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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).

Original publication

DOI

10.1016/j.tetlet.2017.02.082

Type

Journal article

Journal

Tetrahedron Lett

Publication Date

12/04/2017

Volume

58

Pages

1467 - 1469

Keywords

Dimroth rearrangement, Quinazoline, Tyrosine kinase inhibitor, Vandetanib