4.4 Article

An efficient synthesis of rufinamide, an antiepileptic drug

Journal

TETRAHEDRON LETTERS
Volume 51, Issue 24, Pages 3229-3231

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2010.04.060

Keywords

Azide; Cycloaddition; Epilepsy; Heterocycles; Pharmaceuticals

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A two-step, one-pot synthesis of rufinamide, an antiepileptic drug, has been developed. 2,6-Difluorobenzyl azide reacts with methyl 3-methoxyacrylate followed by methanolic ammonia to afford rufinamide in 89% yield. The new method generates less waste and uses reagents that are both less expensive and less toxic than other reported syntheses. (C) 2010 Elsevier Ltd. All rights reserved.

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