Morpholine → HCID 11156013, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 6-[(4-methylphenylsulphonyloxy)methyl]-2-{2-[3-(pyrid-2-yl)isoxazol-5-yl]pyrrolidin-1-yl}-4-(5-methyl-2-N-[4-methylphenylsulphonyl]-1H-pyrazol-3-ylamino)pyrimidine (Method 52) (214 mg, 0.295 mmol) and morpholine (5 ml, 83.2 mmol) was heated at reflux for 2 hours. The volatiles were removed by evaporation and the residue was dissolved in methanol (10 ml) and 10M aqueous sodium hydroxide solution (3 ml). The mixture was heated at 60° C. for 1 hour. The volatiles were removed by evaporation and the residue dissolved in water, extracted with dichloromethane. The extracts were combined and the solvent removed by evaporation. The residue was purified by chromatography on silica gel, eluting with dichloromethane (100%) and then diethylether (100%). The purified product was triturated with diethylether and collected by filtration to give the title compound (125 mg).

Provenance & Evidence