N-ethylquinolin-2-amine | 52430-55-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N-ethylquinolin-2-amine
• 英文别名: 2-ethylaminoquinoline
• CAS: 52430-55-4
• 化学式: C₁₁H₁₂N₂
• mdl: MFCD11124101
• 分子量: 172.23
• InChiKey: GVBLKFLAWLSBBF-UHFFFAOYSA-N

物化性质

• 沸点：
  315.7±15.0 °C(Predicted)
• 密度：
  1.127±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.181
• 拓扑面积：
  24.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  苯乙烯 、 N-ethylquinolin-2-amine 在 bis(1,5-cyclooctadiene)iridium(I) tetrafluoroborate 、 (±)-2,2 '-二(二-对甲苯基膦)-1,1 '-联萘 作用下， 以 乙二醇二甲醚 为溶剂， 反应 24.0h， 以72%的产率得到(+)-N-(4-phenylbutan-2-yl)quinolin-2-amine
  参考文献：
  名称：

  阳离子铱催化与氮原子相邻的次级sp 3 C–H键的对映选择性活化

  摘要：

  阳离子Ir（I）–tolBINAP复合物催化对映选择性C–C键的形成，这是由邻近氮原子的次级sp 3 C–H键断裂引发的。各种2-（烷基氨基）吡啶和烯烃被选择性地转化为具有中等至几乎完美对映体过量的手性胺。还研究了炔烃作为偶联伙伴。研究了烷基结构对底物和导向基团的影响。该转变代表了亚甲基高度对映选择性的C–H键活化的第一个例子，而不是在烯丙基或苄基位置。

  DOI：

  10.1016/j.tet.2012.08.071
• 作为产物：
  描述：

  2-氨基喹啉 、 triethyl((3-ethylpent-3-yl)peroxy)silane 在 copper(l) iodide 、 4,7-二甲氧基-1,10-菲咯啉 作用下， 以 苯 为溶剂， 反应 6.0h， 以68%的产率得到N-ethylquinolin-2-amine
  参考文献：
  名称：

  烷基甲硅烷基过氧化物作为伯酰胺和芳胺在铜催化的选择性单-N-烷基化中的烷基化剂

  摘要：

  报道了使用烷基甲硅烷基过氧化物作为烷基化剂的伯酰胺或芳基胺的铜催化的选择性单-N-烷基化。该反应在温和的反应条件下进行，并且相对于烷基甲硅烷基过氧化物以及伯酰胺和芳基胺表现出广泛的底物范围。机理研究表明，本反应应通过自由基过程进行，该自由基过程包括由烷基甲硅烷基过氧化物产生的烷基。

  DOI：

  10.1002/chem.201702217

文献信息

• Benzenesulfonyl-ureas
  申请人：Hoechst Aktiengesellschaft

  公开号：US04025519A1

  公开（公告）日：1977-05-24

  Sulfonyl-ureas of the formula ##STR1## wherein X represents a heteroaromatic 5- or 6-ring substituted, if desired, by one or two methyl groups and/or annellated with benzene, which ring may contain in addition to a nitrogen atom a further nitrogen, oxygen or sulfur atom and which, in vicinal position to the nitrogen atom, is linked to the rest of the molecule portion, R is alkyl having 1 to 3 carbon atoms, R.sup.1 is alkyl having 3 to 6 carbon atoms, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkenyl, alkylcycloalkenyl having each 5 to 9 carbon atoms, cyclohexenylmethyl, chlorocyclohexyl, bicycloheptenylmethyl, bicycloheptylmethyl, bicycloheptenyl, bicycloheptyl, nortricyclyl, adamantyl, benzyl, which as substance or in form of the salts thereof have hypoglycemic properties and are distinguished by a strong and continuous lowering of the blood sugar level, process for preparing them as well as pharmaceutical preparations containing the sulfonyl-ureas as an active substance.

  磺酰脲的化学式为##STR1##，其中X代表一个杂芳环，该环可以是5-或6-环，如果需要，可以被一个或两个甲基基团取代，并/或与苯环相连，该环除了含有一个氮原子外，还可以含有另一个氮、氧或硫原子，并且在与氮原子相邻的位置上与分子其余部分相连，R是具有1至3个碳原子的烷基，R.sup.1是具有3至6个碳原子的烷基，环烷基，烷基环烷基，环烷基烷基，环烯基，具有5至9个碳原子的烷基环烯基，环己烯基甲基，氯代环己基，双环庚烯基甲基，双环庚基甲基，双环庚烯基，双环庚基，诺三环基，莰基，苄基，这些物质或其盐具有降糖作用，并以强烈和持续降低血糖水平而著称，制备它们的方法以及含有磺酰脲作为活性物质的药物制剂。
• [EN] PHARMACEUTICAL USE OF SUBSTITUTED 1,2,4-TRIAZOLES<br/>[FR] UTILISATION PHARMACEUTIQUE DE 1,2,4-TRIAZOLES SUBSTITUEES
  申请人：NOVO NORDISK AS

  公开号：WO2004089367A1

  公开（公告）日：2004-10-21

  The use of substituted 1,2,4-triazoles for modulating the activity of 11 β-hydroxysteroid dehydrogenase type 1 (11 βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of substituted 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11 βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

  已描述了使用取代的1,2,4-三唑来调节11β-羟基甾醇脱氢酶1（11βHSD1）活性以及将这些化合物用作药物组合物的用途。还描述了一类新型的取代的1,2,4-三唑，它们在治疗中的用途，包含这些化合物的药物组合物，以及它们在制造药物中的用途。这些化合物是11βHSD1活性的调节剂，更具体地是抑制剂，并且可能在治疗、预防和/或预防一系列需要降低细胞内活性糖皮质激素浓度的医学疾病中有用。
• Pharmaceutical use of substituted 1,2,4-triazoles
  申请人：Andersen Sune Henrik

  公开号：US20060100235A1

  公开（公告）日：2006-05-11

  The use of substituted 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of substituted 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

  使用替代1,2,4-三唑来调节11β-羟基类固醇脱氢酶1型（11βHSD1）的活性，并将这些化合物用作制药组合物已被描述。还描述了一种新的替代1,2,4-三唑类，它们在治疗中的用途，包含这些化合物的制药组合物，以及它们在制药中的用途。这些化合物是11βHSD1活性的调节剂，更具体地是抑制剂，可能在治疗、预防和/或预防一系列医学疾病中有用，其中降低细胞内活性糖皮质激素的浓度是可取的。
• Pharmaceutical use of substituted amides
  申请人：Andersen Sune Henrik

  公开号：US20060111366A1

  公开（公告）日：2006-05-25

  The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

  本文介绍了使用取代酰胺来调节11β-羟化甾体脱氢酶1型（11βHSD1）的活性以及将这些化合物用作制药组合物的方法。还介绍了一类新型的取代酰胺，它们在治疗中的应用、包含这些化合物的制药组合物以及它们在药物制剂制造中的应用。这些化合物是11βHSD1的调节剂，更具体地说是抑制剂，可用于治疗、预防和/或预防一系列需要降低活性糖皮质激素细胞内浓度的医学疾病。
• Amide Derivatives and Pharmaceutical Use Thereof
  申请人：Andersen Henrik Sune

  公开号：US20090264414A1

  公开（公告）日：2009-10-22

  The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

  本文描述了使用取代酰胺来调节11β-羟化类固醇脱氢酶1型（11βHSD1）活性以及这些化合物作为药物组分的用途。还描述了一类新型的取代酰胺，它们在治疗中的用途，包括含有这些化合物的药物组分以及它们在制造药物中的用途。这些化合物是调节剂，更具体地说是11βHSD1活性的抑制剂，可用于治疗、预防和/或预防一系列医学疾病，其中降低细胞内活性糖皮质激素的浓度是可取的。