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...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.展开更多
基金supported by Scientific Research Cadre Project(AMSCP)2021National Key Research and Development Program of China(No.2020YFA0509200 to C.Sheng)。
文摘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.
