Methanesulfonic Acid → Eprosartan Mesylate

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

Eprosartan free base (8 gm, obtained in example 3) is suspended in acetone (120 ml) at 25-30° C., the suspension is cooled to 0-5° C., methanesulfonic acid (5.4 gm) is added drop wise while maintaining the temperature at 0-5° C. The temperature of the mass is raised to 25-30° C. and stirred for 5 hours. The mass is cooled to 0-5° C., stirred for 1 hour, the material is filtered and then suck dried. To the resulting wet cake is added acetone (16 ml) and stirred for 15 minutes at 25-30° C. The material is filtered, washed with acetone (8 ml) and then dried to give 9 gm of pure eprosartan mesylate [HPLC Purity: 99.96%; Specific Surface Area: 1.11 m2/g; Mean particle size (D50): 11.23 μm and 90 volume-% of the particles (D90): 30.42 μm].

Herkunft & Nachweise