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Design and Combinatorial Synthesis of a Library of Methylenesulfonamides and Related Compounds as Potential Kinase Inhibitors

[ Vol. 12 , Issue. 3 ]


Jane E. Torr, Jonathan M. Large and Edward McDonald   Pages 275 - 284 ( 10 )


An effective parallel solid phase route to methylenesulfonamides and amides bearing a wide variety of substituents is described. The three key reaction steps were reductive amination of a haloheteroaromatic aldehyde onto a benzhydrylamine type polystyrene resin, sulfonamide or amide formation and palladium catalysed transformation of the remaining heteroaromatic halogen. A process of virtual library design and filtering, together with solution and solid phase optimisations, aided the preparation of several novel drug-like product classes in high purities and should allow access to a variety of further useful analogues.


Kinase inhibitors, sulfonamides, heterocyclic scaffolds, cross-couplings


Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Belmont, Surrey SM2 5NG, UK.

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