N'-(1,4-dihydropyrazin-2-yl)-N-oxomethanimidamide | 51519-20-1

• 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'-(1,4-dihydropyrazin-2-yl)-N-oxomethanimidamide
• 英文别名: N-Pyrazinylformamide Oxime；N'-hydroxy-N-(pyrazin-2-yl)formimidamide；N-hydroxy-N'-pyrazin-2-yl-formamidine；N-pyrazin-2-yl-formamide oxime
• CAS: 51519-20-1
• 化学式: C₅H₆N₄O
• mdl: MFCD19236774
• 分子量: 138.13
• InChiKey: LYTCTZSLBVYHRA-UHFFFAOYSA-N

物化性质

• 熔点：
  195-200 °C(Solv: ethanol (64-17-5))
• 沸点：
  325.6±45.0 °C(Predicted)
• 密度：
  1.37±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  70.4
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• SUBSTITUTED SULFONAMIDE COMPOUNDS
  申请人：OBERBOERSCH Stefan

  公开号：US20080153843A1

  公开（公告）日：2008-06-26

  Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.

  磺胺取代物，其制备方法，含有这些化合物的药物组合物，以及磺胺取代物在治疗或抑制疼痛和/或各种疾病或疾病状态中的用途。
• [EN] SUBSTITUTED SULFONAMIDE DERIVATIVES<br/>[FR] DÉRIVÉS DE SULFONAMIDES SUBSTITUÉS
  申请人：GRUENENTHAL GMBH

  公开号：WO2009090055A1

  公开（公告）日：2009-07-23

  The invention relates to substituted sulfonamide derivatives of the general formula (I'); processes for their preparation, medicaments containing these compounds, and the use of substituted sulfonamide derivatives for the preparation of medicaments

  该发明涉及一般式（I'）的取代磺胺基衍生物，其制备方法，含有这些化合物的药物，以及用于制备药物的取代磺胺基衍生物的用途
• [EN] AMINOCYCLOHEXANES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES<br/>[FR] AMINOCYCLOHEXANES EN TANT QU'INHIBITEURS DE DIPEPTIDYL PEPTIDASE-IV POUR LE TRAITEMENT OU LA PRÉVENTION DE DIABÈTES
  申请人：MERCK & CO INC

  公开号：WO2006009886A1

  公开（公告）日：2006-01-26

  The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DPP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

  本发明涉及一种新型的取代氨基环己烷，它们是二肽基肽酶-IV酶（'DPP-IV抑制剂'）的抑制剂，并且在治疗或预防涉及二肽基肽酶-IV酶的疾病中具有用处，如糖尿病，特别是2型糖尿病。该发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及二肽基肽酶-IV酶的这类疾病中使用这些化合物和组合物。
• CXCR7 ANTAGONISTS
  申请人：ChemoCentryx, Inc.

  公开号：US20140154179A1

  公开（公告）日：2014-06-05

  Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.

  提供具有化学式I的化合物，或其药用可接受的盐、水合物或N-氧化物，并且这些化合物可用于与CXCR7结合，治疗部分或完全依赖于CXCR7活性的疾病。因此，根据本发明的进一步方面，提供含有上述化合物之一或多个的组合物与药用可接受的赋形剂混合物。
• T3P-Mediated N–N Cyclization for the Synthesis of 1,2,4-Triazolo[1,5-<i>a</i>]pyridines
  作者：Rajaram Ayothiraman、Durgarao Bandaru、Ranjitha Paranthaman、Michaël Fenster、Martin D. Eastgate、Rajappa Vaidyanathan

  DOI：10.1021/acs.oprd.9b00396

  日期：2019.11.15

  Propylphosphonic anhydride has been shown to be an effective reagent for the synthesis of substituted [1,2,4]triazolo[1,5-a]pyridines from the corresponding N′-hydroxy-N-formimidamides. The reactions worked under mild conditions and exhibited wide functional group tolerance, delivering the triazolopyridines in good to excellent yields and purities.

  丙基膦酸酐已被证明是从相应的N'-羟基-N-甲酰胺基化合物合成取代的[1,2,4]三唑并[1,5- a ]吡啶的有效试剂。反应在温和的条件下进行，并表现出宽泛的官能团耐受性，从而以优异的产率和纯度提供了三唑并吡啶。