5-(phthalimidomethyl)-6-quinolinol | 84174-51-6

• 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: 5-(phthalimidomethyl)-6-quinolinol
• 英文别名: 2-[(6-hydroxyquinolin-5-yl)methyl]isoindoline-1,3-dione；2-[(6-hydroxyquinolin-5-yl)methyl]isoindole-1,3-dione
• CAS: 84174-51-6
• 化学式: C₁₈H₁₂N₂O₃
• 分子量: 304.305
• InChiKey: HJEAFWXZCFGVRV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  70.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-(phthalimidomethyl)-6-quinolinol 以42%的产率得到
  参考文献：
  名称：

  DEANA, A. A.;STOKKER, G. E.;SCHULTZ, E. M.;SMITH, R. L.;CRAGOE, E. J. ,, +, J. MED. CHEM., 1983, 26, N 4, 580-585

  摘要：

  DOI：
• 作为产物：
  描述：

  6-羟基喹啉 、 N-羟甲基邻苯二甲酰亚胺 在 硫酸 作用下， 反应 18.0h， 生成 5-(phthalimidomethyl)-6-quinolinol
  参考文献：
  名称：

  2-(Aminomethyl)phenols, a new class of saluretic agents. 5. Fused-ring analogs

  摘要：

  A number of bicyclic ring-fused analogues of 2-(aminomethyl)phenol were synthesized and tested orally in rats and intravenously in dogs for saluretic and diuretic effects. Of the 15 alicylic, aromatic, and heterocyclic ring-fused compounds tested, only 2-(aminomethyl)-4-chloro-1-naphthalenol hydrochloride (2) and 7-(aminomethyl)-6-hydroxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalene hydrochloride (6) displayed a high order of activity.

  DOI：

  10.1021/jm00358a023

文献信息

• 3-QUINOLINE-2-(1H)-YLIDENEINDOLIN-2-ONE DERIVATIVES
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1396490A1

  公开（公告）日：2004-03-10

  There is provided medicaments, particularly a vascular endothelial growth factor (VEGF) inhibitor which is useful as a therapeutic drug for solid tumors, diabetic retinopathy and the like diseases in which angiogenesis is taking a role. That is, since a novel 3-quinolin-2(1H)-ylideneindolin-2-one derivative or a salt thereof has good VEGF inhibitory action, angiogenesis inhibitory action and anti-tumor action, it is useful as ideal VEGF inhibitor, angiogenesis inhibitor and anti-tumor agent.

  提供了药物，特别是一种血管内皮生长因子（VEGF）抑制剂，它可作为固体肿瘤、糖尿病视网膜病变等疾病的治疗药物，这些疾病中血管生成起着作用。也就是说，由于一种新型的3-喹啉-2（1H）-基吲哚-2-酮衍生物或其盐具有良好的VEGF抑制作用、血管生成抑制作用和抗肿瘤作用，因此它可作为理想的VEGF抑制剂、血管生成抑制剂和抗肿瘤药剂。
• 3-Quinolin-2(1h)-ylideneindolin-2-one derivative
  申请人：Samizu Kiyohiro

  公开号：US20050090498A1

  公开（公告）日：2005-04-28

  There is provided medicaments, particularly a vascular endothelial growth factor (VEGF) inhibitor which is useful as a therapeutic drug for solid tumors, diabetic retinopathy and the like diseases in which angiogenesis is taking a role. That is, since a novel 3-quinolin-2(1H)-ylideneindolin-2-one derivative or a salt thereof has good VEGF inhibitory action, angiogenesis inhibitory action and anti-tumor action, it is useful as ideal VEGF inhibitor, angiogenesis inhibitor and anti-tumor agent.

  提供药物，特别是一种血管内皮生长因子（VEGF）抑制剂，可用作固体肿瘤、糖尿病视网膜病变等疾病的治疗药物，在这些疾病中血管生成扮演着重要角色。也就是说，由于一种新型的3-喹啉-2（1H）-基亚胺吲哚-2-酮衍生物或其盐具有良好的VEGF抑制作用、血管生成抑制作用和抗肿瘤作用，因此它作为理想的VEGF抑制剂、血管生成抑制剂和抗肿瘤剂是非常有用的。
• 2-(Aminomethyl)phenols, a new class of saluretic agents. 5. Fused-ring analogs
  作者：A. A. Deana、G. E. Stokker、E. M. Schultz、R. L. Smith、E. J. Cragoe、H. F. Russo、L. S. Watson

  DOI：10.1021/jm00358a023

  日期：1983.4

  A number of bicyclic ring-fused analogues of 2-(aminomethyl)phenol were synthesized and tested orally in rats and intravenously in dogs for saluretic and diuretic effects. Of the 15 alicylic, aromatic, and heterocyclic ring-fused compounds tested, only 2-(aminomethyl)-4-chloro-1-naphthalenol hydrochloride (2) and 7-(aminomethyl)-6-hydroxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalene hydrochloride (6) displayed a high order of activity.
• DEANA, A. A.;STOKKER, G. E.;SCHULTZ, E. M.;SMITH, R. L.;CRAGOE, E. J. ,, +, J. MED. CHEM., 1983, 26, N 4, 580-585
  作者：DEANA, A. A.、STOKKER, G. E.、SCHULTZ, E. M.、SMITH, R. L.、CRAGOE, E. J. ,, +

  DOI：——

  日期：——