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Catalytic sp3 -sp3 Functionalisation of Sulfonamides: Late-Stage Modification of Drug-Like Molecules

Abdulla, Othman, Clayton, Adam D., Faulkner, Robert A., Gill, Duncan M., Rice, Craig R., Walton, Scarlett M. and Sweeney, Joseph B. (2017) Catalytic sp3 -sp3 Functionalisation of Sulfonamides: Late-Stage Modification of Drug-Like Molecules. Chemistry - A European Journal, 23 (7). pp. 1494-1497. ISSN 0947-6539

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Abstract

A new application of Pd-catalysed allylation is reported that enables the synthesis of a range of branched sp3-functionalised sulfonamides, a compound class for which few reported methods exist. By reacting benzyl sulfonamides with allylic acetates in the presence of Pd0 catalysts and base at room temperature, direct allylation was efficiently performed, yielding products that are analogues of structural motifs seen in biologically active small molecules. The reaction was performed under mild conditions and could be applied to nanomolar sigma-receptor binders, thus enabling a late-stage functionalisation and efficient expansion of drug-like chemical space.

Item Type: Article
Subjects: Q Science > QD Chemistry
Schools: School of Applied Sciences
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Depositing User: Joseph Sweeney
Date Deposited: 12 May 2017 10:14
Last Modified: 12 May 2017 10:14
URI: http://eprints.hud.ac.uk/id/eprint/31859

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