(+/-)-2-chloro-4-(3-chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)-6-quinolinemethanol | 280143-17-1

• 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: (+/-)-2-chloro-4-(3-chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)-6-quinolinemethanol
• 英文别名: (+/-)-2-chloro-4-(3-chlorophenyl)-alpha-(4-chlorophenyl)-alpha-(1-methyl-1H-imidazol-5-yl)-6-quinolinemethanol；[2-chloro-4-(3-chlorophenyl)quinolin-6-yl]-(4-chlorophenyl)-(3-methylimidazol-4-yl)methanol
• CAS: 280143-17-1
• 化学式: C₂₆H₁₈Cl₃N₃O
• 分子量: 494.807
• InChiKey: MCLYBENAEYWYGO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.5
• 重原子数：
  33
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  50.9
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (+/-)-2-chloro-4-(3-chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)-6-quinolinemethanol 在 肼 作用下， 以 1,4-二氧六环 、 水 为溶剂， 以76%的产率得到(4-Chlorophenyl)-[4-(3-chlorophenyl)-2-hydrazinylquinolin-6-yl]-(3-methylimidazol-4-yl)methanol
  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：

  N-[2-(3-chlorobenzoyl)-4-(4-chlorobenzoyl)phenyl]acetamide 在 正丁基锂 、 potassium tert-butylate 、 三氯氧磷 作用下， 以 四氢呋喃 、 乙二醇二甲醚 为溶剂， 生成 (+/-)-2-chloro-4-(3-chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)-6-quinolinemethanol
  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：EP1322635B1

  公开（公告）日：2006-03-22
• US7053105B2
  申请人：——

  公开号：US7053105B2

  公开（公告）日：2006-05-30
• Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors
  作者：Patrick Angibaud、Xavier Bourdrez、David W. End、Eddy Freyne、Michel Janicot、Patricia Lezouret、Yannick Ligny、Geert Mannens、Siegrid Damsch、Laurence Mevellec、Christophe Meyer、Philippe Muller、Isabelle Pilatte、Virginie Poncelet、Bruno Roux、Gerda Smets、Jacky Van Dun、Pieter Van Remoortere、Marc Venet、Walter Wouters

  DOI：10.1016/j.bmcl.2003.08.080

  日期：2003.12

  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.