2-(2-hydrazino-pyridin-5-yl)benzothiazole | 1440676-53-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 英文名称: 2-(2-hydrazino-pyridin-5-yl)benzothiazole
• 英文别名: [5-(1,3-Benzothiazol-2-yl)pyridin-2-yl]hydrazine
• CAS: 1440676-53-8
• 化学式: C₁₂H₁₀N₄S
• 分子量: 242.304
• InChiKey: USYXGOPPCSKSSE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  92.1
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-(2-hydrazino-pyridin-5-yl)benzothiazole 、 diacetyl mono-4-methyl-3-thiosemicarbazone 以 乙醇 为溶剂， 反应 4.0h， 以76%的产率得到1-[3-[[5-(1,3-Benzothiazol-2-yl)pyridin-2-yl]hydrazinylidene]butan-2-ylideneamino]-3-methylthiourea
  参考文献：
  名称：

  [EN] METAL COMPLEXES AS IMAGING AGENTS
  [FR] COMPLEXES MÉTALLIQUES UTILISÉS COMME AGENTS D'IMAGERIE

  摘要：

  本发明涉及铜、镓和锝配合物硫代半胱氨酮-吡啶肼（在吡啶环上取代苯并噻唑或双苯乙烯基团）复合物及其方法。这些化合物在PET成像和淀粉样疾病的诊断中具有实用性。

  公开号：

  WO2013082661A1
• 作为产物：
  描述：

  6-氯烟酸 在 氯化亚砜 、 一水合肼 作用下， 以 乙醇 为溶剂， 反应 5.0h， 生成 2-(2-hydrazino-pyridin-5-yl)benzothiazole
  参考文献：
  名称：

  [EN] METAL COMPLEXES AS IMAGING AGENTS
  [FR] COMPLEXES MÉTALLIQUES UTILISÉS COMME AGENTS D'IMAGERIE

  摘要：

  本发明涉及铜、镓和锝配合物硫代半胱氨酮-吡啶肼（在吡啶环上取代苯并噻唑或双苯乙烯基团）复合物及其方法。这些化合物在PET成像和淀粉样疾病的诊断中具有实用性。

  公开号：

  WO2013082661A1

文献信息

• Diagnostic Imaging Agents for Alzheimer’s Disease: Copper Radiopharmaceuticals that Target Aβ Plaques
  作者：James L. Hickey、SinChun Lim、David J. Hayne、Brett M. Paterson、Jonathan M. White、Victor L. Villemagne、Peter Roselt、David Binns、Carleen Cullinane、Charmaine M. Jeffery、Roger I. Price、Kevin J. Barnham、Paul S. Donnelly

  DOI：10.1021/ja4057807

  日期：2013.10.30

  One of the pathological hallmarks of Alzheimer's disease is the presence of amyloid-beta plaques in the brain and the major constituent of these plaques is aggregated amyloid-beta peptide. New thiosemicarbazone-pyridylhydrazine based ligands that incorporate functional groups designed to bind amyloid-beta plaques have been synthesized. The new ligands form stable four coordinate complexes with a positron-emitting radioactive isotope of copper, Cu-64. Two of the new Cu-II complexes include a functionalized styrylpyridine group and these complexes bind to amyloid-beta plaques in samples of post-mortem human brain tissue. Strategies to increase brain uptake by functional group manipulation have led to a Cu-64 complex that effectively crosses the blood-brain barrier in wild-type mice. The new complexes described in this manuscript provide insight into strategies to deliver metal complexes to amyloid-beta plaques.
• METAL COMPLEXES AS IMAGING AGENTS
  申请人：The University of Melbourne

  公开号：US20150037253A1

  公开（公告）日：2015-02-05

  The present invention relates to copper, gallium and technetium coordinated thiosemicarbazone-pyridylhydrazine (substituted at the pyridine ring with a substituted benzothiazole or stilbene moiety) complexes and methods thereof. Such compounds possess utility in PET imaging and diagnosis of amyloid diseases.