WU Xiaoguo, MAO Yaqin. Improved Synthetic Procedure of Zafirlukast[J]. Chinese Journal of Modern Applied Pharmacy, 2009, (1): 36-38.
    Citation: WU Xiaoguo, MAO Yaqin. Improved Synthetic Procedure of Zafirlukast[J]. Chinese Journal of Modern Applied Pharmacy, 2009, (1): 36-38.

    Improved Synthetic Procedure of Zafirlukast

    • OBJECTIVE To improve the synthetic procedure of zafirlukast.METHODS Zafirlukast was synthesized from 5-nitro-1H-indole via methylation, alkylation, condensation, reduction and acylation. The methylation, alkylation and reduction are key steps in the procedure. RESULTS Zafirlukast was prepared in an overall yield of 31.6%.The structure of the target compound was confirmed by IR spectra, MS, H-NMR and elemental analysis.CONCLUSION The improved procedure avoids the use of expensive reagents and the target compound was synthesized in a convenient way. The method is suitable for industrial manufacture.
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