1-(3-氟吡啶-2-基)-4-甲基哌嗪 | 85386-90-9

• 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-(3-氟吡啶-2-基)-4-甲基哌嗪
• 英文名称: 1-methyl-4-(3-fluoro-2-pyridinyl)piperazine
• 英文别名: 1-(3-Fluoropyridin-2-yl)-4-methylpiperazine
• CAS: 85386-90-9
• 化学式: C₁₀H₁₄FN₃
• 分子量: 195.24
• InChiKey: KZNJAAWCEFRAPW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  19.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  N-甲基哌嗪 、 2-氯-3-氟吡啶 在 乙醚 、 sodium hydroxide 、 氯化钠 、 Sodium sulfate-III 、 hydrogen fumarate salt 、 富马酸 、 甲醇 作用下， 以 正丁醇 为溶剂， 反应 18.0h， 生成 1-(3-氟吡啶-2-基)-4-甲基哌嗪
  参考文献：
  名称：

  1-(3-Halo-2-pyridinyl) piperazine

  摘要：

  1-(3-卤代-2-吡啶基)哌嗪及其酸加成盐是选择性α2-肾上腺素能受体拮抗剂，因此可用作抗抑郁剂，用于治疗抗高血压药物引起的镇静作用。

  公开号：

  US04456604A1

文献信息

• [EN] MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR<br/>[FR] MODULATEURS DU RÉGULATEUR DE LA CONDUCTANCE TRANSMEMBRANAIRE DE LA MUCOVISCIDOSE
  申请人：VERTEX PHARMA

  公开号：WO2022076627A1

  公开（公告）日：2022-04-14

  This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having the core structure:, pharmaceutical compositions containing at least one such modulator, methods of treating CFTR mediated diseases, including cystic fibrosis using such modulators and pharmaceutical compositions, combination therapies and combination pharmaceuticals employing those modulators, and processes and intermediates for making such modulators.

  本公开提供囊性纤维化跨膜传导调节因子（CFTR）的调节剂，其具有以下核心结构：，包含至少一种这样的调节剂的药物组合物，使用这样的调节剂和药物组合物治疗CFTR介导的疾病，包括囊性纤维化的方法，使用这些调节剂的组合疗法和组合药物，以及制造这些调节剂的过程和中间体。
• 1-(3-Halo-2-pyridinyl)piperazines, processes for their preparation and pharmaceutical composition containing them
  申请人：Merck & Co., Inc.

  公开号：EP0065757A1

  公开（公告）日：1982-12-01

  1-(3-Halo-2-pyridinyl)piperazine and its acid addition salts are selective a2-adrenergic receptor antagonists and thereby useful as antidepressant agents and for treating sedation caused by antihypertensive therapy.

  1-（3-卤代-2-吡啶基）哌嗪及其酸加成盐是选择性的 a2 肾上腺素能受体拮抗剂，因此可用作抗抑郁药和治疗降压治疗引起的镇静。
• Pyridinylpiperazines, a new class of selective .alpha.2-adrenoceptor antagonists
  作者：Walfred S. Saari、Wasyl Halczenko、Stella W. King、Joel R. Huff、James P. Guare、Cecilia A. Hunt、William C. Randall、Paul S. Anderson、Victor J. Lotti

  DOI：10.1021/jm00366a007

  日期：1983.12

  A series of 1-(2-pyridinyl)piperazine derivatives was synthesized and evaluated for adrenergic activity. In vitro activity was assessed through the antagonism of clonidine's effect in the rat, isolated, field-stimulated vas deferens and by the displacement of [3H]clonidine from membrane binding sites of calf cerebral cortex. Antagonism of clonidine-induced mydriasis in the rat was used as an in vivo assay. Several members of the series proved to be potent, selective alpha 2-adrenoceptor antagonists. 1-(3-Fluoro-2-pyridinyl)piperazine was more potent than either yohimbine or rauwolscine in displacement of [3H]clonidine and had a higher affinity for this binding site (alpha 2) than for the [3H]prazosin site (alpha 1). In vivo, the 3-F derivative was more potent than the reference standards in reversing clonidine-induced mydriasis. None of the members of this series was more selective or potent than rauwolscine in antagonizing clonidine in the rat vas deferens.
• SAARI, W. S.
  作者：SAARI, W. S.

  DOI：——

  日期：——
• US4456604A
  申请人：——

  公开号：US4456604A

  公开（公告）日：1984-06-26