Research on the Improvement of Synthesis Process of Lufenamide
This article improves the synthesis process of the antiepileptic drug Lufenamide.Using DPPA as a diazotizing reagent,it reacted with 2,6-difluorobenzyl bromide to obtain 1-azidomethyl-2,6-difluorobenzene,which was then click cyclized with methyl propargonate to obtain 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxylic acid methyl ester.Finally,the antiepileptic drug Lufenamide was obtained by ammonolysis,with a total yield of about 63%.The method developed in this article avoids the direct use of sodium azide and uses water as the reaction medium,which has good industrial application prospects.
lufenamidediazotizationantiepileptic drugssynthesis process
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