他折洛芬 | 85702-89-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 中文名称: 他折洛芬
• 中文别名: 达泽布洛芬
• 英文名称: Tazeprofen
• 英文别名: 2-(2-phenyl-1,3-benzothiazol-6-yl)propanoic acid
• CAS: 85702-89-2
• 化学式: C₁₆H₁₃NO₂S
• 分子量: 283.3
• InChiKey: DPRKTNKWAXPYNW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  78.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  他折洛芬 在 ammonium peroxydisulfate 、 disodium hydrogenphosphate 、 3,8-二溴菲罗啉 、 triethylamine tris(hydrogen fluoride) 、 silver(l) oxide 作用下， 以 1,2-二氯乙烷 、 氯苯 为溶剂， 以47 %的产率得到
  参考文献：
  名称：

  脂肪族羧酸的脱羧亲核氟化

  摘要：

  在此，我们提出了用银催化剂对羧酸进行脱羧亲核氟化。该策略使得能够在温和条件下合成无数多样且有价值的氟化基序，表现出良好的官能团耐受性和后期官能化的实用性。与传统的亲电氟化相比，这种亲核方法利用更容易获得的亲核氟化试剂，在成本效益、广泛的底物范围和官能团兼容性方面具有显着的优势。

  DOI：

  10.1021/acs.orglett.4c01185

文献信息

• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• ESTER-SUBSTITUTED THIENOTRIAZOLODIAZEPINE COMPOUNDS AND THEIR MEDICINAL USE
  申请人：Yoshitomi Pharmaceutical Industries, Ltd.

  公开号：EP0316456A1

  公开（公告）日：1989-05-24

  Ester-substituted thienotriazolodiazepine compoundsre- presented by general formula (1) (wherein Ar represents pyridyl, phenyl or phenyl having one to three same or different substituents R1 and R3, which may be the same or different, each represents hydrogen or C1-4 alkyl, R2 represents hydrogen, C1-4 alkyl ortrifluoromethyl, and R represents C1-18 straight or branched-chain alkyl, C2-18 straight or branched-chain alkenyl, aryl, aryl having one to three same or different substituents, aralkyl, aralkyl having one or more same or different substituents on the aromatic ring or alkyl chain, aralkyl fused with a heterocyclic ring, aralkenyl, aralkenyl having one to three same or different substituents, heteroarylalkyl, or optionally substituted indenylalkyl), pharmaceutically acceptable salts thereof, and their medicinal use are disclosed. These compounds are useful as drugs for treating various diseases induced by thrombocyte activator.

  由通式(1)表示的酯取代的噻吩三唑并二氮杂卓化合物 (其中 Ar 代表吡啶基、苯基或具有一至三个相同或不同取代基的苯基，R1 和 R3 可以相同或不同，各自代表氢或 C1-4 烷基，R2 代表氢、C1-4 烷基或三氟甲基，R 代表 C1-18 直链或支链烷基、C2-18 直链或支链烯基、芳基、具有一至三个相同或不同取代基的芳基、烷基、在芳香环或烷基链上具有一个或多个相同或不同取代基的烷基、与杂环融合的烷基、芳烯基、具有一至三个相同或不同取代基的芳烯基、杂芳烷基或任选取代的茚基烷基）、其药学上可接受的盐及其药用用途均已公开。这些化合物可作为治疗血小板活化剂诱发的各种疾病的药物。
• 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。
• Dérivés du benzothiazole, leur procédé de préparation et leurs applications en thérapeutique
  申请人：Albert ROLLAND S.A. Société dite

  公开号：EP0017543B1

  公开（公告）日：1983-09-28