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Direct sulfonylation of anilines mediated by visible light†
Chemical Science ( IF 8.4 ) Pub Date : 2017-11-16 00:00:00 , DOI: 10.1039/c7sc03891g
Tarn C. Johnson 1, 2, 3, 4, 5 , Bryony L. Elbert 1, 2, 3, 4, 5 , Alistair J. M. Farley 1, 2, 3, 4, 5 , Timothy W. Gorman 1, 2, 3, 4, 5 , Christophe Genicot 6, 7, 8, 9 , Bénédicte Lallemand 6, 7, 8, 9 , Patrick Pasau 6, 7, 8, 9 , Jakub Flasz 5, 6, 10 , José L. Castro 5, 6, 10 , Malcolm MacCoss 11, 12, 13 , Darren J. Dixon 1, 2, 3, 4, 5 , Robert S. Paton 1, 2, 3, 4, 5 , Christopher J. Schofield 1, 2, 3, 4, 5 , Martin D. Smith 1, 2, 3, 4, 5 , Michael C. Willis 1, 2, 3, 4, 5
Affiliation  

Sulfones feature prominently in biologically active molecules and are key functional groups for organic synthesis. We report a mild, photoredox-catalyzed reaction for sulfonylation of aniline derivatives with sulfinate salts, and demonstrate the utility of the method by the late-stage functionalization of drugs. Key features of the method are the straightforward generation of sulfonyl radicals from bench-stable sulfinate salts and the use of simple aniline derivatives as convenient readily available coupling partners.

中文翻译:

可见光介导的苯胺直接磺酰化

砜在生物活性分子中具有显着特征,并且是有机合成的关键功能基团。我们报告了一个温和的,光氧化还原催化的亚磺酸盐与苯胺衍生物的磺酰化反应,并通过药物的后期功能化证明了该方法的实用性。该方法的主要特点是可以从稳定的亚磺酸盐直接生成磺酰基,并使用简单的苯胺衍生物作为便捷的偶联剂。
更新日期:2017-11-16
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