A convenient and versatile S N Ar-decarboxylation protocol for the construction of C(sp 2 )-C(sp 3 ) bonds

Increasing saturation (Fsp ) 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 a nucleophilic aromatic substitution-decarboxylation sequence to construc...

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Bibliographic Details
Published inChemical communications (Cambridge, England) Vol. 58; no. 53; pp. 7435 - 7438
Main Authors Burtea, Alexander, DeForest, Jacob, Baldwin, Neil, Leverett, Carolyn, Gallego, Gary M
Format Journal Article
LanguageEnglish
Published England 30.06.2022
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Summary:Increasing saturation (Fsp ) 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 a nucleophilic aromatic substitution-decarboxylation sequence to construct C(sp )-C(sp ) bonds. The method is tolerant of a variety of biologically privileged moieties and has been demonstrated in a library format.
ISSN:1359-7345
1364-548X
DOI:10.1039/D2CC01551J