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An alternative synthesis of Vandetanib (Caprelsa™) via a microwave accelerated Dimroth rearrangement
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2017-03-26 02:21:35
Kayleigh L. Brocklesby, Jennifer S. Waby, Chris Cawthorne, Graham Smith

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).

中文翻译:

Vandetanib(Caprelsa™)的另一种合成方法是通过微波加速Dimroth重排

Vandetanib是口服可利用的酪氨酸激酶抑制剂,可用于治疗癌症。除了需要顺序的保护和脱保护步骤外,当前的合成还通过使用刺激性试剂的不稳定的4-氯喹唑啉进行。在目前的工作中,在关键的喹唑啉形成步骤中使用Dimroth重排使得能够在9个步骤中合成Vandetanib(与之前报道的12-14比较)。
更新日期:2017-03-26
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