Wimmer Alexander, König Burkhard
Department of Chemistry and Pharmacy, Institute of Organic Chemistry , University of Regensburg , Universitätsstraße 31 , 93051 Regensburg , Germany.
Org Lett. 2019 Apr 19;21(8):2740-2744. doi: 10.1021/acs.orglett.9b00698. Epub 2019 Apr 2.
The pharmaceutically underexplored sulfoximine moiety has emerged as a potentially active pharmaceutical ingredient. We developed a scalable synthetic route to N-arylated sulfoximines from the respective "free" NH-sulfoximines and bromoarenes. Our strategy is based on a dual nickel photocatalytic approach, is applicable for a broad scope of substrates, and exhibits a highly functional group tolerance. In addition, we could demonstrate that other sulfoximidoyl derivatives like sulfonimidamides and sulfinamides proceed smoothly under the developed reaction conditions.
尚未得到充分药学研究的磺胺肟部分已成为一种潜在的活性药物成分。我们开发了一种可扩展的合成路线,从相应的“游离”NH-磺胺肟和溴代芳烃制备N-芳基磺胺肟。我们的策略基于双镍光催化方法,适用于广泛的底物范围,并且对官能团具有高度耐受性。此外,我们可以证明,其他磺胺亚胺基衍生物,如磺酰亚胺酰胺和亚磺酰胺,在开发的反应条件下反应顺利。