4-氧代-10-丙基-6,7,8,9-四氢苯并[g]苯并吡喃-2-羧酸 | 60400-86-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 萘并吡喃类
• 中文名称: 4-氧代-10-丙基-6,7,8,9-四氢苯并[g]苯并吡喃-2-羧酸
• 英文名称: 6,7,8,9-Tetrahydro-4-oxo-10-propyl-4H-naphtho[2,3-b]-pyran-2-carboxylic acid
• 英文别名: Procromil；4-oxo-10-propyl-6,7,8,9-tetrahydrobenzo[g]chromene-2-carboxylic acid
• CAS: 60400-86-4
• 化学式: C₁₇H₁₈O₄
• 分子量: 286.328
• InChiKey: DLKZWVIRKURGIR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  63.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-oxo-10-(2-oxopropyl)-6,7,8,9-tetrahydro-4H-naphtho[2,3-b]pyran-2carboxylic acid 在 sodium borohydrid 作用下， 以 sodium hydroxide 、 水 为溶剂， 生成 4-氧代-10-丙基-6,7,8,9-四氢苯并[g]苯并吡喃-2-羧酸
  参考文献：
  名称：

  Tricyclic mono-chromone-2-carboxylic acids

  摘要：

  描述了化合物的化学式I，其中R.sub.3代表氢或烷基C 1至6，R.sub.5代表氢，羟基，烷氧基C 1至6，烷酰氧基C 2至6，烯酰氧基C 2至6，硝基，-NR.sub.1 R.sub.2，卤素，烷基C 1至6，羟基烷基C 1至6，或羟基烷氧基C 1至6，相邻的X、Y和Z形成一个--(CH.sub.2).sub.4--，--CH.dbd.CH--CH.dbd.CH--或--O(CH.sub.2).sub.3--链，每个链可选择地被一个或两个C 1至6烷基取代，其余的取代基X或Z代表烯基C2至6，可选择地被苯基；卤素；或烷基C 1至9，可选择地被羟基，卤素，羰基氧，苯基或烷氧基C 1至6中的一个或多个基团取代，或者，当相邻的X、Y和Z形成一个链，被一个或两个C 1至6烷基取代，其余的取代基X或Z可以是氢，R.sub.1和R.sub.2，可以相同也可以不同，分别是氢或烷基C 1至6，以及它们的药学上可接受的衍生物。还描述了制备这些化合物的方法和含有这些化合物的药物，例如抗过敏组合物。

  公开号：

  US04159273A1

文献信息

• Improved process for the production of 6,7,8,9-tetrahydro-5-hydroxy-4-oxo-10-propyl-4H-naphtho(2,3-b)pyran-2-carboxylic acid
  申请人：FISONS plc

  公开号：EP0008167A1

  公开（公告）日：1980-02-20

  There is described an improved process for the production of the biologically active compound 6,7,8,9-tetra- hydro-5-hydroxy-4-oxo-10-propyl-4H-naphtho [2,3-b] pyran-2-carboxylic acid of the formula which comprises hydrolysis of 6,7,8,9-tetrahydro-5-diazo-4-oxo-1 0-propyl-4H-naphtho [2,3-b] pyran-2-carboxylic acid or an ester thereof, characterised in that the hydrolysis is carried out in the presence of less than 10% w/w nitrite anion. The diazo compound may be made by diazotisation of 6,7,8,9-tetrahydro-5-amino-4-oxo-10-propyl-4H-naphtho [2,3-b] pyran-carboxylic acid or an ester thereof in the presence of nitrous acid.

  本发明描述了一种生产生物活性化合物 6,7,8,9-四氢-5-羟基-4-氧代-10-丙基-4H-萘并[2,3-b]吡喃-2-羧酸的改进工艺，其式如下 其中包括 6,7,8,9-四氢-5-重氮-4-氧代-1 0-丙基-4H-萘并[2,3-b]吡喃-2-羧酸或其酯的水解，其特征在于水解是在亚硝酸阴离子少于 10%w/w的存在下进行的。重氮化合物可通过 6，7，8，9-四氢-5-氨基-4-氧代-10-丙基-4H-萘并[2，3-b]吡喃羧酸或其酯在亚硝酸存在下的重氮化反应制得。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• LYOPHILIZATION PROCESS AND PRODUCTS OBTAINED THEREBY
  申请人：Scidose, Llc

  公开号：EP1954244A1

  公开（公告）日：2008-08-13
• CONTROLLED ABSORPTION WATER-SOLUBLE PHARMACEUTICALLY ACTIVE ORGANIC COMPOUND FORMULATION FOR ONCE-DAILY ADMINISTRATION
  申请人：STI Pharma, LLC

  公开号：EP2717860A1

  公开（公告）日：2014-04-16
• Lyophilization process and products obtained thereby
  申请人：Palepu R. Nageswara

  公开号：US20070116729A1

  公开（公告）日：2007-05-24

  A lyophilization process which comprises dissolving a material in one or more solvents for said material to form a solution; forcing said material at least partially out of solution by combining the solution and a non-solvent for the material, which non-solvent is miscible with the solvent or solvents used and wherein said non-solvent is volatilizable under freeze-drying conditions. In addition, for hydrophobic and/or lipophilic materials, the anti-solvent can be omitted, and the solution of the material in the solvent can be subjected directly to freeze drying. The lyophilizates can then be reconstituted with typical aqueous diluent in the case of hydrophilic materials. Hydrophobic and or lipophilic materials can be initially reconstituted with propylene glycol and/or polyethyleneglycol to form a high concentration solution therein and this is further diluted for use with a diluent of Intralipid, plasma, serum, or even whole blood.