5,6,7,8-四氢喹啉-4-胺 | 14807-39-7

• 物质功能分类: 医药中间体 - 杂环化合物 - 喹啉类化合物
• 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
• 中文名称: 5,6,7,8-四氢喹啉-4-胺
• 英文名称: 5,6,7,8-tetrahydroquinolin-4-amine
• CAS: 14807-39-7
• 化学式: C₉H₁₂N₂
• mdl: MFCD18909186
• 分子量: 148.208
• InChiKey: CZVFSRODUXQSSX-UHFFFAOYSA-N

物化性质

• 熔点：
  133 °C(Solv: benzene (71-43-2))
• 沸点：
  325.9±42.0 °C(Predicted)
• 密度：
  1.124±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.444
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5,6,7,8-四氢喹啉-4-胺 在 sodium hypophosphite 、 sodium nitrite 作用下， 生成 5,6,7,8-四氢喹啉-4-醇
  参考文献：
  名称：

  Ishii, Yakugaku Zasshi/Journal of the Pharmaceutical Society of Japan, 1952, vol. 72, p. 1317,1320

  摘要：

  DOI：
• 作为产物：
  描述：

  4-氨基-7-氯喹啉 在 盐酸 、 platinum(IV) oxide 、 高氯酸 、 氢气 作用下， 以 水 、 溶剂黄146 为溶剂， 20.0~70.0 ℃ 、344.75 kPa 条件下， 反应 69.0h， 生成 5,6,7,8-四氢喹啉-4-胺
  参考文献：
  名称：

  Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice

  摘要：

  In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50 < 1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50 < 1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.

  DOI：

  10.1021/acsmedchemlett.8b00053

文献信息

• [EN] INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53<br/>[FR] INHIBITEURS DE L'INTERACTION ENTRE MDM2 ET P53
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2006032631A1

  公开（公告）日：2006-03-30

  The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.

  本发明提供了式（I）的化合物，其用作p53-MDM2相互作用的抑制剂，以及包含所述式（I）的化合物的药物组合物，其中n、m、p、s、t、R1、R2、R3、R4、R5、R6、R7、X、Y、Q和Z具有定义的含义。
• A Strategy to Aminate Pyridines, Diazines, and Pharmaceuticals via Heterocyclic Phosphonium Salts
  作者：Chirag Patel、Margaret Mohnike、Michael C. Hilton、Andrew McNally

  DOI：10.1021/acs.orglett.8b00813

  日期：2018.5.4

  A straightforward process to aminate pyridines and diazines is presented by reacting phosphonium salt derivatives with sodium azide. The iminophosphorane products are versatile precursors to several nitrogen-containing functional groups, and the process can be applied to building block heterocycles, to drug-like fragments, and for late-stage functionalization of complex pharmaceuticals. Appealing features

  通过使鏻盐衍生物与叠氮化钠反应，提出了一种胺化吡啶和二嗪的简单方法。亚氨基正膦产品是多种含氮官能团的多功能前体，该工艺可应用于构建杂环、类药物片段以及复杂药物的后期功能化。该策略的吸引人的特点包括使用 C-H 键作为前体、精确的区域选择性以及与其他胺化方法（特别是依赖于卤化氮杂芳烃的胺化方法）不同的范围。
• HETEROARYL COMPOUNDS COMPRISING NITROGEN AND USE THEREOF
  申请人：ImmunoMet Therapeutics, Inc

  公开号：US20170305861A1

  公开（公告）日：2017-10-26

  The present invention relates to heteroaryl compounds comprising nitrogen and use thereof, and more specifically to compounds which exhibit a remarkable effect on inhibiting proliferation of cancer cells and metastasis and recurrence of cancer, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compounds according to the present invention exhibit a remarkable effect on inhibiting proliferation of cancer cells and metastasis and recurrence of cancer with a reduced dose compared to that of existing drugs. Accordingly, the compounds can be effectively used for treating various types of cancer, such as uterine cancer, breast cancer, gastric cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, pancreatic cancer, renal cancer, prostate cancer, bladder cancer, and liver cancer, and for inhibiting proliferation of cancer cells and metastasis of cancer.

  本发明涉及含氮的杂环化合物及其使用，更具体地涉及对抑制癌细胞增殖、转移和复发具有显著作用的化合物、其制备方法以及包含其作为活性成分的药物组合物。与现有药物相比，本发明的化合物在减少剂量的情况下具有显著的抑制癌细胞增殖、转移和复发的作用。因此，这些化合物可以有效地用于治疗各种类型的癌症，如子宫癌、乳腺癌、胃癌、脑癌、直肠癌、结直肠癌、肺癌、皮肤癌、血液癌、胰腺癌、肾癌、前列腺癌、膀胱癌和肝癌，并用于抑制癌细胞的增殖和癌症的转移。
• [EN] BET BROMODOMAIN INHIBITORS AND THERAPEUTIC METHODS USING THE SAME<br/>[FR] INHIBITEURS DE BROMODOMAINES BET ET MÉTHODES THÉRAPEUTIQUES LES UTILISANT
  申请人：UNIV MICHIGAN

  公开号：WO2014164596A1

  公开（公告）日：2014-10-09

  Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

  本文披露了BET bromodomain抑制剂及含有它们的组合物。还披露了使用BET bromodomain抑制剂治疗疾病和状况的方法，其中BET bromodomain的抑制提供益处，如癌症等疾病。
• 1,2,3,4-tetrahydroisoquinolines derivatives
  申请人：——

  公开号：US20040242564A1

  公开（公告）日：2004-12-02

  The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists.

  本发明涉及新型1,2,3,4-四氢异喹啉衍生物及相关化合物，以及它们作为制备药物组成部分的活性成分的用途。本发明还涉及相关方面，包括制备化合物的过程，含有其中一种或多种化合物的药物组成物，特别是它们作为神经荷尔蒙拮抗剂的用途。