Wang We
2014
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Journal
Chinese Journal of New Drugs
Abstract
Objective:To improve the synthesis process of retigabine.Methods:The target compound was synthesized from 3-fluoroaniline by acetylation and nitrification to give N-(5-fluoro-2-nitrophenyl) acetamide(2),which was subjected to condensation with(4-fluorophenyl) methanamine to afford N-(5-((4-fluorobenzyl) amino)-2-nitrophenyl) acetamide(3),followed by deacetylation,reduction,and acylation.Results:The structure of retigabine was confirmed by1H-NMR and MS.The overall yield was 39.6%.Conclusion:This synthetic process is easy to scale up for its convenient operation.