A novel route for the synthesis of androgen receptor antagonist enzalutamide - Université de Montpellier
Article Dans Une Revue Chinese Chemical Letters Année : 2023

A novel route for the synthesis of androgen receptor antagonist enzalutamide

Résumé

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.

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Xiangguo Meng, Siju Bi, Shixin Jin, Kai Wu, Shanchao Wu, et al.. A novel route for the synthesis of androgen receptor antagonist enzalutamide. Chinese Chemical Letters, 2023, 34 (6), pp.108096. ⟨10.1016/j.cclet.2022.108096⟩. ⟨hal-04620345⟩
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