目的合成非甾体抗炎药物替诺昔康。方法以丙烯腈为原料经6步反应制得本品,光谱确证结构。结果对各步反应条件进行了优化,收率较文献有所提高或与文献相近。结论本合成路线简便可行,适合工业化生产。
Abstract
OBJECTIVE To synthesize tenoxicam,a nonsteroidal antiinflammatory drug. METHOD The target compound was prepared through six steps reaction from acrylonitrile.Its structure was confirmed by IR,1HNMR,MS and elemental analysis respectively. RESULT The reaction method was improved and the yield was higher or equal to that reported. CONCLUSION The synthesis route was convenient for the tenoxicam synthesis and the process may be used in industry.
关键词
替诺昔康 /
非甾体抗炎药 /
合成
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Key words
tenoxicam /
NSAIDs /
synthesis
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参考文献
[1]Todd PA,Clissold SP.Tenoxicam,An update of its pharmacology and therapeutic efficacy in rheumatic diseases[J]. Drugs, 1991,41(4):625.
[2]Gonzalez JP,Todd PA.Tenoxicam,A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy[J]. Drugs, 1987,34(3):289.
[3]Binder D,Hromatka O,Geissler F, et al. Analogues and derivatives of tenoxicam.1.synthesis and antiinflammatory activity of analogues with different residues on the ring nitrogen and the amide nitrogen[J]. J Med Chem, 1987,30:678.
[4]Corral C,Lissavetzky J,Alvarez-insua AS, et al. Synthesis of 3-mercaptothiophene-2-and 4-carboxylic Acids[J]. Org Prep Proced Int, 1985,17(3):163.
[5]Huddleston PR,Barker JM.A convenient synthesis of 2-substituted 3-hydroxy and 3-amino-thiophens from derivatives of 2-chloroacrylic acid[J]. Synth Commun, 1979,9(8):731.
[6]Pfister R,Zeller P,Binder D, et al. Thiazine derivatives[P].US.Patent,4180662.1979-12-25.
[7]Pfister R,Zeller P,Binder D, et al. Thiazine derivatives[P].United Kingdom Patent Specification,1519811.1978-08-02.
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脚注
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