The Synthesis Of Antiandrogen Drug Bicalutamide

This paper gives a brief account of the medicines that have been used to treat prostate cancer , and the studies of the synthetic method for the antiandrogen drug Bicalutamide and its quality control were performed.Through the analysis of the structure and the methods reported , 4-cyano-3-(trifluoromethyl) aniline and 2-methylacryloyl chloride were chosen as the stating material, through acylation, cyclization, substitution and oxidization reaction, and the process optimization, Bicalutamide was prepared in a total yield of 22.5% from 4-cyano-3-(trifluoromethyl) aniline . The synthesis of the key intermediate was accomplished through nitration, reduction and cyanogenation starting from 2-Bromo-(trifiuormethyl)benzene.The chemical structure of the target compound was determined by IR,¹H-NMR,¹³C-NMR and MS, which is completely identical with that of Bicalutamide control sample .The related substances and content of Bicalutamide were determined with high-performance liquid chromatography. It is proved through systematic suitability test that the method selected is highly effective and specific, and suitable for the determination of the related substances and content of Bicalutamide.