chloramine phosphorus | 73447-20-8

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 卤代醇
• 英文名称: chloramine phosphorus
• 英文别名: O,S-dimethyl (2,2,2-trichloro-1-hydroxyethyl)phosphoramidothioate；chloramidophos；2,2,2-Trichloro-1-[[methoxy(methylsulfanyl)phosphoryl]amino]ethanol
• CAS: 73447-20-8
• 化学式: C₄H₉Cl₃NO₃PS
• 分子量: 288.519
• InChiKey: MBIOGXSXQDUSPT-UHFFFAOYSA-N

物化性质

• 沸点：
  318.8±52.0 °C(Predicted)
• 密度：
  1.603±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  83.9
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  chloramine phosphorus 生成 2,2-dichloro-N-[methoxy(methylsulfanyl)phosphoryl]ethenamine
  参考文献：
  名称：

  摘要：

  DOI：
• 作为产物：
  描述：

  在 potassium carbonate 、 苯硫酚 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成 chloramine phosphorus
  参考文献：
  名称：

  新的5-HT 4受体激动剂的设计，合成和生物学评估：作为淀粉样蛋白级联调节剂的应用和在阿尔茨海默氏病中的潜在治疗作用

  摘要：

  5-羟色胺5-HT 4受体（5-HT 4 R）激动剂特别适合治疗阿尔茨海默氏病，因为它们具有缓解认知缺陷和调节淀粉样β蛋白（Aβ）产生的能力。然而，尽管迄今为止合成了范围广泛的5-HT 4 R激动剂，但仍然缺乏有效的和选择性的5-HT 4 R激动剂。在本研究中，基于ML10302支架的分子的两个文库，即高度特异性和部分5-HT 4R激动剂可通过平行支持的合成方法有效制备，并评估其结合亲和力和激动剂活性。此外，我们表明，在体内，通过增加小鼠皮质和海马中淀粉样前体蛋白（sAPPα）的可溶形式的水平，两个最佳候选物表现出神经保护活性。有趣的是，这些化合物中的一种还可以在体外抑制Aβ原纤维的形成。

  DOI：

  10.1021/jm801327q

文献信息

• Mechanisms of Composition Change and Toxic Potentiation of Chloramidophos Emulsifiable Concentrate during Storage
  作者：Shanshan Zhou、Datong Zhang、Huayun Yang、Ying Zhang、Weiping Liu

  DOI：10.1021/jf803188f

  日期：2009.2.11

  Storage instability is one of the serious problems that greatly restrict pesticide use. Routine checks on the composition and toxicity of 30% emulsifiable concentrates (EC) of chloramidophos (CP) during storage indicated that 78.6% of the active ingredient had decreased, whereas the anti-acetylcholinesterase (AChE) activity of the formulation was potentiated by 3.5 times. To understand the mechanism for these changes, detailed knowledge of the products present and their effects on anti-AChE potential deserves attention. It was likely that the basis for these changes was methanol, the cosolvent of CP EC, because when the purified CP was stored in methanol at 50 degrees C for 2 weeks, CP drop and toxic potentiation similar to those observed in CP EC also appeared. The major products of the CP-methanol reaction mixture were isolated and identified by HPLC and GC-MS, respectively, and their inhibitory potentials against AChE and effectiveness as potentiators were assessed. Following redetermination of the main product (O, S-dimethyl-[(2,2,2)-trichloro-1-methoxyethyllphosphoramidothioate (MCP)) and high anti-AChE material (methamidophos), which were preconfirmed in the reaction mixture in CP EC, it was successfully demonstrated that the majority of CP in the formulation had been transformed to a new stable compound, MCP. Meanwhile, formation of another product, methamidophos, resulted in toxic potentiation.
• ——
  作者：TEICHMANN H.、 SCHNELL M.、 STEINKE W.、 GRIMMER F.

  DOI：——

  日期：——
• Design, Synthesis, and Biological Evaluation of New 5-HT₄ Receptor Agonists: Application as Amyloid Cascade Modulators and Potential Therapeutic Utility in Alzheimer’s Disease
  作者：Olivier Russo、Marthe Cachard-Chastel、Céline Rivière、Mireille Giner、Jean-Louis Soulier、Magali Berthouze、Tristan Richard、Jean-Pierre Monti、Sames Sicsic、Frank Lezoualc’h、Isabelle Berque-Bestel

  DOI：10.1021/jm801327q

  日期：2009.4.23

  based on the scaffold of ML10302, a highly specific and partial 5-HT4R agonist, were efficiently prepared by parallel supported synthesis and their binding affinities and agonist activities evaluated. Furthermore, we showed that, in vivo, the two best candidates exhibited neuroprotective activity by increasing the level of the soluble form of the amyloid precursor protein (sAPPα) in the cortex and hippocampus

  5-羟色胺5-HT 4受体（5-HT 4 R）激动剂特别适合治疗阿尔茨海默氏病，因为它们具有缓解认知缺陷和调节淀粉样β蛋白（Aβ）产生的能力。然而，尽管迄今为止合成了范围广泛的5-HT 4 R激动剂，但仍然缺乏有效的和选择性的5-HT 4 R激动剂。在本研究中，基于ML10302支架的分子的两个文库，即高度特异性和部分5-HT 4R激动剂可通过平行支持的合成方法有效制备，并评估其结合亲和力和激动剂活性。此外，我们表明，在体内，通过增加小鼠皮质和海马中淀粉样前体蛋白（sAPPα）的可溶形式的水平，两个最佳候选物表现出神经保护活性。有趣的是，这些化合物中的一种还可以在体外抑制Aβ原纤维的形成。