Methanesulfonic Acid → Safinamide Mesylate

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

A mixture of (S)-2-[4-(3-fluorobenzyloxy)benzylamino]propanamide (20 g, 66 mmol, prepared in Example 12 a) and ethyl acetate (510 g) is heated, under stirring up to 65° C. and kept under these conditions until a clear solution is obtained. Methanesulfonic acid (7 g, 72.6 mmol) is added in 40 min to the solution precooled to 55° C. The mixture is gradually cooled to 20° C. in 3 hours, kept at 20° C. for 2 hours. The heterogeneous mixture is filtered, the solid is dried at reduced pressure at 40° C. to yield 26.1 g of title compound as white powder (99% yield).

Herkunft & Nachweise