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醋氯芬酸的合成 被引量:3

Synthesis of Aceclofenac
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摘要 醋氯芬酸(aceclofenac,1),化学名为2-(2,6-二氯苯胺基)苯乙酰氧基乙酸,由西班牙Almirall-Prodesfarma制药公司研发,1992年首先在西班牙上市,1998年收入欧洲药典和英国药典。本品是口服强效非甾体抗炎药,适用于治疗各种风湿性关节炎、类风湿性关节炎、骨关节炎和脊椎炎,也适用于各种疾病引起的疼痛和发热,是治疗急慢性疼痛、抗炎的安全可靠的药物。 Aceclofenac was synthesized from sodium diclofenac and t-butyl chloroacetate by esterification and acidolysis with an overall yield of 81%.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2008年第6期408-409,共2页 Chinese Journal of Pharmaceuticals
关键词 二氯苯 类风湿性关节炎 非甾体抗炎药 合成 乙酰氧基 制药公司 骨关节炎 aceclofenac non-steroid anti-inflammatory drugs (NSAIDs) synthesis
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参考文献7

  • 1苏杰,张钧寿,吴葆金,张秀芝.醋氯芬酸缓释片的研制[J].中国现代应用药学,2000,17(1):19-22. 被引量:14
  • 2唐华,王红刚,张晓龙,刘明言.新型非甾体抗炎药醋氯芬酸的研究进展[J].西北药学杂志,2006,21(1):47-48. 被引量:15
  • 3Casas AV. 2- [ (2,6-Dichlorophenyl) amino]phenylacetoxyl derivatives and therapeutic compositions containing same: US, 4548952 [P]. 1985-10-22. (CA 1986, 104: 88301).
  • 4Kim JC, Namgoong SK, Chae JK, et al. Haloethyl-2- [ (2,6-dichlorophenyl) amino] phenylacetoxyacetate derivatives and their use as an intermediate to synthesize aceclofenac: WO, 9962865 [P]. 1999-12-09. (CA 2000, 132: 22759).
  • 5Schickaneder H, Nikolopoulos A, Murphy T. Process for the preparation of aceclofenac: WO, 9955660 [P]. 1999-11-04. (CA 1999, 131: 322421).
  • 6姜妮丽,范朋高,程国侯.醋氯芬酸的合成[J].中国医药工业杂志,2005,36(7):393-394. 被引量:9
  • 7Smith MB, March J. March's Advanced Organic Chemistry [M]. 5th ed, New York: John Wiley & Sons, Inc., 2001: 473.

二级参考文献25

  • 1曹于平 杨英莉 戴岳 等.醋氯芬酸解热、镇痛及抗炎作用[J].中国药科大学学报,1997,28:18-20.
  • 2Vila Cagas A. Ester of 2- [ (2,6-dichloroanilino) phenyl]acetic acid with glycolic acid[P]. ES: 520813, 1984-05-16.(CA 1984, 104: 88301)
  • 3Vila Cagas A. 2- [ (2,6-Dichlorophenyl) amino] phenylacetoxyacetyl derivatives and therapeutic composition containing same [P]. US: 4548952, 1985-10-22.
  • 4Kim JC, Namgoong SK. Haloethyl-2- [ (2,6-dichlorophenyl)amino]phenylacetoxyacetate derivatives and their use as an intermediate to synthesize aceclofenac [P]. WO: 9962865,1999-12-09. (CA 1999, 132: 22759)
  • 5Schickaneder H, Nikolopoulos A, Murphy T. Process for the preparation of aceclofenac [P]. WO: 9955660, 1999-11-04.(CA 1999, 131: 322421)
  • 6Blot L. Effects of diclofenac, aceclofenac and meloxicam on the metabolism of proteoglycans and hyaluronin in osteoarthritic human cartilage [ J ]. Br J Pharmcol,2000,131 (7) :1413 - 1421.
  • 7Gonzalez - Mvaro I, et al. Aceclofenac, a new nonstemidal antiinflammatory drug,decreases the expression and function of some adhesion molecules on human neutrophils[J]. Rheumatol Int, 1996,23 (4) :723.
  • 8Kornasoff D, et al. The efficacy and tolerability of aceclofenac compared to indomethacin in patients with rheumatoid arthritis [ J ]. Rheumatol Int, 1996,16 (6) :225.
  • 9Martin - Mola E, et al. Aceclofenac in comparison to ketoprofen in the treatment of rheumatoid arthristis [ J ]. Rheumatol Int,1995,15(3) :111.
  • 10Y. S. E1 - Saharty, M. Refaat, et al. Stability - Indicating Spectrophotometric and Densitometric Methods for Determination of Aceclofenac [ J ]. Drug Development and Industrial Pharmacy,2002,28 (5) :571 - 582.

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