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卢帕他定中间体5-甲基吡啶-3-羧酸的合成工艺改进 被引量：3

Improved Synthesis of 5-Methylpyridine-3-carboxylic Acid, the Intermediate of Rupatadine
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摘要 目的:改进5-甲基吡啶-3-羧酸的合成工艺。方法:以3,5-二甲基吡啶为原料,经KMnO4氧化得卢帕他定中间体5-甲基吡啶-3-羧酸,经正交试验,优化工艺。结果:得出较佳的工艺条件,提高了产率,收率可达51％。结论:该方法易于工业化生产。 Objective: To improve the synthesis of 5-methylpyridine-3-carboxylic acid. Methods: 5-methylpyridine-3-carboxylic acid, the intermediate of Rupatadine, was synthesized from 3,5-lutidine by the reaction of oxidation with KMnO4. The reaction conditions were optimized with the orthogonal matrix. Results: The suitable conditions were obtained, and the yield was 51 % . Conclusion: The process is practical and easy to popularize in industry.
作者 王震宇 朱雄 王尔华
机构地区 中国药科大学医药化工研究所
出处 《药学进展》 CAS 2005年第1期31-33,共3页 Progress in Pharmaceutical Sciences
关键词 3 5-二甲基吡啶 5-甲基吡啶-3-羧酸 氧化 正交试验 合成 3,5-Lutidine 5-Methylpyridine-3-carboxylic acid Oxidation Orthogonal test Synthesis
分类号 TQ25 [化学工程—有机化工]
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参考文献5

  • 1Inaki L, Manuel M, Julian G, et al. New selective histamine H, receptor and platelet-activating factor (PAF) antagonist[J]. Drugs of Today, 2003, 39(6):451-468.
  • 2Evan P K, Shiuh-Tzung L, Kannappan C, et al. A General Synthesis of Substituted Fluorenones and Azafuwrenones[ J]. J Org Chem, 1988, 53:3513-3521.
  • 3Elena C, Manuel M, Marta G, et al. [ (3-Pyridylakyl) piperidylidene] benzocyeloheptapyridine Derivatives as Dual Antagonists of PAF and Histamine[J]. J Med Chem, 1994, 37: 2697-2730.
  • 4Andrests K. Microbiological Oxidation of Methyl Gmoups inHeterocydes[P]. US 5104798, 1992-04-14.
  • 5Joseph E, Toomey Jr. Electrochemical Oxidation of Pyridine bases[P]. US 4482439,1984-11-13.

同被引文献15

  • 1张万金,罗艳,张燕梅.卢帕他定的合成[J].中国医药工业杂志,2006,37(7):433-435. 被引量：7
  • 2卜今,陈志强.卢帕他定——新型的组胺H1受体和血小板活化因子受体双重拮抗剂[J].中国中西医结合皮肤性病学杂志,2006,5(3):182-184. 被引量：7
  • 3Izquierdo I, Merlos M, Garcia - Rafanell J. Rupatadine : a new selective histamine H1 receptor and platelet -activating factor(PAF) antagonist. A review of pharmacological profile and clinical management of allergic rhinitis. Drugs Today (Barc) ,2003,39 ( 6 ) :451
  • 4Solans A, Izquierdo I, Donado E, et al. Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady - state levels : a randomized, open - label, two - way, crossover, Phase Ⅰ study. Clin Ther,2008,30 (9) : 1639
  • 5John G, Dan S, David D,etal. Degradation product of loratadine[J].Journal of Pharmaceutical and Biomedical Analysis , 2007, 43: 1191-1192.
  • 6Carceller E, Recasens N, etal. 8 - chloro- 11 - [ 1 - [ (5 - met hyl - 3 - pyridyl ) -methyl ] - 4 - piperidyliden] 6, 11 - dihydro - 5H - benzo [5,6]cyclohepta [1,2- b]pyridine [P]. US5407941,1995-9-18.
  • 7Carceller E, Merlos N, et al. [(3- pridylalakyl) piperidy lidene] benzocyclo heptapyridine Derivatives as Dual Antagonists of PAF and Histamine [J]. J Med Chem,1994,37(17) :2697-2703.
  • 8Garcia-Rafanell J.Rupatadine fumarate.UR-12592 fumarate.Antiallergic.Histamine and PAF antagonist[J].Drugs Future,1996,21(10):1032-1036.
  • 9Bryant HU,Grese TA.Methods for inhibiting bone loss using pyrolidine and piperidine substituted benzopyrans:US,5407947[P].1995-04-18.(CA 1995,123:988)
  • 10Carceller E,Merlos M,Giral M,et al.[(3-Pyridylalkyl)-piperidylidene] benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine[J].J Med Chem,1994.37(17):2697-2703.

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药学进展
2005年 第1期

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