'novel process for the synthesis of aprepitant and fosaprepitant and pharmaceutically acceptable salts thereof'

摘要

The present invention is related to a novel process of synthesis of 5-[[(2R,3S)-2-[(lR)-l-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyi]methyl]-l,2dihydro-3H-l,2,4-triazol-3-one . (Aprepitant) and 3-{[(2R53S)-2-[(lR)-l-[3,5-bis(trifluoromethyl)phenyl] ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl} -5-oxo-2H-1,2,4-triazol-1 -yl]phosphonic acid (Fosaprepitant) and pharmaceutically acceptable salts thereof.