Process for preparing 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorfenyl)morpholino)methyl)-1H-1,2,4-triazol-5(4H)-one (aprepitant) in polymorphous form II

摘要

In the present invention, there is disclosed a process for preparing aprepitant of the general formula 1, in crystalline form II, wherein the preparation process is characterized in that the intermediate of the general formula 12 is extracted in water immiscible high-boiling n-pentanol and after washing with water and/or a brine the solution is heated to the boiling point of the given solvent when recycling to aprepitant takes place. After cooling, the obtained aprepitant is then isolated.