Yang Linjie, Zhong Yuanfang, Chen Wanzhi
Department of Chemistry, Zhejiang University, Hangzhou 310027, China.
Org Lett. 2025 Mar 14;27(10):2532-2536. doi: 10.1021/acs.orglett.5c00684. Epub 2025 Mar 3.
An efficient Pd-catalyzed N-arylation of sulfoximines with (hetero)aryl chlorides was developed under mild aqueous conditions. This reaction proceeded smoothly with a low loading of the Pd catalyst (down to 0.5 mol %) and was completed rapidly within 30 min. A wide range of (hetero)aryl chlorides and sulfoximines were well tolerated, delivering the corresponding (hetero)aryl sulfoximines in good to excellent yields. The gram-scale reaction and pharmaceutical derivatization demonstrated good practicality.
在温和的水相条件下,开发了一种高效的钯催化的磺胺氧化亚胺与(杂)芳基氯化物的N-芳基化反应。该反应在低负载量的钯催化剂(低至0.5 mol%)下顺利进行,并在30分钟内迅速完成。各种(杂)芳基氯化物和磺胺氧化亚胺都具有良好的耐受性,以良好至优异的产率得到相应的(杂)芳基磺胺氧化亚胺。克级反应和药物衍生化显示出良好的实用性。