Facile preparation of 3-substituted-2,6-difluoropyridines: application to the synthesis of 2,3,6-trisubstituted pyridines

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• 作者：Taisuke Katoh ; ^{taisuke.katoh@takeda.com" class="auth_mail" title="E-mail the corresponding author} ; Yoshihide Tomata ; Tetsuya Tsukamoto ; Yoshihisa Nakada
• 关键词：Difluorination ; 3-Substituted-2 ; 6-difluoropyridines ; 2 ; 3 ; 6-Trisubstituted pyridines
• 刊名：Tetrahedron Letters
• 出版年：2015
• 出版时间：28 October 2015
• 年：2015
• 卷：56
• 期：44
• 页码：6043-6046
• 全文大小：913 K

文摘

We report a facile method for the difluorination of 3-substituted-2,6-dichloropyridines using cesium fluoride as a fluorination reagent in dimethyl sulfoxide. It is proposed that this method for preparing 3-substituted-2,6-difluoropyridines is simpler and easier than those reported in previous literature. To examine the utility of 3-substituted-2,6-difluoropyridines in synthetic chemistry, we also demonstrate a subsequent conversion to 2,3,6-trisubstituted pyridines by a tandem nucleophilic aromatic substitution.