2-N-(4-methyl)piperidinopyrazine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-N-(4-methyl)piperidinopyrazine
• 英文别名: 2-(4-Methylpiperidin-1-yl)pyrazine
• 化学式: C₁₀H₁₅N₃
• 分子量: 177.249
• InChiKey: XTFDEAZCIHJMTC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  29
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-氯吡嗪 、 4-甲基哌啶 反应 2.0h， 以77%的产率得到2-N-(4-methyl)piperidinopyrazine
  参考文献：
  名称：

  Synthesis and Fluorescence Properties 2-N-Piperidinopyrazines

  摘要：

  通过 2-氯吡嗪分别与哌啶、3-甲基哌啶和 4-甲基哌啶反应合成了 2-N-哌啶基吡嗪、2-N-（3-甲基）哌啶基吡嗪和 2-N-（4-甲基）哌啶基吡嗪。通过光谱方法确认了这些化合物的结构。在四氢呋喃、乙腈、乙酸乙酯和乙醇中进行了荧光研究。在四氢呋喃中，2-N-哌啶基吡嗪的荧光强度最高，其次是 2-N-4-甲基哌啶基吡嗪。荧光强度随着溶剂极性的增加而降低。

  DOI：

  10.14233/ajchem.2013.15201

文献信息

• Direct Uncatalyzed Amination of 2-Chloropyridine Using a Flow Reactor
  作者：Bruce Hamper、Eden Tesfu

  DOI：10.1055/s-2007-985574

  日期：——

  Chloropyridines are efficiently converted into 2-amino­pyridines by uncatalyzed nucleophilic aromatic substitution (SNAr) in NMP using a continuous-flow reactor. A variety of secondary amines undergo SNAr with both electron-rich and electron-deficient 2-chloropyridines to afford 2-aminopyridines in good to excellent yield. The flow reactor, which provides a short reaction time and high temperatures up to 300 °C, can overcome the activation barrier for reactions with unactivated substrates. Short reaction times result in fewer side products and can afford milligram to multigram ­quantities of product using continuous flow.

  氯代吡啶在无催化剂的亲核芳香取代（SNAr）作用下，通过连续流动反应器在NMP中高效转化为2-氨基吡啶。多种仲胺能够与电子丰富和电子缺乏的2-氯代吡啶进行SNAr反应，以良好至优异的产率得到2-氨基吡啶。这种连续流动反应器提供了短暂的反应时间和高达300°C的高温，能够克服非活化底物反应的活化能障碍。短暂的反应时间导致副产品较少，并且使用连续流动的方式可以在毫克至多克的量级上得到产物。
• Modulators of muscarinic receptors
  申请人：Makings R. Lewis

  公开号：US20080015179A1

  公开（公告）日：2008-01-17

  The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.

  本发明涉及肌胆碱受体调节剂。本发明还提供包含这种调节剂的组合物，并提供了用于治疗肌胆碱受体介导疾病的方法。
• Carboxyesterase polypeptides for amide coupling
  申请人：Codexis, Inc.

  公开号：US11015180B2

  公开（公告）日：2021-05-25

  The present invention provides engineered carboxyesterase enzymes having improved properties as compared to a naturally occurring wild-type carboxyesterase enzymes, as well as polynucleotides encoding the engineered carboxyesterase enzymes, host cells capable of expressing the engineered carboxyesterase enzymes, and methods of using the engineered carboxyesterase enzymes in amidation reactions.

  本发明提供了经过改良的羧酯酶酶，其性能优于天然存在的野生型羧酯酶酶，以及编码这些经过改良的羧酯酶酶的多核苷酸序列，能够表达这些经过改良的羧酯酶酶的宿主细胞，以及在酰胺化反应中使用这些经过改良的羧酯酶酶的方法。
• Fused Triazole Tachykinin Receptor Antagonists
  申请人：DeVita Robert J.

  公开号：US20090221611A1

  公开（公告）日：2009-09-03

  The present invention is directed to certain fused triazole compounds which are useful as neurokinin-1 (NK-I) receptor antagonists, and inhibitors of tachykinin and in particular substance P- The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

  本发明涉及某些融合的三唑化合物，它们可用作神经激肽-1（NK-I）受体拮抗剂和快速激肽，特别是物质P的抑制剂。本发明还涉及包含这些化合物作为活性成分的制药配方以及这些化合物及其配方在治疗某些疾病，包括呕吐、尿失禁、抑郁症和焦虑症方面的用途。
• Piperidinyl Piperidine Tachykinin Receptor Antagonists
  申请人：Devita Robert J.

  公开号：US20080146588A1

  公开（公告）日：2008-06-19

  The present invention is directed to certain piperidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

  本发明涉及某些哌啶化合物，其可用作神经激肽1（NK-1）受体拮抗剂，并且是缓激肽，特别是物质P的抑制剂。本发明还涉及包含这些化合物作为活性成分的制药配方以及利用这些化合物及其配方治疗某些疾病，包括呕吐、尿失禁、抑郁症和焦虑症。