Methanesulfonyl chloride → N-(6-((5-chloro-2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)hexahydrofuro[3,2-b]furan-3-yl)methanesulfonamide

Participants

Reaction Conditions

Reaction Steps

To a solution of N4-(6-aminohexahydrofuro[3,2-b]furan-3-yl)-5-chloro-N2-(1-methyl-1H-pyrazol-4-yl)pyrimidine-2,4-diamine (57.0 mg, 0.16 mmol) in dichloromethane (5 mL) were added TEA (26.2 mg, 0.26 mmol) and N,N-dimethylpyridin-4-amine (4.1 mg, 0.03 mmol). The mixture was cooled to 0° C., and methanesulfonyl chloride (28.3 mg, 0.25 mmol) was added to. The mixture was stirred at 0° C. for 30 min, and stirred at room temperature overnight. The solution was concentrated in vacuo, and the residue was purified with a silica gel column chromatography (MeOH/DCM (v/v)=1/30) to afford the target product as an off-white solid (28.0 mg, 40.2%).

Provenance & Evidence