亲核芳香族取代
脱羧
化学
组合化学
亲核细胞
分子
药物发现
亲核取代
立体化学
有机化学
催化作用
生物化学
作者
Alexander Burtea,Jacob DeForest,Neil J. Baldwin,Carolyn A. Leverett,Gary M. Gallego
摘要
Increasing saturation (Fsp3) remains a central strategy in the optimization of properties of molecules during drug discovery. Here, we describe a versatile and operationally simple one-pot procedure for accomplishing this goal via a nucleophilic aromatic substitution-decarboxylation sequence to construct C(sp2)-C(sp3) bonds. The method is tolerant of a variety of biologically privileged moieties and has been demonstrated in a library format.
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