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Facile and stereospecific synthesis of diverse β-N-glycosyl sulfonamide scaffolds via palladium catalysis
Zhong, Lei1; Wang, Qunliang1; Wang, Yujuan1; Cheng, Yiyang1; Xiong, Yimeng1; Peng, Haibo2; Zhou, Zhen1; He, Yun1; Dai, Yuanwei1
2023-10-26
摘要Glycosylation is an important strategy to improve the druggability of lead compounds. Here, we present a palladium-catalysed stereospecific N-glycosylation of sulfonamides. This approach stands out with wide substrate scope, high functional group tolerance, and easy scalability, furnishing a broad spectrum of densely functionalized beta-N-glycosyl sulfonamides with good efficiency and exceptional regio-/stereoselectivity. Diverse drug-like glycosulfonamido scaffolds have been constructed via a late-stage diversification strategy and various facile synthetic transformations of the products. Collectively, the established protocol provides a valuable tool for efficiently preparing glycosyl sulfonamides to facilitate drug discovery.
DOI10.1039/d3cc04063a
发表期刊CHEMICAL COMMUNICATIONS
ISSN1359-7345
卷号59期号:86页码:12907-12910
通讯作者He, Yun(yun.he@cqu.edu.cn) ; Dai, Yuanwei(ydai20@cqu.edu.cn)
收录类别SCI
WOS记录号WOS:001084589900001
语种英语