Methylamine → HCID 24811038, compound

Participants

Reaction Steps

Using a procedure analogous to Example A2, the sulfide was oxidized with mCPBA to the sulfone and then treated with methylamine to provide 1-(1-tert-butyl-1H-pyrazol-4-yl)-3-(4-chloro-2-fluoro-5-(1-methyl-7-(methylamino)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)urea (0.448 mmol, 73% yield). 1H NMR (400 MHz, DMSO-d6): δ 8.76 (s, 1H), 8.72 (brs, 1H), 8.32 (d, J=8.5 Hz, 1H), 7.96 (brs, 1H), 7.82 (s, 1H), 7.60 (d, J=11 Hz, 1H), 7.41 (s, 1H), 7.04 m, 1H), 6.34 s, 1H), 4.56 (d, J=14 Hz, 1H), 4.41 (d, J=14 Hz, 1H), 3.25 (brs, 3H), 2.78 (d, J=5 Hz, 3H), 1.47 (m, 9H); MS (ESI) m/z: 502.2 (M+H).

Provenance & Evidence