Show simple item record

dc.contributor.authorBrocklesby, K.L.
dc.contributor.authorWaby, Jennifer S.
dc.contributor.authorCawthorne, C.
dc.contributor.authorSmith, G.
dc.date.accessioned2019-10-10T15:43:06Z
dc.date.accessioned2019-10-10T16:03:17Z
dc.date.available2019-10-10T15:43:06Z
dc.date.available2019-10-10T16:03:17Z
dc.date.issued2017-04-12
dc.identifier.citationBrocklesby KL, Waby JS, Cawthorne C et al (2017) An alternative synthesis of Vandetanib (CaprelsaTM) via a microwave accelerated Dimroth rearrangement. Tetrahedron Letters. 58(15): 1467-1469.en_US
dc.identifier.urihttp://hdl.handle.net/10454/17298
dc.descriptionYesen_US
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).en_US
dc.description.sponsorshipThis work was supported by the Cancer Research UK-Cancer Imaging Centre (grant: C1060/ A16464), the Institute of Cancer Research and the University of Hull.en_US
dc.language.isoenen_US
dc.relation.isreferencedbyhttps://doi.org/10.1016/j.tetlet.2017.02.082en_US
dc.rights©2017 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (http:// creativecommons.org/licenses/by/4.0/).en_US
dc.subjectVandetaniben_US
dc.subjectQuinazolineen_US
dc.subjectDimroth rearrangementen_US
dc.subjectTyrosine kinase inhibitoren_US
dc.titleAn alternative synthesis of Vandetanib (CaprelsaTM) via a microwave accelerated Dimroth rearrangementen_US
dc.status.refereedYesen_US
dc.date.Accepted2017-02-27
dc.date.application2017-02-28
dc.typeArticleen_US
dc.type.versionPublished versionen_US
dc.date.updated2019-10-10T14:43:09Z
refterms.dateFOA2019-10-10T16:03:50Z


Item file(s)

Thumbnail
Name:
Vandetanib.pdf
Size:
621.3Kb
Format:
PDF
Description:
Waby_Tetrahedron_Letters

This item appears in the following Collection(s)

Show simple item record