[C:1]12([NH:6][C:7]3[C:12]([C:13]#[N:14])=[CH:11][N:10]=[C:9]([S:15][CH3:16])[N:8]=3)[CH2:5][CH:3]([CH2:4]1)[CH2:2]2.[OH:17]O.[OH-].[Na+]>CS(C)=O>[C:1]12([NH:6][C:7]3[C:12]([C:13]([NH2:14])=[O:17])=[CH:11][N:10]=[C:9]([S:15][CH3:16])[N:8]=3)[CH2:2][CH:3]([CH2:5]1)[CH2:4]2To a solution of 4-(bicyclo[1.1.1]pentan-1-ylamino)-2-(methylthio)-pyrimidine-5-carbonitrile (3.45 g, 14.9 mmol) in DMSO (15 mL) was added aqueous hydrogen peroxide solution (8.4 g, 30%, 74.5 mmol) and aqueous sodium hydroxide solution (12.4 mL, 6 mol/L, 74.5 mmol) at 0° C. The mixture was stirred at 50° C. for 15 min and then quenched by the addition of water (30 mL). The solid formed was collected and dried under vacuum to give the desired product (3.5 g, 14.0 mmol, 94% yield). MS (ESI)/m/z=251.2 [M+1]+.
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