Methylamine → HCID 67063103, compound

Participants

Reaction Steps

Using a procedure analogous to Example A2, 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-5-(1-methyl-7-(methylthio)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)urea was oxidized with mCPBA to the sulfone and then treated with methylamine to provide 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-5-(1-methyl-7-(methylamino)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)urea (0.045 g, 16% yield). 1H NMR (400 MHz, DMSO-d6: δ 9.55 (s, 1H), 8.77 (s, 1H), 8.12 (d, J=2.5 Hz, 1H)), 8.09 (dd, J=8, 2.5 Hz, 1H), 7.96 (brs, 1H), 7.59 (m, 2H), 7.28 (dd, J=12.9 Hz, 1H), 7.01 (m, 2H), 5.74 (s, 1H), 4.58 (s, 2H), 3.28 (brs, 3H), 2.78 (d, J=5 Hz, 3H); MS (ESI) m/z: 524.0 (M+H+)

Provenance & Evidence