HCID 67063098, compound → HCID 67063019, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of Example A1 (700 mg, 2.2 mmol) in THF (10 mL) was added Raney-Ni (50% wt slurry in water, 1.0 g) and then the reaction mixture was stirred under 1 atm of H2 at 60° C. for 5 h. The mixture was filtered through diatomite and the cake was washed with THF. The combined filtrate was concentrated to give 3-(3-amino-4-fluoro-phenyl)-1-methyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one (460 mg, 76% yield) as a yellow solid. 1H NMR (300 MHz, DMSO-d6): δ 8.77 (s, 1 H), 8.39 (s, 1 H), 6.99 (dd, J=11.4, 8.7 Hz, 1 H), 6.72 (d, J=8.1 Hz, 1 H), 6.49 (m, 1 H), 5.24 (br s, 2 H), 4.73 (s, 2 H), 3.28 (s, 3 H). MS (ESI) m/z: 274.2 (M+H+).

Provenance & Evidence