intermediate compound 11 | 932376-61-9

• 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
• 英文名称: intermediate compound 11
• 英文别名: 6-Bromo-2-methoxy-3-[(4-methylphenyl)methyl]quinoline
• CAS: 932376-61-9
• 化学式: C₁₈H₁₆BrNO
• 分子量: 342.235
• InChiKey: AHVYYBBVAJDYOE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(3,5-difluorophenyl)-3-(dimethylamino)prop-1-one 、 intermediate compound 11 在 正丁基锂 、 二异丙胺 作用下， 以 四氢呋喃 为溶剂， 反应 5.33h， 以11%的产率得到1-(3,5-Difluorophenyl)-3-(dimethylamino)-1-[2-methoxy-3-[(4-methylphenyl)methyl]quinolin-6-yl]propan-1-ol
  参考文献：
  名称：

  [EN] QUINOLINE DERIVATIVES AS ANTIBACTERICAL AGENTS
  [FR] DERIVES DE QUINOLEINE UTILISES COMME AGENTS ANTIBACTERIENS

  摘要：

  公开号：

  WO2007014940A3

文献信息

• QUINOLINE DERIVATIVES AND THEIR USE AS MYCOBACTERIAL INHIBITORS
  申请人：Janssen Pharmaceutica NV

  公开号：EP1527050B1

  公开（公告）日：2010-04-07
• EP2301544A1
  申请人：——

  公开号：EP2301544A1

  公开（公告）日：2011-03-30
• Quinoline derivatives as intermediates to mycobacterial inhibitors
  申请人：Janssen Pharmaceutica N.V.

  公开号：EP2301544B1

  公开（公告）日：2012-09-19
• Novel mycobacterial inhibitors
  申请人：Guillemont Emile Georges Jerome

  公开号：US20070093478A1

  公开（公告）日：2007-04-26

  The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof the tautomers forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases. In particular, compounds are claimed in which, independently from each other, R 1 is halo; p=1; R 2 is optionally substituted alkyloxy, alkyl, Ar, Het, or a radical of formula R 3 is optionally substituted Ar or Het; q=1, R 4 and R 5 each independently are alkyl; R 6 is hydrogen or a radical of formula is equal to 0 or 1 and R 7 is hydrogen or Ar. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of 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：Andries Koenraad Jozef Lodewijk Marcel

  公开号：US20080255116A1

  公开（公告）日：2008-10-16

  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 (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof 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, 2 or 3; R 2 is hydrogen; 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 zero, 1, 2, 3 or 4; X is a direct bond or CH 2 ; 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 or a radical of formula R 7 is hydrogen, alkyl, Ar or Het; R 8 is hydrogen or alkyl; R 9 is oxo; or R 8 and R 9 together form the radical —CH═CH—N═;