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dc.contributor.authorMcDonald, T
dc.date.accessioned2018-06-28T09:46:02Z
dc.date.issued2009
dc.identifierhttp://publications.icr.ac.uk/7991/
dc.identifier.citationCOMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING, 2009, 12 (3), pp. 275 - 284
dc.identifier.issn1386-2073
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/1961
dc.description.abstractAn 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.
dc.format.extent275 - 284
dc.languageeng
dc.language.isoeng
dc.subjectKinase inhibitors sulfonamides heterocyclic scaffolds cross-couplings ASYMMETRIC-SYNTHESIS TARGETS INDOLES
dc.titleDesign and Combinatorial Synthesis of a Library of Methylenesulfonamides and Related Compounds as Potential Kinase Inhibitors
dc.typeJournal Article
rioxxterms.licenseref.startdate2009
rioxxterms.typeJournal Article/Review
dc.relation.isPartOfCOMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
pubs.issue3
pubs.notesnone 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.
pubs.notesNot known
pubs.organisational-group/ICR
pubs.organisational-group/ICR
pubs.volume12
pubs.embargo.termsNot known
dc.contributor.icrauthorTorr, Janeen
dc.contributor.icrauthorLarge, Jonathanen
dc.contributor.icrauthorMcDonald, Edwarden


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