Pfizer Inc., Eastern Point Road, Groton, Connecticut 06340, United States.
Org Lett. 2013 Dec 20;15(24):6226-9. doi: 10.1021/ol403072r. Epub 2013 Nov 20.
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.
描述了一种新型钯催化的芳基和杂芳基卤化物的磺化反应。该反应在温和条件下进行,并提供了广泛的芳基和杂芳基磺酸盐,这是一类有用且多功能的合成中间体。利用该磺化反应,还开发了一锅法方案,可直接得到砜和磺胺类化合物。这些转化的实用性通过平行合成药物伟哥的类似物得到了说明。