An alternative synthesis of Vandetanib (Caprelsa™) via a microwave accelerated Dimroth rearrangement.
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Date
2017-04-12ICR Author
Author
Brocklesby, KL
Waby, JS
Cawthorne, C
Smith, G
Type
Journal Article
Metadata
Show full item recordAbstract
Vandetanib 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).
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Research team
PET Radiochemistry
Language
eng
Date accepted
2017-02-27
License start date
2017-04
Citation
Tetrahedron letters, 2017, 58 (15), pp. 1467 - 1469
Publisher
PERGAMON-ELSEVIER SCIENCE LTD