3-(3-Pyridyl)-2-aminopyridine | 163563-02-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-(3-Pyridyl)-2-aminopyridine
• 英文别名: [3,3']-bipyridinyl-2-ylamine；[3,3'-Bipyridin]-2-amine；3-pyridin-3-ylpyridin-2-amine
• CAS: 163563-02-8
• 化学式: C₁₀H₉N₃
• 分子量: 171.202
• InChiKey: ZKDRHGPINCUARO-UHFFFAOYSA-N

物化性质

• 熔点：
  89-91 °C(Solv: ethyl acetate (141-78-6))
• 沸点：
  346.5±27.0 °C(Predicted)
• 密度：
  1.193±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  51.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(3-Pyridyl)-2-aminopyridine 在 溴化氰 、 水 、 氯化铵 作用下， 以 乙醇 为溶剂， 反应 2.33h， 以87%的产率得到(E)-3-(1H-pyrrolo[2,3-b]pyridin-3-yl)-propenal
  参考文献：
  名称：

  通过吡啶鎓盐的开环合成氮杂环。

  摘要：

  DOI：

  10.1002/anie.200602996
• 作为产物：
  描述：

  (E,Z)-α-<3-(Dimethylamino)-2-propenylidene>-3-pyridineacetonitrile 在 氨 作用下， 以 甲醇 为溶剂， 反应 100.0h， 以93%的产率得到3-(3-Pyridyl)-2-aminopyridine
  参考文献：
  名称：

  New Synthetic Routes to 3-, 5-, and 6-Aryl-2-chloropyridines

  摘要：

  The efficient synthesis of 3-, 5-, and 6-aryl-2-chloropyridines via the facile preparation of 5-(dimethyamino)aryl-substituted pentadienyl nitriles and cyclization with hydro chloric acid is described. This approach allows for the introduction of other electron-withdrawing substituents on the pyridine ring as well as the preparation of the desired unsubstituted arylpyridines. Some differences in the rates of cyclization of the pentadienyl nitriles as well as the yields of chloropyridines were observed that depended on the position and degree of substitution in the aryl substituent. The arylpentadienyl nitriles 5 and 6 could also be converted directly into the corresponding 2-aminopyridines.

  DOI：

  10.1021/jo00117a029

文献信息

• [EN] ANTI-MALARIAL AGENTS<br/>[FR] AGENTS ANTIPALUDIQUES
  申请人：UNIV TEXAS

  公开号：WO2021123266A1

  公开（公告）日：2021-06-24

  The present invention is related to new pyrrole derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to pyrrole derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.

  本发明涉及新吡咯衍生物在制造用于预防或治疗疟疾的药物方面的应用。具体而言，本发明涉及对用于制备用于抑制疟疾寄生虫增殖的药物配方的吡咯衍生物的应用。
• PANTOTHENAMIDE ANALOGUES
  申请人：MMV Medicines for Malaria Venture

  公开号：EP3674288A1

  公开（公告）日：2020-07-01

  The present invention provides compounds that have antimalarial activity. More in particular, the present invention provides novel compounds that are analogues of pantothenamides. The pantothenamide analogues of this invention have particularly low IC50 values against the asexual blood stages and gametocytes of malaria parasites. Furthermore, the pantothenamide analogues of this invention are characterized by low hepatic metabolism. Therefore, pantothenamide analogues of the invention are particularly suitable for use in therapeutic and/or prophylactic treatment of protozoan infections in a human or animal subject in need thereof. The invention further provides pharmaceutical formulations comprising the pantothenamide analogues as well as the therapeutic and/or prophylactic uses of the pantothenamide analogues and pharmaceutical formulations comprising them.

  本发明提供具有抗疟疾活性的化合物。更具体地说，本发明提供了类泛酰胺的新化合物。本发明的泛酰胺类似物对疟疾寄生虫的无性血液阶段和配子体具有特别低的IC50值。此外，本发明的泛酰胺类似物具有低肝代谢特性。因此，本发明的泛酰胺类似物特别适用于用于治疗和/或预防人类或动物主体中原虫感染。本发明还提供包含泛酰胺类似物的药物配方，以及泛酰胺类似物的治疗和/或预防用途以及包含它们的药物配方。
• Preparation and use of combustion derived Bi2O3 for the generation of novel heterocycles via Suzuki-Coupling Reactions: potential application as anti-cancer agents
  作者：Anusha Sebastian、Anandakumar B Siddappa、Chakrabhavi Dhananjaya Mohan、Nagabhushana G T、PRIYA BABU SHUBHA、Kanchugarakoppal S Rangappa、Salundi Basappa、Chandrappa G T

  DOI：10.1039/c4ra07839j

  日期：——

  Bismuth oxide was synthesized via simple, rapid and energy efficient solution combustion synthesis (SCS) by employing sucrose as a fuel. This SCS-Bi2O3 was characterized by analytical techniques such as PXRD, SEM, EDX, UV-Visible and BET surface area measurement. Using the prepared SCS-Bi2O3, several classes of heterocyclic compounds were synthesized in good yields via Suzuki-coupling reaction in aqueous medium. Interestingly, the recovered SCS-Bi2O3 could be reused three times without a significant loss of catalytic activity. Further, the synthesized compounds were tested for cytotoxic activity against a human hepatoma cancer cell line (HepG2). Among these, compound 3n effectively inhibited the proliferation of these cells with an IC50 value of 8.4 μM. Thus, this paper describes the preparation of highly effective Bi2O3, which can be used for synthesizing various classes of heterocycles, including those having anti-cancer property.

  铋氧化物通过简单、快速且能源高效的溶液燃烧合成（SCS）法合成，采用蔗糖作为燃料。所得到的SCS-Bi2O3通过PXRD、SEM、EDX、UV-可见光谱以及BET比表面积测量等分析技术进行了表征。利用制备的SCS-Bi2O3，通过在水相体系中进行铃木偶联反应合成了几类的杂环化合物，并且产率良好。有趣的是，回收的SCS-Bi2O3在没有显著失去催化活性的情况下可以重复使用三次。此外，合成的化合物还针对人肝癌细胞系（HepG2）进行了细胞毒性活性测试。其中，化合物3n有效抑制了这些细胞的增殖，IC50值为8.4 μM。因此，本文描述了高效的Bi2O3的制备，这可以用于合成包括具有抗癌特性的多种杂环化合物。
• NEW SUBSTITUTED TRIAZOLOPYRIMIDINES AS ANTI-MALARIAL AGENTS
  申请人：Board Of Regents Of the University Of Texas System

  公开号：EP3072894A1

  公开（公告）日：2016-09-28

  The present invention is related to a use of triazolopyrimidine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to triazolopyrimidine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.

  本发明涉及三唑吡咯嘧啶衍生物在制造用于预防或治疗疟疾的药物方面的用途。具体而言，本发明涉及三唑吡咯嘧啶衍生物，用于制备用于抑制疟原虫增殖的药物配方。
• NEW ANTI-MALARIAL AGENTS
  申请人：MMV Medicines for Malaria Venture

  公开号：EP3309156A1

  公开（公告）日：2018-04-18

  The present invention is related to new trioxolane derivatives of formula (I) in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to trioxolane derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.

  本发明涉及公式（I）的新三氧杂环戊烷衍生物在制备用于预防或治疗疟疾的药物方面的应用。具体而言，本发明涉及对用于制备药物配方以抑制疟疾寄生虫增殖的三氧杂环戊烷衍生物的应用。