4.7 Article

A novel route for the synthesis of androgen receptor antagonist enzalutamide

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CHINESE CHEMICAL LETTERS
卷 34, 期 6, 页码 -

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ELSEVIER SCIENCE INC
DOI: 10.1016/j.cclet.2022.108096

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Enzalutamide; Condensation; Deprotection; Ullmann coupling; Cyclization; Amination

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A novel synthetic route for enzalutamide was developed in five steps, providing a total yield of 41.0%. This route avoids the use of toxic chemicals, unstable intermediates, and high-risk reactions, making it a potential efficient and economical procedure for industrialization.
A novel route of enzalutamide was developed in five steps. Starting from 4-amino-2-(trifluoromethyl)benzonitrile (7) and Boc-2-aminoisobutyric acid (16), condensation, deprotection, Ullmann coupling, cyclization and amination provided enzalutamide in 41.0% total yield. This route avoids the using of toxic chemical, unstable intermediate and high-risk reaction. It is a potential efficient and economical procedure for industrialization. (c) 2023 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.

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