摘要
An improved and practical synthesis of enzalutamide was accomplished in five steps.Starting from 4-bromo-2-fluoro-benzonic acid,a methyl esterification,Ullmann ligation,methyl esterification,ring closing reaction and final methyl amidation provided the target in 35% total yield with 99.8% purity.Five identified impurities were also synthesized.This efficient and economical procedure avoids the use of highly toxic reagents and multiple recrystallization operations,which is suitable for further industrialization.
An improved and practical synthesis of enzalutamide was accomplished in five steps.Starting from 4-bromo-2-fluoro-benzonic acid,a methyl esterification,Ullmann ligation,methyl esterification,ring closing reaction and final methyl amidation provided the target in 35% total yield with 99.8% purity.Five identified impurities were also synthesized.This efficient and economical procedure avoids the use of highly toxic reagents and multiple recrystallization operations,which is suitable for further industrialization.
基金
the 2016 Shanghai Pujiang Talent program (No. 16PJ1432800)
China State Institute of Pharmaceutical Institute Industry for financially supporting this program
