An efficient synthesis of rufinamide, an antiepileptic drug

被引：38

作者：

Mudd, Whitney H. ^{[1
]}

Stevens, Erland P. ^{[1
]}

机构：

[1] Davidson Coll, Dept Chem, Davidson, NC 28035 USA

来源：

TETRAHEDRON LETTERS | 2010年 / 51卷 / 24期

关键词：

Azide; Cycloaddition; Epilepsy; Heterocycles; Pharmaceuticals; AZIDE;

D O I：

10.1016/j.tetlet.2010.04.060

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：3229 / 3231

页数：3

共 13 条

[1] 1.3-DIPOLARE CYCLOADDITIONEN .32. KINETIK DER ADDITIONEN ORGANISCHER AZIDE AN CC-MEHRFACHBINDUNGEN [J].