2-((tert-butylamino)methyl)-3,5,6-trimethylpyrazine | 1083171-74-7

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-((tert-butylamino)methyl)-3,5,6-trimethylpyrazine
• 英文别名: 2-methyl-N-[(3,5,6-trimethylpyrazin-2-yl)methyl]propan-2-amine
• CAS: 1083171-74-7
• 化学式: C₁₂H₂₁N₃
• 分子量: 207.319
• InChiKey: MNKRQDJQKTXMHV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  37.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-((tert-butylamino)methyl)-3,5,6-trimethylpyrazine 以36的产率得到硝酮嗪
  参考文献：
  名称：

  NITRONE COMPOUNDS, PROCESS OF PREPARATION THEREOF, AND USE THEREOF IN MEDICAMENT MANUFACTURE

  摘要：

  本发明提供了新型的亚硝基酮，它们的制备和用途。新型化合物的化学式如下：I。本发明的化合物具有强大的抗氧化活性，并具有溶血性。这些化合物可以用于治疗和/或预防由自由基过度产生和/或血栓形成引起的疾病。

  公开号：

  US20110034485A1
• 作为产物：
  描述：

  叔丁胺 、 2-(溴甲基)-3,5,6-三甲基吡嗪 反应 4.0h， 以100%的产率得到2-((tert-butylamino)methyl)-3,5,6-trimethylpyrazine
  参考文献：
  名称：

  Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke

  摘要：

  Ischemic stroke results from brain blood vessel blockage by thrombus, and produces neuronal cell damage and death. While thrombolytic therapy with tPA has achieved some success in clinic, the strategy of using neuroprotective agents to treat ischemic stroke has been disappointing thus far. In the present work, we synthesized TBN, a derivative of the clinically useful stroke drug TMP armed with a powerful free radical-scavenging nitrone moiety. TBN retains the thrombolytic activity of the parent TMP and possesses strong antioxidative properties. TBN demonstrates significant activity in the rat MCAo stroke model. The results suggest that design of molecules possessing both thrombolytic and neuroprotective properties may be a novel strategy for effective stroke therapeutics. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2008.08.075

文献信息

• [EN] PYRAZINE DERIVATIVES,PROCESS FOR MANUFACTURE AND USE THEREOF<br/>[FR] DÉRIVÉS DE PYRAZINE, LEUR PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION
  申请人：UNIV JINAN

  公开号：WO2012003784A1

  公开（公告）日：2012-01-12

  Pyrazine derivatives of formula (I) and pharmaceutically acceptable salts thereof are disclosed, wherein the designation of R1, R2, R3 and R4 are provided herein. Syntheses for preparation of such compounds are disclosed. Methods of use of these compounds and pharmaceutical compositions containing them for treatment and/or prevention of diseases and for manufacture of medicaments are disclosed. These compounds and pharmaceutical compositions have antioxidative and thrombolytic effects, and thus can be used for the treatment and/or prevention of cerebral stroke caused by ischemia, and used for manufacture of medicaments for the treatment and/or prevention of nervous system diseases caused by excessive amount of radicals and/or thrombosis, infectious diseases, metabolic system diseases, cardiovascular and cerebrovascular diseases, and age-related degenerative diseases.

  本文披露了式（I）的吡嗪衍生物及其药用可接受盐，其中提供了R1、R2、R3和R4的指定。披露了制备这些化合物的合成方法。披露了这些化合物的使用方法和含有它们的药物组合物，用于治疗和/或预防疾病以及制造药物。这些化合物和药物组合物具有抗氧化和溶栓作用，因此可用于治疗和/或预防由缺血引起的脑卒中，并用于制造用于治疗和/或预防由自由基和/或血栓形成引起的神经系统疾病、传染病、代谢系统疾病、心血管和脑血管疾病以及与年龄相关的退行性疾病的药物。
• NITRONE COMPOUNDS, PROCESS OF PREPARATION THEREOF, AND USE THEREOF IN MEDICAMENT MANUFACTURE
  申请人：Wang Yuqiang

  公开号：US20110034485A1

  公开（公告）日：2011-02-10

  The present invention provides novel nitrones, their preparation and use. The novel compounds have the following formula: I The compounds of the present invention have strong antioxidative activity, and are thrombolytic. These compounds can be used to treat and/or prevent diseases caused by overproduction of free radicals and/or formation of thrombus.

  本发明提供了新型的亚硝基甲酰亚胺，其制备和用途。这些新化合物的化学式为：I。本发明化合物具有强抗氧化活性和溶栓作用。这些化合物可用于治疗和/或预防由自由基过度产生和/或血栓形成引起的疾病。
• [EN] NITRONE COMPOUNDS, PROCESS OF PREPARATION THEREOF, AND USE THEREOF IN MEDICAMENT MANUFACTURE<br/>[FR] COMPOSÉS DE NITRONE, PROCÉDÉ DE PRÉPARATION DE CEUX-CI, ET UTILISATION DE CEUX-CI DANS LA FABRICATION DE MÉDICAMENTS
  申请人：UNIV JINAN

  公开号：WO2009129726A1

  公开（公告）日：2009-10-29

  The present invention provides novel nitrones, their preparation and use. The novel compounds have the following formula: I The compounds of the present invention have strong antioxidative activity, and are thrombolytic. These compounds can be used to treat and/or prevent diseases caused by overproduction of free radicals and/or formation of thrombus.

  本发明提供了新型亚硝基甲酰胺，其制备和用途。新化合物具有以下公式：I。本发明的化合物具有强的抗氧化活性，并具有溶血性。这些化合物可用于治疗和/或预防由自由基过度产生和/或血栓形成引起的疾病。
• PYRAZINE DERIVATIVES, PROCESS FOR MANUFACTURE AND USE THEREOF
  申请人：Wang Yuqiang

  公开号：US20120115874A1

  公开（公告）日：2012-05-10

  The present invention provides pyrazine derivatives of formula I and pharmaceutically acceptable salts thereof, wherein the designation of R 1 , R 2 , R 3 and R 4 is provided herein. The invention also provides syntheses for preparation of such compounds. The invention further provides methods of use of these compounds and pharmaceutical compositions containing them for treatment and/or prevention of diseases and for manufacture of medicaments. These compounds and pharmaceutical compositions have antioxidative and thrombolytic effects, and thus can be used for the treatment and/or prevention of cerebral stroke caused by ischemia, and used for manufacture of medicaments for the treatment and/or prevention of nervous system diseases caused by excessive amount of radicals and/or thrombosis, infectious diseases, metabolic system diseases, cardiovascular and cerebrovascular diseases, and age-related degenerative diseases.
• US8796281B2
  申请人：——

  公开号：US8796281B2

  公开（公告）日：2014-08-05