3-(Phenylsulfonyl)pyrrolidine → 5-{9-(Cyclopropylmethyl)-6-morpholin-4-yl-8-[3-(phenylsulfonyl)pyrrolidin-1-yl]-9H-purin-2-yl}pyrimidin-2-amine

Participants

Reaction Conditions

Reaction Steps

3-(Phenylsulfonyl)pyrrolidine (110 mg, 0.52 mmol) and dimethyl sulfoxide (0.8 ml) were added to 5-[8-chloro-9-(cyclopropylmethyl)-6-morpholin-4-yl-9H-purin-2-yl]pyrimidin-2-amine (80 mg, 0.21 mmol) and the resulting mixture was stirred at 150° C. for 4 hours. The reaction mixture was partitioned with ethyl acetate and water and the organic layer was washed with saturated brine and dried over magnesium sulfate. The solvent was evaporated under reduced pressure and then the residue was purified by silica gel chromatography (ethyl acetate:hexane=2:1) to give the title compound (20 mg, 17%) as a white solid.

Provenance & Evidence