2,4-二氨基-5-苯基噻唑氢溴酸 | 6020-54-8

• 物质功能分类: 医药中间体 - 原料药中间体
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 2,4-二氨基-5-苯基噻唑氢溴酸
• 中文别名: 2,4-二氨基-5-苯基噻唑氢溴酸盐酸盐；5-苯基-2,4-噻唑二胺氢溴酸盐
• 英文名称: 5-phenyl-thiazole-2,4-diyldiamine; hydrobromide
• 英文别名: 5-Phenyl-thiazol-2,4-diyldiamin; Hydrobromid；2,4-diamino-5-phenylthiazole hydrobromide；Hydron;5-phenyl-1,3-thiazole-2,4-diamine;bromide；hydron;5-phenyl-1,3-thiazole-2,4-diamine;bromide
• CAS: 6020-54-8
• 化学式: BrH*C₉H₉N₃S
• 分子量: 272.168
• InChiKey: JFSDUFWHNHMSRU-UHFFFAOYSA-N

物化性质

• 熔点：
  283 °C
• 溶解度：
  DMSO（少量）、甲醇（少量）、水（少量）
• 稳定性/保质期：

  在常温常压下，该物质保持稳定。

计算性质

• 辛醇/水分配系数(LogP)：
  2.55
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  93.2
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 危险等级：
  6.1(b)
• 危险品运输编号：
  3249
• 海关编码：
  2934100090
• 包装等级：
  III
• 危险类别：
  6.1(b)
• 安全说明：
  S24/25

制备方法与用途

用途

5-苯基-2,4-噻唑二胺氢溴酸盐是一种杂环有机化合物，可作为医药中间体使用。

反应信息

• 作为反应物：
  描述：

  甲氧基乙酰氯 、 2,4-二氨基-5-苯基噻唑氢溴酸 在 吡啶 作用下， 反应 3.0h， 以65%的产率得到2-Methoxy-N-[2-(2-methoxy-acetylamino)-5-phenyl-thiazol-4-yl]-acetamide
  参考文献：
  名称：

  Novel antiallergic and antiinflammatory agents. Part I: Synthesis and pharmacology of glycolic amide derivatives

  摘要：

  A series of mono-glycoloylamino derivatives was synthesized by treatment of the corresponding aromatic monoamine derivatives with glycoloyl chloride derivatives in pyridine or dichloromethane, in the presence of a base such as triethylamine or pyridine. Hydrolysis of acetoxy compounds in aqueous ammonia and methanol solution produced hydroxy derivatives with ease. These compounds were tested in the rat PCA (passive cutaneous anaphylaxis) assay by oral administration. Thiazole and thiadiazole derivatives showed moderate inhibition in this assay. In contrast, benzothiazole and benzonitrile derivatives exhibited marked inhibition. In particular, compound 5t also showed marked inhibition of eosinophil adhesion to TNF (tumor necrosis factor) -alpha-treated HUVEC (human umbilical vein endothelial cells) in the range of 10(-8)-10(-5) M. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(98)00065-0

文献信息

• Oxazolidinone combinatorial libraries, compositions and methods of preparation
  申请人：——

  公开号：US20020183371A1

  公开（公告）日：2002-12-05

  Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

  本发明提供了噁唑烷酮及其合成方法。还提供了包含噁唑烷酮的组合式文库以及制备这些文库的方法。此外，还提供了制备生物活性噁唑烷酮以及包含这些噁唑烷酮的药用组合物的方法。文库制备方法包括将噁唑烷酮附着到固体支持上。在一种实施例中，化合物制备方法涉及使用亚胺磷酰胺与含羰基的聚合物支持物反应。
• Thiazole derivatives to counter advanced glycation
  申请人：Avon Products, Inc.

  公开号：EP1543824A2

  公开（公告）日：2005-06-22

  Methods are disclosed for improving the appearance of skin by topical administration of thiazole derivatives which inhibit the formation of advanced glycation endproducts, break advanced glycation endproduct-associated crosslinks, and inhibit the function of glucose oxidase. Cosmetic and pharmaceutical compositions comprising the thiazole derivatives are also disclosed.

  本发明公开了通过局部施用噻唑衍生物来改善皮肤外观的方法，噻唑衍生物可抑制高级糖化终产物的形成、断裂高级糖化终产物相关的交联以及抑制葡萄糖氧化酶的功能。此外，还公开了包含噻唑衍生物的化妆品和药物组合物。
• L-FABP IMMUNOASSAY METHOD AND ASSAY REAGENT USED IN SAID METHOD
  申请人：Sekisui Medical Co., Ltd.

  公开号：EP3264083A1

  公开（公告）日：2018-01-03

  A problem to be solved by the invention is to provide an immunological measurement method for L-FABP in a sample using an anti-L-FABP antibody having a detection sensitivity equal to or greater than that of an existing pharmaceutical product for in-vitro diagnosis and having a favorable correlation. The problem is solved by a method of detecting L-FABP (liver-type fatty acid binding protein) in a sample with an anti-L-FABP antibody, comprising the step of bringing an anti-L-FABP antibody and a compound having a partial structure of NH2-C=N- and a cyclic structure in a molecule into contact with a sample suspected of containing L-FABP.

  本发明要解决的问题是提供一种使用抗 L-FABP 抗体检测样品中 L-FABP 的免疫学测 量方法，该方法的检测灵敏度等于或高于现有体外诊断用药品的检测灵敏度，并且具有 良好的相关性。抗 L-FABP 抗体检测样品中 L-FABP（肝脏型脂肪酸结合蛋白）的方法解决了这一问 题，该方法包括以下步骤：将抗 L-FABP 抗体和分子中部分结构为 NH2-C=N- 和环状结构的化合物 与疑似含有 L-FABP 的样品接触。
• IMMUNOASSAY METHOD AND ASSAY REAGENT USED IN SAID METHOD
  申请人：Sekisui Medical Co., Ltd.

  公开号：EP3264084A1

  公开（公告）日：2018-01-03

  An object of the present invention is to provide a more accurate and sensitive measurement method lowering the possibility of occurrence of nonspecific reaction in immunological measurement of L-FABP. More specifically, an object is to provide a measurement method that is accurate and sensitive even when the concentration of an analyte is low (e.g., an L-FABP concentration is around the normal value). In an immunological measurement method of L-FABP using an anti-L-FABP antibody, nonspecific reaction can easily be suppressed by a polypeptide consisting of amino acids No. 419 to No. 607 of the amino acid sequence of DnaK, a heat shock protein (HSP), derived from E. coli as set forth in SEQ ID NO: 1 or a polypeptide having at least 90 % sequence identity with the polypeptide even in highly sensitive measurement.

  本发明的目的是提供一种更准确、更灵敏的测量方法，以降低在免疫学测量 L-FABP 时发生非特异性反应的可能性。更具体地说，本发明的目的是提供一种即使在分析物浓度较低时（如 L-FABP 浓度在正常值附近）也能准确灵敏地进行测量的方法。在使用抗 L-FABP 抗体的 L-FABP 免疫学测量方法中，即使在高灵敏度测量中，由 SEQ ID NO: 1 所述大肠杆菌热休克蛋白（HSP）DnaK 的氨基酸序列第 419 号至第 607 号氨基酸组成的多肽或与该多肽具有至少 90 % 序列相同性的多肽也能很容易地抑制非特异性反应。
• Image making medium
  申请人：——

  公开号：US20030035917A1

  公开（公告）日：2003-02-20

  The invention relates to an image support medium for creation of an aesthetic image that is an work or object for display. This support medium includes a polymer in an amount sufficient to enable the image to have at least one aesthetic element. In different embodiments, the image support medium is an image support stabilizer, the polymer is a synthetic absorbent or conductive polymer, or the polymer is a transparent or synthetic translucent polymer and a property of this transparent or translucent polymer is enhanced to facilitate the creation or preservation of the image by at least one stabilizer. The invention also relates to a method for preparing this image support medium. The method includes forming a reaction mixture comprising a monomer in an amount sufficient to provide or enable the image to have an aesthetic element, and processing the reaction mixture into a 2- or 3-dimensional shape.

  本发明涉及一种图像支持介质，用于创建作为作品或展示对象的美学图像。这种支撑介质包括一种聚合物，其用量足以使图像具有至少一种审美元素。在不同的实施例中，图像支持介质是一种图像支持稳定剂，聚合物是一种合成的吸收性或导电性聚合物，或者聚合物是一种透明或合成的半透明聚合物，并且这种透明或半透明聚合物的特性被至少一种稳定剂增强，以促进图像的创建或保存。本发明还涉及一种制备这种图像支持介质的方法。该方法包括形成由单体组成的反应混合物，其用量足以提供或使图像具有美学元素，并将反应混合物加工成 2 维或 3 维形状。

表征谱图