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dc.contributor.authorKing, Thomasen
dc.contributor.authorStewart, Hannah Len
dc.contributor.authorMortensen, Kim Ten
dc.contributor.authorNorth, Andrew JPen
dc.contributor.authorSore, Hannahen
dc.contributor.authorSpring, Daviden
dc.date.accessioned2019-07-12T23:30:34Z
dc.date.available2019-07-12T23:30:34Z
dc.date.issued2019-09en
dc.identifier.issn1434-193X
dc.identifier.urihttps://www.repository.cam.ac.uk/handle/1810/294591
dc.description.abstractIn recent years the pharmaceutical industry has benefited from the advances made in fragment-based drug discovery (FBDD) with more than 30 fragment-derived drugs currently marketed or progressing through clinical trials. The success of fragment-based drug discovery is entirely dependent upon the composition of the fragment screening libraries used. Heterocycles are prevalent within marketed drugs due to the role they play in providing binding interactions; consequently, heterocyclic fragments are important components of FBDD libraries. Current screening libraries are dominated by flat, sp2-rich compounds, primarily owing to their synthetic tractability, despite the superior physicochemical properties displayed by more three-dimensional scaffolds. Herein, we report step-efficient routes to a number of biologically relevant, fragment-like heterocyclic spirocycles. The use of both electron-deficient and electron-rich 2-atom donors was explored in complexity-generating [3+2]-cycloadditions to furnish products in 3 steps from commercially available starting materials. The resulting compounds were primed for further fragment elaboration through the inclusion of synthetic handles from the outset of the syntheses.
dc.format.mediumPrint-Electronicen
dc.languageengen
dc.publisherJohn Wiley & Sons Ltd.
dc.rightsAll rights reserved
dc.rights.uri
dc.titleCycloaddition Strategies for the Synthesis of Diverse Heterocyclic Spirocycles for Fragment-Based Drug Discovery.en
dc.typeArticle
prism.endingPage5229
prism.issueIdentifier31-32en
prism.publicationDate2019en
prism.publicationNameEuropean journal of organic chemistryen
prism.startingPage5219
prism.volume2019en
dc.identifier.doi10.17863/CAM.41699
dcterms.dateAccepted2019-07-05en
rioxxterms.versionofrecord10.1002/ejoc.201900847en
rioxxterms.versionAM
rioxxterms.licenseref.urihttp://www.rioxx.net/licenses/all-rights-reserveden
rioxxterms.licenseref.startdate2019-09en
dc.contributor.orcidKing, Thomas [0000-0001-6992-8016]
dc.contributor.orcidStewart, Hannah L [0000-0002-7891-2590]
dc.contributor.orcidSore, Hannah [0000-0002-6542-0394]
dc.contributor.orcidSpring, David [0000-0001-7355-2824]
dc.identifier.eissn1099-0690
rioxxterms.typeJournal Article/Reviewen
pubs.funder-project-idRoyal Society (WM150022)
pubs.funder-project-idEPSRC (EP/P020291/1)
cam.orpheus.successThu Jan 30 10:43:27 GMT 2020 - Embargo updated*
rioxxterms.freetoread.startdate2020-09-30


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