4-(3-Chloro-phenyl)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-quinoline-2-carbaldehyde | 280143-22-8

• 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: 4-(3-Chloro-phenyl)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-quinoline-2-carbaldehyde
• 英文别名: 4-(3-Chlorophenyl)-6-[(4-chlorophenyl)-hydroxy-(3-methylimidazol-4-yl)methyl]quinoline-2-carbaldehyde
• CAS: 280143-22-8
• 化学式: C₂₇H₁₉Cl₂N₃O₂
• 分子量: 488.373
• InChiKey: LQHAJDSGHCTBQT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  68
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-(3-Chloro-phenyl)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-quinoline-2-carbaldehyde 在 氯化亚砜 、 对甲苯磺酰肼 作用下， 以 甲醇 为溶剂， 生成 7-[Chloro-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-5-(3-chloro-phenyl)-[1,2,3]triazolo[1,5-a]quinoline
  参考文献：
  名称：

  Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors

  摘要：

  A series of (4-chlorophenyl)-alpha-(1-methyl-1H-imidazol-5-yl)azoloquinolines and -quinazolines was prepared. These compounds displayed potent Farnesyl Protein Transferase inhibitory activity and tetrazolo[1,5-a]quinazolines are promising agents for oral in vivo inhibition. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2003.08.080
• 作为产物：
  描述：

  (+/-)-4-(3-chlorophenyl)-α-(4chlorophenyl)-2-methyl-α-(1-methyl-1H-imidazol-5-yl)-6-quinolinemethanol 在 selenium(IV) oxide 、 水 作用下， 以 1,4-二氧六环 为溶剂， 生成 4-(3-Chloro-phenyl)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-quinoline-2-carbaldehyde
  参考文献：
  名称：

  Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors

  摘要：

  A series of (4-chlorophenyl)-alpha-(1-methyl-1H-imidazol-5-yl)azoloquinolines and -quinazolines was prepared. These compounds displayed potent Farnesyl Protein Transferase inhibitory activity and tetrazolo[1,5-a]quinazolines are promising agents for oral in vivo inhibition. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2003.08.080

文献信息

• Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors
  申请人：——

  公开号：US20030203904A1

  公开（公告）日：2003-10-30

  This invention comprises the novel compounds of formula (I)wherein r, s, t, Y 1 -Y 2 , R 1 , R 2 , R 3 , R 4 , R 5 and R 7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

  这个发明包括式（I）的新化合物，其中r，s，t，Y1-Y2，R1，R2，R3，R4，R5和R7具有定义的含义，具有法尼醇转移酶抑制活性；它们的制备，含有它们的组合物以及它们作为药物的用途。
• FARNESYL TRANSFERASE INHIBITING QUINOLINE AND QUINAZOLINE DERIVATIVES AS FARNESYL TRANSFERASE INHIBITORS
  申请人：JANSSEN PHARMACEUTICA N.V.

  公开号：EP1322635A1

  公开（公告）日：2003-07-02
• US7053105B2
  申请人：——

  公开号：US7053105B2

  公开（公告）日：2006-05-30
• [EN] FARNESYL TRANSFERASE INHIBITING QUINOLINE AND QUINAZOLINE DERIVATIVES AS FARNESYL TRANSFERASE INHIBITORS<br/>[FR] DERIVES DE QUINOLINE ET DE QUINAZOLINE INHIBANT LA FARNESYL TRANSFERASE COMME INHIBITEURS DE FARNESYL TRANSFERASE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2002024682A1

  公开（公告）日：2002-03-28

  This invention comprises the novel compounds of formula (I)wherein r, s, t, Y?1-Y2, R1, R2, R3, R4, R5 and R7¿ have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.