(6-Bromo-2-chloro-4-phenylquinolin-8-yl)-phenylmethanol | 862543-50-8

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二芳基庚烷
• 英文名称: (6-Bromo-2-chloro-4-phenylquinolin-8-yl)-phenylmethanol
• CAS: 862543-50-8
• 化学式: C₂₂H₁₅BrClNO
• 分子量: 424.724
• InChiKey: VNIUHGXCVPMVSF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.3
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  33.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (6-Bromo-2-chloro-4-phenylquinolin-8-yl)-phenylmethanol 在 三乙基硅烷 、 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 24.0h， 以38%的产率得到8-Benzyl-6-bromo-2-chloro-4-phenylquinoline
  参考文献：
  名称：

  [EN] QUINOLINE DERIVATIVES FOR USE AS MYCOBACTERIAL INHIBITORS
  [FR] DERIVES DE QUINOLEINE UTILISES EN TANT QU'INHIBITEURS MYCOBACTERIENS

  摘要：

  本发明涉及一种新型的取代喹啉衍生物，符合一般式（I），可用于治疗结核病等分枝杆菌疾病。

  公开号：

  WO2005075428A1
• 作为产物：
  描述：

  2-chloro-6-bromo-4-phenylquinoline 、 苯甲醛 在 2,2,6,6-四甲基哌啶 、 正丁基锂 作用下， 以 四氢呋喃 为溶剂， 反应 5.33h， 以71%的产率得到(6-Bromo-2-chloro-4-phenylquinolin-8-yl)-phenylmethanol
  参考文献：
  名称：

  [EN] QUINOLINE DERIVATIVES FOR USE AS MYCOBACTERIAL INHIBITORS
  [FR] DERIVES DE QUINOLEINE UTILISES EN TANT QU'INHIBITEURS MYCOBACTERIENS

  摘要：

  本发明涉及一种新型的取代喹啉衍生物，符合一般式（I），可用于治疗结核病等分枝杆菌疾病。

  公开号：

  WO2005075428A1

文献信息

• [EN] QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS<br/>[FR] DERIVES DE QUINOLEINE UTILISES COMME AGENTS ANTIBACTERIENS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2007014941A3

  公开（公告）日：2007-03-29
• QUINOLINE DERIVATIVES FOR USE AS MYCOBACTERIAL INHIBITORS
  申请人：Janssen Pharmaceutica NV

  公开号：EP1713776B1

  公开（公告）日：2008-05-14
• NOVEL MYCOBACTERIAL INHIBITORS
  申请人：Guillemont Emile Georges Jerome

  公开号：US20070299106A1

  公开（公告）日：2007-12-27

  The present invention relates to novel substituted quinoline derivatives according to the general Formula (I) pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms thereof, wherein R 1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2 or 3; s is 0, 1, 2, 3 or 4; R 2 is hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het, a radical of formula R 3 is alkyl, Ar, Ar-alkyl, Het, Het-alkyl; q is 0, 1, 2, 3 or 4; R 4 and R 5 are hydrogen, alkyl, benzyl; or R 4 and R 5 may be taken together including the N to which they are attached; R 6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R 6 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R 7 is hydrogen, alkyl, Ar or Het; R 8 is hydrogen-, alkyl, hydroxyl, aminocarbonyl, mono-or di(alkyl)aminocarbonyl, Ar, Het, substituted alkyl, Het-C(═O)— or Ar—C(═O)—; provided that when the quinoline substituent carrying the R 3 to R 6 substituents is placed in position 3 of the quinoline moiety; R 7 is placed in position 4 and R 2 is placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula then s is 1, 2, 3 or 4; also claimed is a composition comprising the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.
• Quinoline Derivatives as Antibacterial Agents
  申请人：Guillemont Jerome Emile Georges

  公开号：US20080207687A1

  公开（公告）日：2008-08-28

  Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I) a pharmaceutically acceptable acid or base addition salt, a quaternary amine, a stereochemically isomeric form, a tautomeric form or a N-oxide form thereof, wherein R 1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1 to 3; s is 0 to 4; R 2 is hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula R 3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 0 to 4; R 4 and R 5 each independently are hydrogen, alkyl or benzyl; or R 4 and R 5 may be taken together including the N to which they are attached; R 6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R 6 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1 to 5; R 7 is hydrogen, alkyl, Ar or Het; R 8 is hydrogen, alkyl, hydroxyl, aminocarbonyl, mono- or di(alkyl)aminocarbonyl, Ar, Het, alkyl substituted with one or two Het, alkyl substituted with one or two Ar, Het-C(═O)— or Ar—C(═O)—; provided that when the R 3 bearing radical is placed in position 3 of the quinoline moiety; R 7 is placed in position 4 and R 2 is placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula then s is 1 to 4.
• US7790894B2
  申请人：——

  公开号：US7790894B2

  公开（公告）日：2010-09-07