Ethanol → 5-Chloro-N-((2R)-2-hydroxy-3-((4-(3-oxo-4-morpholinyl)phenyl)amino)propyl)-2-thiophenecarboxamide

Participants

Reaction Conditions

Reaction Steps

55 g of N-((S)-3-bromo-2-hydroxypropyl)-5-chlorothiophene-2-carboxamide (IX) and 29.4 g of 4-(4-aminophenyl)-3-morpholinone (III) (a preparation method is described, for example, in WO-A 01/47919 on pages 55 to 57) are suspended at from 20 to 25° C. in 500 ml of toluene and admixed with 18.5 g of collidine and 10 ml of ethanol. The reaction mixture is heated to from 103 to 105° C. for 6 hours and then admixed while hot with 50 ml of 1-butanol. After cooling to 30° C., the precipitated reaction product is filtered off with suction, washed with toluene and water and dried.

Provenance & Evidence