2,6,7-trichloro-3-benzylquinoxaline | 281209-08-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 2,6,7-trichloro-3-benzylquinoxaline
• 英文别名: 2-Benzyl-3,6,7-trichloroquinoxaline
• CAS: 281209-08-3
• 化学式: C₁₅H₉Cl₃N₂
• 分子量: 323.609
• InChiKey: NEHAOFMTCFSZNF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2,6,7-trichloro-3-benzylquinoxaline 在 肼 作用下， 以 异丙醇 为溶剂， 反应 0.25h， 以80.23%的产率得到1-(3-Benzyl-6,7-dichloroquinoxalin-2-yl)hydrazine
  参考文献：
  名称：

  Synthesis of 3-benzyl-2-substituted quinoxalines as novel monoamine oxidase A inhibitors

  摘要：

  A new series of 3-benzyl-2-substituted quinoxalines have been synthesized by means of microwave enhancement of nucleophilic substitution reaction involving the corresponding 2-chloroquinoxaline analogs and substituted amines or hydrazine. The synthesized compounds were evaluated for their monoamine oxidase A and B inhibitory activity by determination of their IC50. All the newly synthesized compounds showed more selective inhibitory activity toward NIAO-A than MAO-B. In addition, the acute toxicity of the synthesized compounds was determined. This work may be a fruitful matrix of the synthesis of a new series of novel MAO-A inhibitors with good safety margins. (C) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.11.088
• 作为产物：
  描述：

  6,7-dichloro-3-benzylquinoxalin-2(1H)-one 在 三氯氧磷 作用下， 反应 2.0h， 以69.5%的产率得到2,6,7-trichloro-3-benzylquinoxaline
  参考文献：
  名称：

  Synthesis of 3-benzyl-2-substituted quinoxalines as novel monoamine oxidase A inhibitors

  摘要：

  A new series of 3-benzyl-2-substituted quinoxalines have been synthesized by means of microwave enhancement of nucleophilic substitution reaction involving the corresponding 2-chloroquinoxaline analogs and substituted amines or hydrazine. The synthesized compounds were evaluated for their monoamine oxidase A and B inhibitory activity by determination of their IC50. All the newly synthesized compounds showed more selective inhibitory activity toward NIAO-A than MAO-B. In addition, the acute toxicity of the synthesized compounds was determined. This work may be a fruitful matrix of the synthesis of a new series of novel MAO-A inhibitors with good safety margins. (C) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.11.088

文献信息

• [EN] NON-PEPTIDE GLP-1 AGONISTS<br/>[FR] AGONISTES NON PEPTIDIQUES DE GLP-1
  申请人：NOVO NORDISK AS

  公开号：WO2000042026A1

  公开（公告）日：2000-07-20

  Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.

  小说性非肽类GLP-1激动剂，包括它们的制药组合物，使用非肽类GLP-1激动剂制备制药组合物的方法以及治疗和/或预防人类GLP-1受体激活有益的疾病和疾病的方法，特别是代谢紊乱，如IGT，1型糖尿病，2型糖尿病和肥胖症。
• NON-PEPTIDE GLP-1 AGONISTS
  申请人：NOVO NORDISK A/S

  公开号：EP1147094A1

  公开（公告）日：2001-10-24
• US6927214B1
  申请人：——

  公开号：US6927214B1

  公开（公告）日：2005-08-09