sodium 5-aminosalicylate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: sodium 5-aminosalicylate
• 英文别名: sodium 5-aminosalicylicate；5-aminosalicylic acid sodium salt；Sodium;4-amino-2-carboxyphenolate；sodium;4-amino-2-carboxyphenolate
• 化学式: C₇H₆NO₃*Na
• 分子量: 175.119
• InChiKey: AWDRBBZJLVNKQS-UHFFFAOYSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  -3.66
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  86.4
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  sodium hydrogensulfite 、 sodium 5-aminosalicylate 生成 disodium 5-amino-2-hydroxy-3-sulfonatobenzoate
  参考文献：
  名称：

  The Piria Reaction. III.¹ Mechanism Studies²

  摘要：

  DOI：

  10.1021/ja01293a011
• 作为试剂：
  描述：

  对乙酰氨基酚 、 sodium hydroxide 、 二氧化碳 在 水 、 sodium 5-aminosalicylate 作用下， 80.0~180.0 ℃ 、266.64 MPa 条件下， 反应 3.0h， 以to obtain the product of 5-aminosalicylic acid的产率得到5-氨基水杨酸
  参考文献：
  名称：

  Preparation of 5-aminosalicylic acid by gas phase catalytic carboxylation

  摘要：

  本发明公开了一种气相催化羧化制备5-氨基水杨酸的方法，其特征在于，在催化剂存在下，将二氧化碳引入对乙酰氨基酚和碱性化合物的系统中，在150℃～220℃和0.5～5.0 MPa的温度和压力下进行气相催化羧化反应，形成5-氨基水杨酸盐，然后分离粗品5-氨基水杨酸盐，酸化制备5-氨基水杨酸（5-ASA）。由于气相催化反应取代了固相热化学反应，因此在工艺流程、反应条件、产品质量和能耗方面都得到了显著的改善。此外，该反应时间短，选择性好，产率高，反应过程中不会产生废物，适用于工业生产。

  公开号：

  US09067867B2

文献信息

• PREPARATION OF 5-AMINOSALICYLIC ACID BY GAS PHASE CATALYTIC CARBOXYLATION
  申请人：Li Guangxing

  公开号：US20130281730A1

  公开（公告）日：2013-10-24

  Disclosed is a process for preparing 5-aminosalicylic acid by gas phase catalytic carboxylation, characterized in that carbon dioxide is introduced into a system of p-acetaminophenol and a basic compound at a temperature of 150° C.˜220° C. and a pressure of 0.5˜5.0 MPa in the presence of a catalyst, so as to carry out a gas phase catalytic carboxylation reaction to form a 5-aminosalicylate, and the crude product 5-aminosalicylate is separated, and then acidified to prepare 5-aminosalicylic acid (5-ASA). Since the gas phase catalytic reaction replaces a solid phase thermo-chemical reaction, the reaction is significantly improved in terms of the process flow, reaction conditions, product quality and energy consumption. In addition, the reaction has a short reaction time, good selectivity, high yield and no formation of wastes during the reaction, and is suitable for industrial production.

  本发明揭示了一种通过气相催化羧化反应制备5-氨基水杨酸的方法，其特征在于，在催化剂的存在下，将二氧化碳引入对乙酰氨基酚和碱性化合物的体系中，在150℃~220℃和0.5~5.0 MPa的温度和压力下进行气相催化羧化反应，形成5-氨基水杨酸盐，并将粗品5-氨基水杨酸盐分离，然后酸化以制备5-氨基水杨酸（5-ASA）。由于气相催化反应取代了固相热化学反应，因此在工艺流程、反应条件、产品质量和能源消耗方面，反应显著改善。此外，反应时间短，选择性好，收率高，反应期间不产生废物，适用于工业生产。
• Colon-specific drug release system
  申请人：——

  公开号：US20020044975A1

  公开（公告）日：2002-04-18

  A system for releasing a drug specifically in the colon of the gastrointestinal tract, which comprises a drug (b) coated with an organic acid-soluble polymer material (a), and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract; a colon-specific drug release oral preparation, which comprises a composition comprising a drug (b) coated with an organic acid-soluble polymer material (a) and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract, said composition being coated with an enteric coating polymer material (d). The invention provides a drug release system and a preparation which utilize enterobacteria, which do not form harmful substances due to the release-starting mechanism, show rapid degradation, and have higher colon specificity.

  一种用于在胃肠道结肠特异性释放药物的系统，包括一种药物（b），其覆盖有一种有机酸溶解性聚合物材料（a），以及一种糖类（c），通过肠道下部的肠道菌作用迅速产生有机酸; 一种结肠特异性药物释放口服制剂，包括一种组成物，其包括一种药物（b），其覆盖有一种有机酸溶解性聚合物材料（a）和一种糖类（c），通过肠道下部的肠道菌作用迅速产生有机酸，该组成物覆盖有一种肠溶涂层聚合物材料（d）。该发明提供了一种药物释放系统和制剂，利用肠道菌，由于释放启动机制不会产生有害物质，显示出快速降解和更高的结肠特异性。
• COLON-SPECIFIC DRUG RELEASE SYSTEM
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP0759303A1

  公开（公告）日：1997-02-26

  A system for releasing a drug specifically in the colon of the gastrointestinal tract, which comprises a drug (b) coated with an organic acid-soluble polymer material (a), and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract; a colon-specific drug release oral preparation, which comprises a composition comprising a drug (b) coated with an organic acid-soluble polymer material (a) and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract, said composition being coated with an enteric coating polymer material (d). The invention provides a drug release system and a preparation which utilize enterobacteria, which do not form harmful substances due to the release-starting mechanism, show rapid degradation, and have higher colon specificity.

  一种在胃肠道结肠中特异性释放药物的系统，它包括涂有有机酸可溶性聚合物材料（a）的药物（b）和在胃肠道下部肠杆菌作用下迅速产生有机酸的糖类（c）；一种结肠特异性药物释放口服制剂，它包括一种组合物，该组合物包含涂有有机酸溶性聚合物材料（a）的药物（b）和在胃肠道下部肠杆菌作用下迅速产生有机酸的糖类（c），所述组合物上涂有肠道包衣聚合物材料（d）。 本发明提供了一种利用肠杆菌的药物释放系统和制剂，这种药物释放系统和制剂不会因释放启动机制而形成有害物质，可快速降解，并具有较高的结肠特异性。
• COLORING COMPOSITION, INKJET RECORDING INK, AND INKJET RECORDING METHOD
  申请人：Fujifilm Corporation

  公开号：EP3202856A1

  公开（公告）日：2017-08-09

  Provided are a coloring composition including a xanthene compound which is soluble in water and a compound represented by the following Formula (A); an ink jet recording ink; and an ink jet recording method. In Formula (A), Q represents a benzene ring or a naphthalene ring. P1 represents -CO2M or -SO3M. Ra1 represents a substituent, and Ra2, Ra3, and Ra4 each independently represent a hydrogen atom or a substituent. na represents an integer of 0 to 3. When na is 2 or more, a plurality of Ra1's may be the same as or different from each other. M represents a counter cation.

  本发明提供了一种着色组合物，其中包括可溶于水的呫吨化合物和下式（A）代表的化合物；一种喷墨记录墨水；以及一种喷墨记录方法。 式（A）中，Q 代表苯环或萘环。P1 代表-CO2M 或-SO3M。Ra1 代表取代基，Ra2、Ra3 和 Ra4 各自独立地代表氢原子或取代基。M 代表反阳离子。
• Method of inhibiting the production and/or effects of intestinal pro-inflammatory cytokines, prostaglandins and others
  申请人：——

  公开号：US20030119792A1

  公开（公告）日：2003-06-26

  The present invention shows that UR-12746-S, a novel locally acting compound which combines 5-ASA (an anti-inflammatory) and UR-12715 (a PAF antagonist) through an azo link, and analogous azo derivatives of 5-aminosalicylic acid compounds are able to inhibit cytokine production (IL-8, IL-1&bgr; and TNF-&agr;) in vitro, and are shown to have intestinal anti-inflammatory activity in vivo. Moreover, daily oral administration of azo derivatives of 5-aminosalicylic acid sodium salts are able to alleviate and/or prevent relapse of inflammatory disease induced in colitic rats. This beneficial effect is evidenced by a significant reduction in colonic myeloperoxidase activity and by a significant decrease in colonic IL-1&bgr; and TNF-&agr;.

  本发明表明，UR-12746-S（一种通过偶氮连接将 5-ASA（一种抗炎剂）和 UR-12715（一种 PAF 拮抗剂）结合在一起的新型局部作用化合物）和 5-氨基水杨酸化合物的类似偶氮衍生物能够在体外抑制细胞因子（IL-8、IL-1&bgr; 和 TNF-&agr;）的产生，并在体内具有肠道抗炎活性。此外，每天口服 5- 氨基水杨酸钠盐的偶氮衍生物能够减轻和/或防止结肠炎大鼠的炎症复发。结肠髓过氧化物酶活性的显著降低以及结肠 IL-1&bgr; 和 TNF-&agr; 的显著减少证明了这种有益作用。

表征谱图