4-羟基-7-碘喹啉 | 22297-71-8

• 物质功能分类: 医药中间体 - 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: 4-羟基-7-碘喹啉
• 英文名称: 7-iodo-quinolin-4-ol
• 英文别名: 7-Jod-chinolin-4-ol；4-Hydroxy-7-iodoquinoline；7-iodoquinolin-4-ol；7-iodo-1H-quinolin-4-one
• CAS: 22297-71-8
• 化学式: C₉H₆INO
• 分子量: 271.057
• InChiKey: QIQHXKFDDHQTKQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933499090

反应信息

• 作为反应物：
  描述：

  4-羟基-7-碘喹啉 在 三氯氧磷 作用下， 反应 2.0h， 以80%的产率得到4-氯-7-碘喹啉
  参考文献：
  名称：

  [EN] NOVEL QUINOLINE DERIVATIVES
  [FR] DERIVES NOUVEAUX DE QUINOLEINE

  摘要：

  该发明涉及由式(I)表示的化合物，以及所述化合物的药学上可接受的盐或溶剂化合物，其中A、R3-8、X3、X5、m和n在此处被定义。该发明还涉及含有式(I)化合物的药物组合物，以及通过给予式(I)化合物治疗哺乳动物的增生性疾病的方法。

  公开号：

  WO2005063739A1
• 作为产物：
  描述：

  ethyl 7-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylate 在 sodium hydroxide 作用下， 以 二苯醚 为溶剂， 反应 1.0h， 生成 4-羟基-7-碘喹啉
  参考文献：
  名称：

  Structure−Activity Relationships for Antiplasmodial Activity among 7-Substituted 4-Aminoquinolines

  摘要：

  Aminoquinolines (AQs) with diaminoalkane side chains (-HNRNEt2) shorter or longer than the isopentyl side chain [-HNCHMe(CH2)(3)NEt2] of chloroquine are active against both chloroquine-susceptible and -resistant Plasmodium falciparum. (De, D.; et al. Am. J. Trop. Med. Hyg. 1996, 55, 579-583). In the studies reported here, we examined structure-activity relationships (SARs) among AQs with different N,N-diethyldiaminoalkane side chains and different substituents at the 7-position occupied by Cl in chloroquine. 7-Iodo- and 7-bromo-AQs with diaminoalkane side chains [-HN(CH2)(2)NEt2, -HN(CH2)(3)NEt2, or -HNCHMeCH2NEt2] were as active as the corresponding 7-chloro-AQs against both chloroquine-susceptible and -resistant P. falciparum (IC(50)s of 3-12 nM). In contrast, with one exception, 7-fluoro-AQs and 7-trifluoromethyl-AQs were less active against chloroquine-susceptible P. falciparum (IC(50)s of 15-50 nM) and substantially less active against chloroquine-resistant P. falciparum (IC(50)s of 18-500 nM). Furthermore, most 7-OMe-AQs were inactive against both chloroquine-susceptible (IC(50)s of 17-150 nM) and -resistant P. falciparum (IC(50)s of 90-3000 nM).

  DOI：

  10.1021/jm980146x

文献信息

• Compounds and Methods of Treatment
  申请人：LACKEY Karen Elizabeth

  公开号：US20080234267A1

  公开（公告）日：2008-09-25

  A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity.

  本文描述了一种作为Ret酪氨酸激酶抑制剂有用的衍生物。所述发明还包括使用相同物质治疗由不当的Ret酪氨酸激酶活性介导的疾病的方法。
• NOVEL QUINOLINE DERIVATIVES
  申请人：Hong Yufeng

  公开号：US20090069316A1

  公开（公告）日：2009-03-12

  The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R 3-8 , X 3 , X 5 , m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).

  该发明涉及由公式（I）表示的化合物，以及该化合物的药学上可接受的盐或溶剂，其中在此定义了A、R3-8、X3、X5、m和n中的每个。该发明还涉及包含公式（I）化合物的药物组合物，以及通过给予公式（I）化合物来治疗哺乳动物的过度增殖性疾病的方法。
• THIOQUINOLONE DERIVATIVE
  申请人：ZENYAKU KOGYO KABUSHIKI KAISHA

  公开号：EP0786454A1

  公开（公告）日：1997-07-30

  Disclosed is a thioquinolone derivative which exhibits highly selective antibacterial activity against Helicobacter pylori and which is represented by the formula I wherein R1 and R2 respectively represent hydrogen atom or R1 and R2 are joined to form ―O―(CH2)2-; R3 represents halogen atom, C1-C12 alkyl group, C1-C12 alkoxy group, lower alkylsulfonyloxy group, carboxy lower alkoxy group, lower alkylthio group, benzyloxy group, benzylthio group, phenoxy group, styryl group, nitro group, phenyl group, naphthyl group, piperazinyl group, morpholino group or hydroxyl group or represents ―CH2R5, ―COR6 or ―NR7R8 wherein R5 represents benzyl group, phenyl group, hydroxyl group, lower alkoxy group, lower alkylcarbonyloxy group, phenoxy group, di-lower alkylamino group or benzimidazolylthio group, R6 represents lower alkyl group or amino group and R7 and R8 respectively represent lower alkyl group; and R4 represents hydrogen atom or lower alkyl group or is coupled with R3 to form cyclohexene ring, benzene ring or pyridine ring, R3 being not halogen atom at any of positions 5 to 8, methyl group at position 6 or methoxy group at position 6 of the quinoline ring when R1, R2 and R4 are respectively hydrogen atom, R3 and R4 being not at positions 6 and 7 or positions 6 and 8 of the quinoline ring when R1 and R2 are respectively hydrogen atom and R4 is lower alkyl group.

  本发明公开了一种硫代喹啉酮衍生物，它对幽门螺旋杆菌具有高选择性抗菌活性，由式 I 表示 其中 R1 和 R2 分别代表氢原子或 R1 和 R2 连接形成-O-(CH2)2-； R3代表卤素原子、C1-C12烷基、C1-C12烷氧基、低级烷基磺酰氧基、低级烷氧基羧基、低级烷硫基、苄氧基、苄硫基、苯氧基、苯乙烯基、硝基、苯基、萘基、哌嗪基、吗啉基或羟基或代表- R5、-其中 R5 代表苄基、苯基、羟基、低级烷氧基、低级烷基羰氧基、苯氧基、二低级烷基氨基或苯并咪唑硫基，R6 代表低级烷基或氨基，R7 和 R8 分别代表低级烷基；和 R4 代表氢原子或低级烷基，或与 R3 结合形成环己烯环、苯环或吡啶环、 当 R1、R2 和 R4 分别为氢原子时，R3 不是喹啉环 5 至 8 位上的卤素原子、6 位上的甲基或 6 位上的甲氧基、 当 R1 和 R2 分别为氢原子和 R4 为低级烷基时，R3 和 R4 不在喹啉环的第 6 和 7 位或第 6 和 8 位。
• Co(III)-Catalyzed Enaminone-Directed C–H Amidation for Quinolone Synthesis
  作者：Pengfei Shi、Lili Wang、Kehao Chen、Jie Wang、Jin Zhu

  DOI：10.1021/acs.orglett.7b00968

  日期：2017.5.5

  We report herein the development of a Co (III)-catalyzed enaminone-directed C-H amidation method for synthetic access to quinolones, an important heterocyclic scaffold for diverse pharmaceutically active structures. The C-H coupling with,dioxazolones and subsequent deacylation of an installed amide group allow consecutive C-N coupling generation of quinolones with wide-ranging compatible substituent patterns.
• Some 7-Substituted 4-Aminoquinoline Derivatives
  作者：Alexander R. Surrey、Henry F. Hammer

  DOI：10.1021/ja01205a036

  日期：1946.1