A Facile Total Synthesis of Mubritinib

Synthesis(2021)

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摘要
A five-step, practical, and concise total synthesis of Mubritinib is described. The synthesis utilized Friedel-Crafts acylation, Click reaction, reduction and demethylation for the construction of the triazole ring system as key steps. Other important features of this synthesis is Bredereck oxazole synthesis. The main advantages of this process are the improved yield and decreased number of reaction steps, which paves the way for the industrial-scale synthesis of Mubritinib.
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关键词
mubritinib, TAK-165, triazoles, click reaction, total synthesis
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