Abstract
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.
Keywords: Kinase inhibitors, sulfonamides, heterocyclic scaffolds, cross-couplings
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Current Computer-Aided Drug Design
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