Palladium-Catalyzed Sulfination of Aryl and Heteroaryl Halides: Direct Access to Sulfones and Sulfonamides

Palladium-Catalyzed Sulfination of Aryl and Heteroaryl Halides: Direct Access to Sulfones and Sulfonamides
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DOI:
10.1021/ol403072r
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发表时间:
2013-12-20
期刊:
影响因子:
5.2
通讯作者:
Mascitti, Vincent
Mascitti, Vincent
中科院分区:
化学1区
文献类型:
--
作者:
Shavnya, Andrei;Coffey, Steven B.;Mascitti, Vincent

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介绍了一种新的钯催化芳基和杂芳基卤化物亚化反应。该反应在温和的条件下进行,并提供了广泛的芳基和杂芳基亚磺酸盐,这是一类有用的和通用的合成中间体。利用这种亚化反应,还开发了一锅方案,允许直接获得砜和磺胺。用平行合成药物伟哥类似物来说明这些转化的实用性。
A novel palladium-catalyzed sulfination of aryl and heteroaryl halides is described. This reaction operates under mild conditions and provides access to a wide range of aryl and heteroaryl sulfinates, a useful and versatile class of synthetic intermediates. Capitalizing on this sulfination reaction, one-pot protocols allowing direct access to sulfones and sulfonamides have also been developed. The practicality of these transformations is illustrated with the parallel synthesis of analogues of the drug Viagra.