Water → Rivaroxaban

Participants

Reaction Steps

N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)formamide (1 g) taken in a mixture of tetrahydrofuran (10 ml) and sodium hydride (0.11 g) stirred reaction mass at 25 to 30° C. for 30 minutes. To this mixture added 5-chlorothiophene carbonyl chloride (0.86 g). Obtained reaction mass then stirred for 1 to 2 h at 25 to 30° C. After completion of reaction, added ethyl acetate and water. Separated organic layer and concentrated under reduced pressure to obtain residue. Added acetic acid and methanol to residue stirred for 30 minutes and obtained solid is filtered off. Washed solid with methanol

Provenance & Evidence