2-amino-6-chloro-4-phenylquinoline | 51478-40-1

• 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: 2-amino-6-chloro-4-phenylquinoline
• 英文别名: ST048871；6-chloro-4-phenyl-quinolin-2-ylamine；6-chloro-4-phenylquinolin-2-amine；2-Amino-4-phenyl-6-chlor-chinolin
• CAS: 51478-40-1
• 化学式: C₁₅H₁₁ClN₂
• 分子量: 254.719
• InChiKey: ZAVHPPBSMGSTHT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 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：

  2-amino-6-chloro-4-phenylquinoline 在 palladium on activated charcoal 氢气 、 sodium acetate 作用下， 以 乙二醇二甲醚 、 乙醇 为溶剂， 反应 5.0h， 生成 ethyl 5-phenylimidazo<1,2-a>quinoline-2-carboxylate
  参考文献：
  名称：

  Synthesis and oral antiallergic activity of carboxylic acids derived from imidazo[2,1-c][1,4]benzoxazines, imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles

  摘要：

  4H-Imidazo[2,1-c][1,4]benzoxazine-2-carboxylic acid (3) was found to possess potent activity in the IgE-induced rat passive cutaneous anaphylaxis model which may be predictive of clinical antiallergic activity. Compared to disodium cromoglycate (DSCG, 1), 3 was less active following iv administration but unlike DSCG showed very significant oral activity. To explore the structural requirements for this activity, a range of tricyclic compounds was prepared and their activities were measured. Individual 2-carboxylic acids derived from imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles showed iv activities up to 10(3) times as potent as DSCG and many of them showed significant oral activity. From these, imidazo[1,2-a]quinoxaline-2-carboxylic acid 114 has been chosen for further development.

  DOI：

  10.1021/jm00401a009
• 作为产物：
  描述：

  (Z)-3-(2-amino-5-chlorophenyl)-3-phenylprop-2-enenitrile 以 乙醇 为溶剂， 反应 7.0h， 以0.12 g的产率得到2-amino-6-chloro-4-phenylquinoline
  参考文献：
  名称：

  Thermochemical behavior of o-azidocinnamonitriles

  摘要：

  DOI：

  10.1021/jo01311a044

文献信息

• QUINOLINES
  申请人：Kolczewski Sabine

  公开号：US20090088451A1

  公开（公告）日：2009-04-02

  The present invention relates to 2-aminoquinolines of formula I wherein R 1 , R 2 and R 3 are as defined in the specification, as 5-HT 5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.

  本发明涉及式I的2-氨基喹啉，其中R1、R2和R3如规范中定义的，作为5-HT5A受体拮抗剂，它们的制造、含有它们的药物组合物以及它们用于治疗中枢神经系统疾病的用途。
• Novel Substituted 2-Amino-4-Phenyldihydroquinolines, Processes for their Preparation, Pharmaceutical Compositions and Methods for Their Use
  申请人：Lang Hans-Jochen

  公开号：US20090118329A1

  公开（公告）日：2009-05-07

  The invention relates to NHE-3 inhibitor compounds of formula I: In which R1-R11 are more specifically defined herein. These substituted 2-amino-4-phenyl-dihydroquinolines are useful the treatment of various renal and respiratory disorders such as acute or chronic renal failure, for impairments of biliary function and respiratory impairments such as snoring, sleep apneas or stroke. Formulations comprising them and methods for their use are also described herein.

  该发明涉及式I的NHE-3抑制剂化合物： 其中R1-R11在此更具体地定义。这些取代的2-氨基-4-苯基-二氢喹啉对于治疗各种肾脏和呼吸系统疾病，如急性或慢性肾功能衰竭，胆功能障碍和呼吸功能障碍，如打鼾、睡眠呼吸暂停或中风是有用的。本文还描述了包含它们的配方和它们的使用方法。
• Azacyanines of the Pyrrolopyrrole Series
  作者：Timo Marks、Ewald Daltrozzo、Andreas Zumbusch

  DOI：10.1002/chem.201304235

  日期：2014.5.19

  The reaction of POCl3‐activated, readily soluble diketopyrrolopyrrole (DPP) with 2‐aminoheteroaromatics to yield 1:1 and 1:2 hydrogen chelates is described. Complexation of these hydrogen chelates with boron reagents results in thermally and photochemically stable fluorescent dyes (PP–azacyanines). The 1:2 complexes in particular absorb at long wavelengths and are brightly fluorescing. The rich photophysics

  描述了POCl 3活化的，易溶的二酮吡咯并吡咯（DPP）与2-氨基杂芳族化合物的反应，生成1：1和1：2的氢螯合物。这些氢螯合物与硼试剂的络合产生了热和光化学稳定的荧光染料（PP-氮杂菁）。1：2络合物尤其在长波长处吸收并且发出明亮的荧光。介绍了新化合物的丰富光物理性质。S 0 →S 1跃迁的明显振动精细结构和观察到的荧光现象都允许对分子结构和光学性质之间的相关性做出详细的结论。
• Amide Compound
  申请人：Ogino Masaki

  公开号：US20090048258A1

  公开（公告）日：2009-02-19

  The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R 1 and R 2 are each independently a hydrogen atom or a substituent, R 3 is a hydrogen atom or a C 1-6 alkyl group, or R 3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra 1 is an optionally substituted hydrocarbon group, and Ra 2 and Ra 3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.

  本发明涉及一种由公式（I）或（II）表示的化合物，其中环A是一个可选的取代环（该环不应为吡咯烷，哌啶和哌嗪），环B是一个可选的取代芳香环，环D是一个可选的取代环，R1和R2分别是氢原子或取代基，R3是氢原子或C1-6烷基，或者R3与环A连接形成非芳香环，环Aa是一个可选的取代芳香烃，Y是CH或N，Ra1是一个可选的取代烃基，Ra2和Ra3分别是氢原子或取代基，或其盐。本发明提供了一种具有DGAT抑制活性的化合物，可用于治疗或改善由高表达或高激活DGAT引起的疾病或病理学。
• Substituted 2-amino-4-phenyldihydroquinolines, processes for their preparation, pharmaceutical compositions and methods for their use
  申请人：Sanofi-Aventis

  公开号：US08106204B2

  公开（公告）日：2012-01-31

  The invention relates to NHE-3 inhibitor compounds of formula I: In which R1-R11 are more specifically defined herein. These substituted 2-amino-4-phenyl-dihydroquinolines are useful the treatment of various renal and respiratory disorders such as acute or chronic renal failure, for impairments of biliary function and respiratory impairments such as snoring, sleep apneas or stroke. Formulations comprising them and methods for their use are also described herein.

  本发明涉及式I的NHE-3抑制剂化合物：其中R1-R11在此更具体地定义。这些取代的2-氨基-4-苯基-二氢喹啉衍生物对于治疗各种肾脏和呼吸系统疾病非常有用，如急性或慢性肾衰竭，胆汁功能障碍和呼吸障碍，如打鼾，睡眠呼吸暂停或中风。本文还描述了包含它们的配方和使用它们的方法。