Design and Combinatorial Synthesis of a Library of Methylenesulfonamides and Related Compounds as Potential Kinase Inhibitors
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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 ASYMMETRIC-SYNTHESIS TARGETS INDOLES
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COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING, 2009, 12 (3), pp. 275 - 284