Ethanol → Edoxaban tosylate monohydrate

Participants

Reaction Conditions

Reaction Steps

The compound (6.2 g) obtained in Example 310 is dissolved in methylene chloride (120 mL), a 1 mol/L ethanol solution (11.28 mL) of p-toluenesulfonic acid was added to the solution, and the solvent was distilled away. Ethanol (95 mL) containing 15% water was added to the residue, and the mixture was stirred at 60° C. to dissolve it. The solution was then cooled to room temperature and stirred for a day. Crystals precipitated were collected by filtration, washed with ethanol and dried at room temperature for 2 hours under reduced pressure to give the title compound (7.4 g).

Provenance & Evidence