A novel route for the synthesis of androgen receptor antagonist enzalutamide

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.

Automated summary

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.