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.

中文翻译：

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雄激素受体拮抗剂恩杂鲁胺的合成新路线

分五步开发了恩杂鲁胺的新路线。从 4-氨基-2-(三氟甲基) 苄腈 ( 7 ) 和 Boc-2-氨基异丁酸 ( 16 ) 开始，缩合、脱保护、Ullmann 偶联、环化和胺化以 41.0% 的总收率提供恩杂鲁胺。该路线避免了使用有毒化学品、不稳定的中间体和高危反应。这是一种潜在的高效和经济的工业化程序。