(N-penta-1,5-diyl-carboxamido)-pyrazine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: (N-penta-1,5-diyl-carboxamido)-pyrazine
• 英文别名: 1-pyrazinecarbonyl-piperidine；1-Pyrazincarbonyl-piperidin；Piperidyl pyrazin-2-yl ketone；piperidin-1-yl(pyrazin-2-yl)methanone
• 化学式: C₁₀H₁₃N₃O
• mdl: MFCD00456750
• 分子量: 191.233
• InChiKey: FKTMADJJKGNCPV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 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：
  46.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  哌啶 、 2-氯吡嗪 、 一氧化碳 在 2,2,6,6-四甲基哌啶 、 dicobalt octacarbonyl 作用下， 以 2-甲基-2-丁醇 为溶剂， 反应 48.0h， 以59%的产率得到(N-penta-1,5-diyl-carboxamido)-pyrazine
  参考文献：
  名称：

  可见光促进钴催化的（杂）芳基卤化物的氨基羰基化

  摘要：

  （杂）芳基卤化物的催化氨基羰基化广泛应用于酰胺的合成，但在很大程度上依赖于贵金属催化的使用。在此，我们报道了在可见光照射下使用简单的钴催化剂对（杂）芳基卤化物进行氨基羰基化。该反应扩展到（杂）芳基氯化物的使用，并在广泛的胺亲核试剂上取得了成功。机理研究与通过分子间电荷转移进行的反应一致，该反应涉及底物和钴酸盐催化剂的供体-受体配合物。

  DOI：

  10.1039/d0sc02178d

文献信息

• Homogeneous catalytic aminocarbonylation of nitrogen-containing iodo-heteroaromatics. Synthesis of N-substituted nicotinamide related compounds
  作者：Attila Takács、Balázs Jakab、Andrea Petz、László Kollár

  DOI：10.1016/j.tet.2007.07.017

  日期：2007.10

  Various primary and secondary amines, including amino acid methyl esters, were used as nucleophiles in palladium-catalysed aminocarbonylation of 2-iodopyridine, 3-iodopyridine and iodopyrazine. N-Substituted nicotinamides and 3-pyridyl-glyoxylamides (2-oxo-carboxamide type derivatives) of potential biological importance can be obtained from 3-iodopyridine as a result of simple and double carbon monoxide

  各种伯胺和仲胺，包括氨基酸甲酯，在钯催化的2-碘吡啶，3-碘吡啶和碘吡嗪的氨基羰基化反应中用作亲核试剂。具有潜在生物学重要性的N-取代的烟酰胺和3-吡啶基-乙二酰乙酰胺（2-氧代-羧酰胺型衍生物）可以分别通过简单和两次一氧化碳插入而从3-碘吡啶获得。后面的例子可以通过使用升高的一氧化碳压力以合成上可接受的产率获得。相反，仅通过使用2-碘吡啶和碘吡嗪在整个压力范围内获得N-烷基/芳基-甲酰胺。
• Compositions For Treating Flushing And Lipid-Associated Disorders Comprising Niacin Receptor Partial Agonists
  申请人：Behan Dominic P.

  公开号：US20080139628A1

  公开（公告）日：2008-06-12

  The invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist. In addition, the invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist and an effective lipid altering amount of niacin or a niacin analog. The invention further provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist and subsequently administering to said subject an effective lipid altering amount of niacin or a niacin analog.

  本发明提供了一种减少烟酸或烟酸类似物引起的面红的方法，包括向该受体中注射有效减少面红量的烟酸受体部分激动剂。此外，本发明还提供了一种减少烟酸或烟酸类似物引起的面红的方法，包括向该受体中注射有效减少面红量的烟酸受体部分激动剂和有效改变脂质含量的烟酸或烟酸类似物。本发明进一步提供了一种减少烟酸或烟酸类似物引起的面红的方法，包括向该受体中注射有效减少面红量的烟酸受体部分激动剂，然后向该受体中注射有效改变脂质含量的烟酸或烟酸类似物。
• Human G Protein-Coupled Receptors and Modulators Thereof for the Treatment of Metabolic-Related Disorders
  申请人：Unett David J.

  公开号：US20110177612A1

  公开（公告）日：2011-07-21

  The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
• Cobalt-catalyzed aminocarbonylation of (hetero)aryl halides promoted by visible light
  作者：Alexander M. Veatch、Erik J. Alexanian

  DOI：10.1039/d0sc02178d

  日期：——

  aminocarbonylation of (hetero)aryl halides is widely applied in the synthesis of amides but relies heavily on the use of precious metal catalysis. Herein, we report an aminocarbonylation of (hetero)aryl halides using a simple cobalt catalyst under visible light irradiation. The reaction extends to the use of (hetero)aryl chlorides and is successful with a broad range of amine nucleophiles. Mechanistic investigations

  （杂）芳基卤化物的催化氨基羰基化广泛应用于酰胺的合成，但在很大程度上依赖于贵金属催化的使用。在此，我们报道了在可见光照射下使用简单的钴催化剂对（杂）芳基卤化物进行氨基羰基化。该反应扩展到（杂）芳基氯化物的使用，并在广泛的胺亲核试剂上取得了成功。机理研究与通过分子间电荷转移进行的反应一致，该反应涉及底物和钴酸盐催化剂的供体-受体配合物。