2,3-dihydro-8-methyl-5-<4-<2-(3,4,5-trimethoxyphenyl)ethyl>phenyl>furo<3,2-c>imidazo<1,2-a>pyridine | 134471-33-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 2,3-dihydro-8-methyl-5-<4-<2-(3,4,5-trimethoxyphenyl)ethyl>phenyl>furo<3,2-c>imidazo<1,2-a>pyridine
• 英文别名: 2,3-Dihydro-8-methyl-5-[4-[2-(3,4,5-trimethoxyphenyl)ethyl]phenyl]furo[3,2-c]imidazo[1,2-a]pyridine；11-methyl-7-[4-[2-(3,4,5-trimethoxyphenyl)ethyl]phenyl]-10-oxa-3,6-diazatricyclo[7.3.0.02,6]dodeca-1(9),2,7,11-tetraene
• CAS: 134471-33-3
• 化学式: C₂₇H₂₈N₂O₄
• 分子量: 444.53
• InChiKey: QQVLNGXUFWKFIG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  56.4
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2,5-二甲基-3-呋喃羧酸甲酯 在 正丁基锂 、 四甲基乙二胺 、 三甲基铝 、 对甲苯磺酸 作用下， 以 苯 为溶剂， 反应 24.5h， 生成 2,3-dihydro-8-methyl-5-<4-<2-(3,4,5-trimethoxyphenyl)ethyl>phenyl>furo<3,2-c>imidazo<1,2-a>pyridine
  参考文献：
  名称：

  Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists

  摘要：

  In an effort to determine the effect of modification of the imidazo[2,1-a]isoquinoline portion of the PAF-receptor antagonist SDZ 64-412 (1), several new analogs were prepared and evaluated in vitro and in vivo. One of these, 5-[4-[2-(3,4,5-trimethoxyphenyl)ethyl]phenyl]-2,3-dihydroimidazo[1,2-a]thieno[2,3-c]pyridine (6) was 4-5 times more potent than 1 in inhibiting PAF-induced bronchoconstriction and hemoconcentration when administered po to the guinea pig.

  DOI：

  10.1021/jm00073a008

文献信息

• 5-Aryl-substituted-2,3-dihydro-imidazo [1,2-a]furo[3,2-c]- or thieno[2,3-c]pyridines
  申请人：SANDOZ AG

  公开号：EP0341213A2

  公开（公告）日：1989-11-08

  5-Aryl-substituted-2,3-dihydro-imidazo[1,2-a]furo[3,2-c]-or thieno[2,3-c]pyridines. The intention discloses compounds of formula I wherein the substituents have various significances. They can be prepared by dehydration. They are indicated for use as inhibitors of platelet activating factor (PAF) and as anti-tumor agents.

  5-Aryl-substituted-2,3-dihydro-imidazo[1,2-a]furo[3,2-c]-or thieno[2,3-c]pyridines. 该意向书公开了式 I 的化合物 其中的取代基具有各种意义。 它们可以通过脱水制备。它们可用作血小板活化因子（PAF）抑制剂和抗肿瘤剂。
• US4992428A
  申请人：——

  公开号：US4992428A

  公开（公告）日：1991-02-12
• US5141932A
  申请人：——

  公开号：US5141932A

  公开（公告）日：1992-08-25
• Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists
  作者：William J. Houlihan、Seung H. Cheon、Vincent A. Parrino、Dean A. Handley、Douglas A. Larson

  DOI：10.1021/jm00073a008

  日期：1993.10

  In an effort to determine the effect of modification of the imidazo[2,1-a]isoquinoline portion of the PAF-receptor antagonist SDZ 64-412 (1), several new analogs were prepared and evaluated in vitro and in vivo. One of these, 5-[4-[2-(3,4,5-trimethoxyphenyl)ethyl]phenyl]-2,3-dihydroimidazo[1,2-a]thieno[2,3-c]pyridine (6) was 4-5 times more potent than 1 in inhibiting PAF-induced bronchoconstriction and hemoconcentration when administered po to the guinea pig.