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An alternative synthesis of Vandetanib (Caprelsa™) via a microwave accelerated Dimroth rearrangement.

dc.contributor.authorBrocklesby, KL
dc.contributor.authorWaby, JS
dc.contributor.authorCawthorne, C
dc.contributor.authorSmith, G
dc.date.accessioned2017-03-24T14:22:54Z
dc.date.issued2017-04-12
dc.identifier.citationTetrahedron letters, 2017, 58 (15), pp. 1467 - 1469
dc.identifier.issn0040-4039
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/497
dc.identifier.doi10.1016/j.tetlet.2017.02.082
dc.description.abstractVandetanib is an orally available tyrosine kinase inhibitor used in the treatment of cancer. The current synthesis proceeds via an unstable 4-chloroquinazoline, using harsh reagents, in addition to requiring sequential protection and deprotection steps. In the present work, use of the Dimroth rearrangement in the key quinazoline forming step enabled the synthesis of Vandetanib in nine steps (compared to the previously reported 12-14).
dc.formatPrint
dc.format.extent1467 - 1469
dc.languageeng
dc.language.isoeng
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD
dc.rights.urihttps://creativecommons.org/licenses/by/4.0
dc.titleAn alternative synthesis of Vandetanib (Caprelsa™) via a microwave accelerated Dimroth rearrangement.
dc.typeJournal Article
dcterms.dateAccepted2017-02-27
rioxxterms.versionofrecord10.1016/j.tetlet.2017.02.082
rioxxterms.licenseref.urihttps://creativecommons.org/licenses/by/4.0
rioxxterms.licenseref.startdate2017-04
rioxxterms.typeJournal Article/Review
dc.relation.isPartOfTetrahedron letters
pubs.issue15
pubs.notesNot known
pubs.organisational-group/ICR
pubs.organisational-group/ICR/Primary Group
pubs.organisational-group/ICR/Primary Group/ICR Divisions
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Closed research teams
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Closed research teams/PET Radiochemistry
pubs.organisational-group/ICR
pubs.organisational-group/ICR/Primary Group
pubs.organisational-group/ICR/Primary Group/ICR Divisions
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Closed research teams
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Closed research teams/PET Radiochemistry
pubs.publication-statusPublished
pubs.volume58
pubs.embargo.termsNot known
icr.researchteamPET Radiochemistry
dc.contributor.icrauthorSmith, Graham


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