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