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dc.contributor.authorTwigg, Daviden
dc.contributor.authorKondo, Nen
dc.contributor.authorMitchell, Sophieen
dc.contributor.authorGalloway, Warrenen
dc.contributor.authorSore, Hannahen
dc.contributor.authorMadin, Aen
dc.contributor.authorSpring, Daviden
dc.date.accessioned2016-10-14T13:01:08Z
dc.date.available2016-10-14T13:01:08Z
dc.date.issued2016-09-06en
dc.identifier.issn1433-7851
dc.identifier.urihttps://www.repository.cam.ac.uk/handle/1810/260773
dc.description.abstractFragment-based lead generation has proven to be an effective means of identifying high-quality lead compounds for drug discovery programs. However, the fragment screening sets often used are principally comprised of sp²-rich aromatic compounds, which limits the structural (and hence biological) diversity of the library. Herein, we describe strategies for the synthesis of a series of partially saturated bicyclic heteroaromatic scaffolds with enhanced sp³ character. Subsequent derivatization led to a fragment collection featuring regio- and stereo-controlled introduction of substituents on the saturated ring system, often with formation of new stereocenters.
dc.description.sponsorshipEPSRC BBSRC MRC Wellcome Trust D.G.T. thanks AstraZeneca for funding. S.L.M. thanks BASF for funding. .
dc.languageengen
dc.language.isoenen
dc.publisherWiley
dc.rightsAttribution 4.0 Internationalen
dc.rightsAttribution 4.0 Internationalen
dc.rightsAttribution 4.0 Internationalen
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.subjectdrug designen
dc.subjectdrug discoveryen
dc.subjectfused-ring systemsen
dc.subjectnitrogen heterocyclesen
dc.subjectsynthetic methodsen
dc.titlePartially Saturated Bicyclic Heteroaromatics as an sp³-Enriched Fragment Collection.en
dc.typeArticle
prism.endingPage12483
prism.issueIdentifier40en
prism.publicationDate2016en
prism.publicationNameAngewandte Chemie International Editionen
prism.startingPage12479
prism.volume55en
dc.identifier.doi10.17863/CAM.5926
dc.identifier.doi10.17863/CAM.5926
dc.identifier.doi10.17863/CAM.5926
dc.identifier.doi10.17863/CAM.5926
dcterms.dateAccepted2016-08-03en
rioxxterms.versionofrecord10.1002/anie.201606496en
rioxxterms.versionAMen
rioxxterms.licenseref.urihttp://creativecommons.org/licenses/by/4.0/en
rioxxterms.licenseref.startdate2016-09-06en
dc.contributor.orcidSore, Hannah [0000-0002-6542-0394]
dc.contributor.orcidSpring, David [0000-0001-7355-2824]
dc.identifier.eissn1521-3773
rioxxterms.typeJournal Article/Reviewen
pubs.funder-project-idEuropean Research Council (279337)
pubs.funder-project-idRoyal Society (WM150022)
pubs.funder-project-idEPSRC (EP/J016012/1)
pubs.funder-project-idEPSRC (EP/K039520/1)
datacite.issupplementedby.doi10.1002/anie.201606496en
rioxxterms.freetoread.startdate2017-08-03


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Attribution 4.0 International
Except where otherwise noted, this item's licence is described as Attribution 4.0 International