Ranbaxy Laboratories, Inc.

Hiten Sharadchandra Mehta

Mohan Prasad

Asok Nath

Subhash Dhar

Deepak Mohanlal Jain

Maneck Khurana

Abhay Tatiya

Sanjay Mahadeo Gade

The present invention provides a process for preparation of crystalline aprepitant having not more than 15% by weight of Form I content which comprises, a) dissolving aprepitant in a suitable solvent to obtain a solution, b) cooling the solution to 10-15&#xb0; C., c) optionally seeding the solution with aprepitant Form I crystals, d) adding an anti-solvent to the solution, and e) isolating crystalline aprepitant having not more than 15% by weight of Form I content.

Process for the preparation of crystalline aprepitant having form I content

The present invention relates to a highly pure (2R,3S)-4-benzyl-3-(4-fluorophenyl)morpholin-2-yl 3,5-bis(trifluoromethyl)benzoate of Formula II, and a process for its preparation. The present invention further provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof, using the highly pure compound of Formula II. The present invention also provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof which comprises of cyclising the compound of Formula VII at elevated temperature, in the absence of solvent.

Process for the preparation of aprepitant

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Ahmedabad, India

Hiten Sharadchandra Mehta