及其酸加成盐，可用于心血管疾病的预防和/或治疗药物，所述二氢吡啶衍生物具有以下式子：##STR1## 其中R.sup.1，R.sup.2和R.sup.3相同或不同，每个都是烷基，环烷基，环烷基烷基或烷氧基烷基; R.sup.4和R.sup.5相同或不同，每个都是氢，卤素，硝基，三氟甲基，烷基，环烷基，烷氧基，氰基，烷氧羰基或烷基硫基; R.sup.6是氢，烷基，环烷基，芳基烷基，芳基或吡啶基; X是氧，硫，乙烯基，偶氮基或式子##STR2## 的基团; A是烷基; Ar是芳基或吡啶基; m是1到3的整数; n是0到2的整数。
• PHENANTHRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS
  申请人：Beke Gyula

  公开号：US20090270411A1

  公开（公告）日：2009-10-29

  The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specification, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.

  本发明涉及公式（I）的新苯并喹啉衍生物，其中变量如规范中所定义，涉及制备这些衍生物的过程，包含这些衍生物的药理组合物以及它们在治疗或预防疼痛和炎症过程中的用途。
• SULFONAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS
  申请人：Bozo Eva

  公开号：US20100075978A1

  公开（公告）日：2010-03-25

  The present invention relates to new sulfonamide derivatives of formula (I) wherein R 1 -R 5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

  本发明涉及公式（I）的新型磺酰胺衍生物， 其中R1-R5和Z如权利要求中所定义，以及其光学对映体或外消旋体和/或盐和/或水合物和/或溶剂化物，它们是缓激肽B1的选择性拮抗剂，用于制备这些化合物的方法，包含它们的药理学组合物以及在治疗或预防疼痛和炎症状况中的使用。
• Dihydropyridinderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
  申请人：Byk Gulden Lomberg Chemische Fabrik GmbH

  公开号：EP0244595A2

  公开（公告）日：1987-11-11

  Monocyclische Ester der Formel 1, worin die Substituenten und Symbole die in der Beschreibung genannten Bedeutungen haben, sind neue Verbindungen mit überraschenden pharmakologischen Eigenschaften.

  式 1 的单环酯（其中的取代基和符号具有说明中给出的含义）是具有惊人药理特性的新化合物。
• [EN] NEW PHENANTHRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS<br/>[FR] NOUVEAUX DERIVES DE PHENANTHRIDINE UTILISES COMME ANTAGONISTES DE LA BRADYKININE
  申请人：RICHTER GEDEON VEGYESZET

  公开号：WO2007072092A3

  公开（公告）日：2007-11-01