Methanol → Nelfinavir Mesylate

Participants

Reaction Steps

Thus in accordance to the present invention Nelfinavir base is suspended in an organic solvent, selected from methanol, ethanol, isopropanol, THF, and methanesulfonic acid is added at temperature below 45° C. over a period of 10 min to 4 hrs. The reaction mass is mixed for about 15 min to 4 hrs to form a solution and then cooled to 10° C. to 35° C. A ketone such as acetone, methyl ethyl ketone, methyl isobutyl ketone, 2-pentanone is added as ante solvent at temperature 10° C. to about 35° C. in about 15 min to 4 hrs. The resulting reaction mass is maintained at temperature of 10° C. to 35° C. for about 30 min to 6 hrs then cooled and maintained at temperature of −10° C. to 15° C. for about 30 min to 4 hrs. The precipitated solid is separated and dried at temperature of 50° C. to 120° C., preferably at 80° C. to 110° C. under reduced pressure to produce novel crystalline forms of Nelfinavir mesylate.

Provenance & Evidence