2-哌啶-1-基吡嗪 | 6705-23-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 2-哌啶-1-基吡嗪
• 英文名称: 2-(piperidin-1-yl)pyrazine
• 英文别名: 2-N-piperidinopyrazine；piperidylpyrazine；2-piperidin-1-yl-pyrazine；2-Piperidino-pyrazin；Piperidino-pyrazin；2-piperidin-1-ylpyrazine
• CAS: 6705-23-3
• 化学式: C₉H₁₃N₃
• mdl: MFCD27927258
• 分子量: 163.222
• InChiKey: FMPQINQOBNERLC-UHFFFAOYSA-N

物化性质

• 沸点：
  288.9±20.0 °C(predicted)
• 密度：
  1.101±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.555
• 拓扑面积：
  29
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-哌啶-1-基吡嗪 在 N-溴代丁二酰亚胺(NBS) 作用下， 以 二甲基亚砜 为溶剂， 生成 3,5-Dibromo-2-(piperidin-1-yl)pyrazine
  参考文献：
  名称：

  2,3-Diaminopyrazines as rho kinase inhibitors

  摘要：

  Inhibition of rho kinase ( ROCK) has been recognized as an important target for a number of diseases, including glaucoma. Herein we report SAR development around two hits from a kinase library that led to the discovery of the ROCK inhibitor compound 38. In vitro and in vivo analysis of this compound, including its effects in a monkey model of glaucoma will be discussed. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.12.012
• 作为产物：
  描述：

  哌啶 、 2-氯吡嗪 在 potassium phosphate 作用下， 以 水 为溶剂， 反应 12.0h， 以78%的产率得到2-哌啶-1-基吡嗪
  参考文献：
  名称：

  Towards aryl C–N bond formation in dynamic thin films

  摘要：

  C–N 键形成反应在有机化学中非常重要。采用受限模式操作的薄膜微流体漩涡流体装置（VFD）可以从 2-氯吡嗪和相应的胺中合成 N-芳基化合物，而无需过渡金属催化剂。

  DOI：

  10.1039/c4ob00926f

文献信息

• [EN] INDENE DERIVATIVES, THEIR PREPARATION AND USE AS MEDICAMENTS<br/>[FR] DÉRIVÉS D'INDÈNE, LEUR PRÉPARATION ET LEUR UTILISATION EN TANT QUE MÉDICAMENTS
  申请人：ESTEVE LABOR DR

  公开号：WO2014006071A1

  公开（公告）日：2014-01-09

  The present invention relates to new indene derivatives having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.

  本发明涉及新的茚衍生物，特别是对sigma受体，尤其是sigma-1受体具有较大亲和力的茚衍生物，以及它们的制备过程、包含它们的组合物，以及它们作为药物的使用。
• Indene derivatives, their preparation and use as medicaments
  申请人：Laboratorios del. Dr. Esteve, S.A.

  公开号：EP2682391A1

  公开（公告）日：2014-01-08

  The present invention relates to new indene derivatives having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.

  本发明涉及新的茚衍生物，这些衍生物对sigma受体，特别是sigma-1受体具有很高的亲和力，以及它们的制备过程，包含它们的组合物，以及它们作为药物的使用。
• THERAPEUTIC COMPOUNDS AND COMPOSITIONS
  申请人：Salituro Francesco G.

  公开号：US20100331307A1

  公开（公告）日：2010-12-30

  Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

  本文描述了调节丙酮酸激酶M2（PKM2）的化合物和含有这些化合物的组合物。本文还描述了利用调节PKM2的化合物治疗癌症的方法。
• Substituted aryl or heteroarylpiperidine derivatives as melanocortin-4 receptor modulators
  申请人：Santhera Pharmaceuticals (Schweiz) AG

  公开号：EP2020405A1

  公开（公告）日：2009-02-04

  The present invention relates to substituted aryl or heteroarylpiperidine derivatives of structure (I) as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.

  本发明涉及结构式(I)的取代芳基或杂芳基哌啶衍生物，作为黑色素皮质素-4受体调节剂。根据结构和立体化学，本发明的化合物可以是人类黑色素皮质素-4受体(MC-4R)的选择性激动剂或选择性拮抗剂。激动剂可用于治疗肥胖、糖尿病和性功能障碍等疾病，而拮抗剂可用于治疗癌症恶病质、肌肉消耗、厌食症、焦虑和抑郁等疾病。一般来说，所有涉及MC-4R调节的疾病和疾病都可以用本发明的化合物进行治疗。
• Phenyl, Pyridine, Quinoline, Isoquinoline, Naphthyridine and Pyrazine Derivatives
  申请人：Binggeli Alfred

  公开号：US20080045544A1

  公开（公告）日：2008-02-21

  This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

  这项发明涉及公式的化合物及其药用盐。该发明还涉及含有这种化合物的药物组合物，以及用于制备它们的过程以及它们用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。