1 |
An alternative synthesis of Vandetanib (CaprelsaTM) via a microwave accelerated Dimroth rearrangementBrocklesby, K.L., Waby, Jennifer S., Cawthorne, C., Smith, G. 10 October 2019 (has links)
Yes / 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). / This work was supported by the Cancer Research UK-Cancer Imaging Centre (grant: C1060/ A16464), the Institute of Cancer Research and the University of Hull.
|
Page generated in 0.2538 seconds