Saccharin → 4-(Dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate disaccharin salt

Participants

Reaction Conditions

Reaction Steps

Saccharin (41.5 g) was added to a stirred solution of the product from step (vi) (50.0 g) in acetonitrile (150 mL). The mixture was heated to 40° C. and stirred at the temperature for 10 minutes. The mixture was diluted with EtOAc (500 mL), seeded with Form A crystals and stirred at 40° C. for 5 hours. The mixture was then cooled to 20° C. and stirred at the temperature for 2 hours. The resulting solid was collected by filtration, washed with EtOAc (200 mL) and dried under reduced pressure to give a crude sample of the subtitle compound as a white solid, 81.5 g.

Provenance & Evidence