Uses
4-amino-2-fluoro-N-methylbenzamide acts as a reagent in the design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists. Also, in the preparation and structure-activity relationship of chiral benzyloxypyridinone derivatives as c-Met kinase inhibitors.
Description
4-amino-2-fluoro-N-methylbenzamide is a novel antiandrogen drug MDV (Marek's Disease Virus) 3100 key intermediate which is the new generation oral androgen antagonist medicine of united states drug developer Medivation company exploitation, be mainly used in treating advanced prostate cancer (CRPC) patient.
Preparation
2-fluoro-4-nitrotoluene as raw material, through potassium permanganate oxidation, the thionyl chloride chlorination, methylamine amination, and Pd/C hydrogenation reduction prepare 4-amino-2-fluoro-N-methylbenzamide.