Methanesulfonic Acid → Eprosartan Mesylate

Participants

Reaction Steps

After numerous trials, the inventor found that: eprosartan was suspended or dissolved in glacial acetic acid, then methanesulfonic acid was added to obtain a clear solution of eprosartan mesylate in glacial acetic acid; after about 1 hour of stirring, eprosartan mesylate solid would precipitate slowly, and thus the salification of eprosartan with methanesulfonic acid avoids embedment; ethyl acetate was added to render eprosartan mesylate crystallized completely, the obtained solid was easy to filter and drain under a reduced pressure, the wet product obtained had a low solvent content and thus was easy to dry. In addition, the new process of adding methanesulfonic acid into a solution of eprosartan in acetic acid did not produce new impurities, and the originally existing impurities decreased by some extent.

Provenance & Evidence