Hydrochloric Acid → (S)-4-(4-(5-(aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one

Participants

Reaction Conditions

Reaction Steps

1360 g of 2-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-1H-isoindole-1,3(2H)-dione (VI) are suspended in 10.2 l of ethanol at 22° C., and 1103 g of methylamine solution (40% strength in water) are added. The reaction mixture is then heated to 60 to 63° C., and the resulting solution is stirred at this temperature for 2 hours. After cooling to 55 to 60° C., a total of 2348 g of hydrochloric acid solution (20% strength in water) is added until the pH is 2.7, after which the product starts to crystallize. After cooling to 20° C., the precipitated reaction product is filtered off with suction, washed with methanol and then dried.

Provenance & Evidence