6-(1H-indazol-4-yl)-8-morpholino-3-(piperazin-1-yl)imidazo[1,2-a]pyrazine | 1252595-00-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 6-(1H-indazol-4-yl)-8-morpholino-3-(piperazin-1-yl)imidazo[1,2-a]pyrazine
• 英文别名: 4-[6-(1H-indazol-4-yl)-3-piperazin-1-ylimidazo[1,2-a]pyrazin-8-yl]morpholine
• CAS: 1252595-00-8
• 化学式: C₂₁H₂₄N₈O
• 分子量: 404.475
• InChiKey: XTFPLMDYICIWIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  86.6
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-氨基-5-溴-3-吗啉-4-基吡嗪 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 potassium carbonate 作用下， 以 乙二醇二甲醚 、 1,2-二氯乙烷 为溶剂， 反应 0.5h， 生成 6-(1H-indazol-4-yl)-8-morpholino-3-(piperazin-1-yl)imidazo[1,2-a]pyrazine
  参考文献：
  名称：

  New use of bis(benzotriazolyl)-1,2-(dialkylamino)ethanes for the synthesis of 2-H-3-dialkylamino imidazo[1,2-a]pyrazine derivatives

  摘要：

  First direct synthesis of 2-H-3-N-dialkyl-imidazo[1,2-a]pyrazines is described. This approach makes use of accessible substituted pyrazines and the assistance of benzotriazole. In such a manner we accomplished the introduction of cyclic amines at C-3 of the scaffold in a convenient formal cyclisation procedure. Detailed examples and utility of this approach are presented herein. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2011.12.077

文献信息

• IMIDAZOPYRAZINES FOR USE AS KINASE INHIBITORS
  申请人：Pastor Fernández Joaquin

  公开号：US20120083492A1

  公开（公告）日：2012-04-05

  There is provided compounds of formula (I), wherein R 1 , R 2 , R 3 , R 4 and R 5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

  提供了式(I)的化合物，其中R1、R2、R3、R4和R5在描述中有给定的含义，以及它们的药用可接受的酯、酰胺、溶剂合物或盐，这些化合物在治疗需要或期望抑制蛋白质或脂质激酶（例如PI3-K和/或mTOR）的疾病方面非常有用，特别是在治疗癌症或增生性疾病方面。
• IMIDAZOPYRAZINES AS INHIBITORS OF PROTEIN KINASES
  申请人：Centro Nacional de Investigaciones Oncológicas (CNIO)

  公开号：EP2419429B1

  公开（公告）日：2014-03-26
• US8778935B2
  申请人：——

  公开号：US8778935B2

  公开（公告）日：2014-07-15
• [EN] IMIDAZOPYRAZINES FOR USE AS KINASE INHIBITORS<br/>[FR] IMIDAZOPYRAZINES POUR UNE UTILISATION EN TANT QU'INHIBITEURS DE KINASE
  申请人：CT NAC DE INVESTIGACIONES ONCO

  公开号：WO2010119264A1

  公开（公告）日：2010-10-21

  There is provided compounds of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
• [EN] COMBINATIONS OF PI3K INHIBITORS WITH A SECOND ANTI -TUMOR AGENT<br/>[FR] COMBINAISONS D'INHIBITEURS DE PI3K AVEC UN SECOND AGENT ANTITUMORAL
  申请人：CT NAC INVESTIGACIONES ONCOLOGICAS CNIO

  公开号：WO2012052745A1

  公开（公告）日：2012-04-26

  There is provided combinations comprising (A) a compound of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, together with (B) one or more therapeutics agents/treatments known to be useful in the treatment of diseases such as cancer or a proliferative disease, which combinations are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.