Department of Dermatology, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041, China.
Department of Chemistry, Technical University of Denmark, 2800, Kgs. Lyngby, Denmark.
Angew Chem Int Ed Engl. 2021 Mar 22;60(13):7353-7359. doi: 10.1002/anie.202014111. Epub 2021 Feb 17.
A new SO surrogate is reported that is cheap, bench-stable, and can be accessed in just two steps from bulk chemicals. Essentially complete SO release is achieved in 5 minutes. Eight established sulfonylation reactions proceeded smoothly by ex situ formation of SO by utilizing a two-chamber system in combination with the SO surrogate. Furthermore, we report the first direct aminosulfonylation between aryl iodides and amines. Broad functional group tolerance is demonstrated, and the method is applicable to pharmaceutically relevant substrates, including heterocyclic substrates.
报告了一种新的 SO 替代物，它廉价、在实验台上稳定，并且只需从大量化学品中经过两步即可获得。基本上在 5 分钟内即可实现完全的 SO 释放。通过利用两室系统结合 SO 替代物原位形成 SO，八种已建立的磺酰化反应顺利进行。此外，我们还报告了芳基碘化物和胺之间的首例直接氨基磺酰化反应。该方法具有广泛的官能团耐受性，适用于药物相关的底物，包括杂环底物。
