4-氯-5,6,7,8-四氢喹啉 | 133092-34-9

• 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: 4-氯-5,6,7,8-四氢喹啉
• 英文名称: 4-chloro-5,6,7,8-tetrahydroquinoline
• 英文别名: 4-chloro-5,6,7,8-tetrahydro-quinoline；4-Chlor-5,6,7,8-tetrahydro-chinolin
• CAS: 133092-34-9
• 化学式: C₉H₁₀ClN
• mdl: MFCD18803310
• 分子量: 167.638
• InChiKey: PAEQYSUYGGYPRU-UHFFFAOYSA-N

物化性质

• 沸点：
  150 °C(Press: 5 Torr)
• 密度：
  1.185±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 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：
  12.9
• 氢给体数：
  0
• 氢受体数：
  1

安全信息

• 海关编码：
  2933499090
• 危险性防范说明：
  P261,P280,P301+P312,P302+P352,P305+P351+P338
• 危险性描述：
  H302,H315,H320,H335

反应信息

• 作为反应物：
  描述：

  4-氯-5,6,7,8-四氢喹啉 在 2-双环己基膦-2',6'-二甲氧基联苯 、 potassium phosphate 、 palladium diacetate 、 溶剂黄146 作用下， 以 1,4-二氧六环 、 甲醇 、 二氯甲烷 为溶剂， 反应 45.0h， 生成 4-{5-[4-({[8-(5,6,7,8-tetrahydroquinolin-4-ylamino)octyl]amino}methyl)phenyl]-2-thienyl}benzonitrile
  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
• 作为产物：
  描述：

  4-氨基-7-氯喹啉 在 盐酸 、 platinum(IV) oxide 、 高氯酸 、 氢气 、 sodium nitrite 作用下， 以 水 、 溶剂黄146 为溶剂， 70.0 ℃ 、344.75 kPa 条件下， 反应 86.17h， 生成 4-氯-5,6,7,8-四氢喹啉
  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。
• UBIQUITIN-SPECIFIC-PROCESSING PROTEASE 7 (USP7) MODULATORS AND USES THEREOF
  申请人：RAPT THERAPEUTICS, INC.

  公开号：US20210317134A1

  公开（公告）日：2021-10-14

  Disclosed herein, inter alia, compounds and methods of use thereof for the modulation of USP7 activity.

  本公开的内容包括化合物及其使用方法，用于调节USP7活性。
• NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION
  申请人：BUCKMAN Brad

  公开号：US20120101032A1

  公开（公告）日：2012-04-26

  The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IV, IVa, V, Va, VI and VIa, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

  本实施例提供了一般式I、Ia、II、IIa、III、IIIa、IV、IVa、V、Va、VI和VIa的化合物，以及包括药物组成物在内的组合物，其中包括一种主体化合物。本实施例还提供了治疗方法，包括治疗丙型肝炎病毒感染和治疗肝纤维化的方法，该方法通常涉及向需要治疗的个体施用一种主体化合物或组合物的有效量。
• N-(2,3-dihydro-1,4-benzodioxinyl)-N-substituted aminopyrido-fused
  申请人：John Wyeth & Brother Limited

  公开号：US05194439A1

  公开（公告）日：1993-03-16

  Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2; R is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, amino, (lower)alkylamino or di(lower)alkylamino; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is --(CH.sub.2).sub.n --R.sup.3 or --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.m --R.sup.3 or --CH.sub.2.C.tbd.C.(CH.sub.2).sub.m --R.sup.3 where n is 1 to 6, and m is 0 to 3; and R.sup.3 is a ring of formula ##STR2## The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are used for the treatment of CNS disorders, e.g. anxiety, as antihypertensives and in treating anorexia.

  本文披露了化学式为 ##STR1## 的吡啶衍生物，其杂环芳香族N-氧化物和药学上可接受的酸盐。在该式中，z为0、1或2；R为氢、羟基、较低的烷基、较低的烷氧基、卤素、三氟甲基、硝基、氨基、(较低)烷基氨基或二(较低)烷基氨基；R.sup.1为氢或较低的烷基；R.sup.2为--(CH.sub.2).sub.n --R.sup.3或--CH.sub.2--CH.dbd.CH--(CH.sub.2).sub.m --R.sup.3或--CH.sub.2.C.tbd.C.(CH.sub.2).sub.m --R.sup.3，其中n为1到6，m为0到3；R.sup.3是一个化学式为 ##STR2## 的环。这些化合物表现出5-HT.sub.1A激动剂、拮抗剂或部分激动剂的活性，并用于治疗中枢神经系统疾病，例如焦虑症，作为降压药物以及治疗厌食症。
• Novel Imidazol-piperidinyl Derivatives as Modulators of Kinase Activity
  申请人：LAN Ruoxi

  公开号：US20150239902A1

  公开（公告）日：2015-08-27

  The invention provides novel imidazol-piperidinyl derivatives of formula (I) in which R 1 , R 2 , X 1 , X 2 , X 3 , X 4 and n have the meanings indicated in above, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

  本发明提供了公式（I）中新颖的咪唑-哌啶衍生物，其中R1，R2，X1，X2，X3，X4和n具有上述所示的含义，以及它们的制造和用于治疗过度增殖性疾病，如癌症的用途。