5-乙氧基-2-氨基吡啶 | 89943-11-3

• 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
• 中文名称: 5-乙氧基-2-氨基吡啶
• 英文名称: 5-ethoxypyridin-2-amine
• 英文别名: 2-amino-5-ethoxypyridine
• CAS: 89943-11-3
• 化学式: C₇H₁₀N₂O
• 分子量: 138.169
• InChiKey: WCKZZIDVKJIEAP-UHFFFAOYSA-N

物化性质

• 熔点：
  86 °C
• 沸点：
  264.4±20.0 °C(Predicted)
• 密度：
  1.101±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  48.1
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2933399090
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  5-乙氧基-2-氨基吡啶 在 palladium on activated charcoal 、 氢气 作用下， 以 乙酸乙酯 为溶剂， 反应 21.0h， 生成 3-(5-Ethoxypyridin-2-yl)imidazo[4,5-b]pyridin-6-amine
  参考文献：
  名称：

  Discovery and optimization of potent broad-spectrum arenavirus inhibitors derived from benzimidazole and related heterocycles

  摘要：

  A series of potent arenavirus inhibitors sharing a benzimidazole core were previously reported by our group. SAR studies were expanded beyond the previous analysis, which involved the attached phenyl rings and methylamino linker portion, to include modifications focused on the benzimidazole core. These changes included the introduction of various substituents to the bicyclic benzimidazole ring system along with alternate core heterocycles. Many of the analogs containing alternate nitrogen-based bicyclic ring systems were found to retain antiviral potency compared to the benzimidazole series from which we derived our lead compound, ST-193. In fact, 21h, built on an imidazopyridine core, possessed a near tenfold increase in potency against Lassa virus pseudotypes compared to ST-193. As found with the benzimidazole series, broad-spectrum arenavirus activity was also observed for a number of the analogs discovered during this study. (c) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.11.093
• 作为产物：
  描述：

  3-乙氧基吡啶 在 sodium hydroxide 、 palladium on activated charcoal 、 硫酸 、 水 、 氢溴酸 、 硝酸 、 溶剂黄146 作用下， 生成 5-乙氧基-2-氨基吡啶
  参考文献：
  名称：

  den Hertog et al., Recueil des Travaux Chimiques des Pays-Bas, 1949, vol. 68, p. 275,282

  摘要：

  DOI：

文献信息

• Copper(I)-Catalyzed Amination of Aryl Halides in Liquid Ammonia
  作者：Pengju Ji、John H. Atherton、Michael I. Page

  DOI：10.1021/jo301204t

  日期：2012.9.7

  of amination of iodobenzene in liquid ammonia is first order in copper(I) catalyst concentration. The small Hammett ρ = 0.49 for the amination of 4-substituted iodobenzenes in liquid ammonia at 25 °C indicates that the C–I bond is not significantly broken in the transition state structure and that there is a small generation of negative charge in the aryl ring, which is compatible with the oxidative

  液态氨（LNH 3）由铜（I）盐/抗坏血酸体系催化生成伯芳族胺，收率好至极好。所需的低浓度催化剂和易于分离的产品表明该方法具有潜在的工业应用价值。通常用于类似金属催化反应的配体是无效的。液态氨中碘苯的胺化速率是铜（I）催化剂浓度的一级。在25°C的氨水中4-取代的碘苯胺的胺化反应中小的Hammettρ= 0.49表明，C–I键在过渡态结构中没有明显断裂，并且在芳基中有一小段负电荷产生环，其与限速的铜离子的氧化加成相容。
• Positive allosteric modulators of the nicotinic acetylcholine receptor
  申请人：——

  公开号：US20030236287A1

  公开（公告）日：2003-12-25

  The invention provides compounds of Formula I: 1 These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which &agr;7 nAChR is known to be involved.

  这项发明提供了I式化合物： 这些化合物可以是药用盐或组合物的形式，可以是纯对映体形式或混合物，对治疗已知涉及α7 nAChR的疾病或症状的药物非常有用。
• Heterocyclic compounds as ligands of the GABAA receptor
  申请人：——

  公开号：US20030105081A1

  公开（公告）日：2003-06-05

  Disclosed are heterocyclic compounds of the formula 1 and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABA A brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA A brain receptor.

  揭示了具有以下公式的杂环化合物及其药用可接受的盐，其中变量A、V、Y、J、E、X、T、G、Q、W、Z、b、n和m在此处被定义。这些化合物是GABA A 脑受体的高度选择性激动剂、拮抗剂或逆激动剂，或者是GABA A 脑受体的激动剂、拮抗剂或逆激动剂的前药。
• Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives
  作者：A. V. Semenov、I. V. Tarasova、V. S. Khramov、E. V. Semenova、V. I. Inchina、S. S. Vakaeva

  DOI：10.1007/s11094-018-1792-7

  日期：2018.6

  A series of previously undescribed N-aryl-N′-pyridin-2-ylureas were prepared via the reaction of 2-aminopyridines with benzoyl azides and tested in vitro as activators of glucokinase. Statistically significant reductions of glucose levels as compared with controls were demonstrated for several compounds.

  一系列之前未描述的 N-芳基-N'-吡啶-2-基脲通过 2-氨基吡啶与苯甲酰叠氮化物的反应制备而成，并在体外测试其作为葡萄糖激酶激活剂的活性。与对照组相比，几个化合物显示出统计学上显著的葡萄糖水平降低。
• [EN] PIPERIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF METABOLIC DISORDERS<br/>[FR] DÉRIVÉS DE PIPÉRIDINE ET LEUR UTILISATION POUR LE TRAITEMENT DE TROUBLES MÉTABOLIQUES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2012001107A1

  公开（公告）日：2012-01-05

  The invention relates to new piperidine derivatives of the formula (I) to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

  本发明涉及一种新的哌啶衍生物，其化学式为（I），以及它们作为药物的用途，它们的治疗用途的方法以及包含它们的制药组合物。