对映选择合成
化学选择性
组合化学
烷基化
硫黄
化学
烷基
芳基
药物发现
催化作用
有机化学
生物化学
作者
Fucheng Wang,Weiyi Xiang,Yuefeng Xie,Linge Huai,Luoqiang Zhang,Xin Zhang
出处
期刊:Science Advances
[American Association for the Advancement of Science (AAAS)]
日期:2024-09-13
卷期号:10 (37)
标识
DOI:10.1126/sciadv.adq2768
摘要
Sulfilimines are versatile synthetic intermediates and important moieties in bioactive molecules. However, their applications in drug discovery are underexplored, and efficient asymmetric synthetic methods are highly desirable. Here, we report a transition metal–free pentanidium-catalyzed sulfur alkylation of sulfenamides with exclusive chemoselectivity over nitrogen and high enantioselectivity. The reaction conditions were mild, and a wide range of enantioenriched aryl and alkyl sulfilimines were obtained. The synthetic utility and practicability of this robust protocol were further demonstrated through gram-scale reactions and late-stage functionalization of drugs.
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