Methylamine → HCID 69037736, compound

Participants

Reaction Steps

Using a procedure analogous to Example A1, 1-(1-tert-butyl-5-methyl-1H-pyrazol-4-yl)-3-(2-fluoro-4-methyl-5-(8-methyl-2-(methylthio)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (31 mg, 0.061 mmol), MCPBA (19 mg, 0.079 mmol) and 2.0N methylamine in THF (0.4 mL) were converted to 1-(1-tert-butyl-5-methyl-1H-pyrazol-4-yl)-3-(2-fluoro-4-methyl-5-(8-methyl-2-(methylamino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (15 mg, 50% yield). 1H NMR (300 MHz, DMSO-d6), δ 1.60 (s, 9H), 2.20 (s, 3H), 2.35 (s, 3H), 2.95 (s, 3H), 3.60-3.70 (m, 3H), 7.20-7.25 (m, 1H), 7.50 (s, 1H), 7.70 (s, 1H), 7.70-7.90 (m, 1H), 8.05 (m, 1H), 8.20 (s, 1H), 8.55 (m, 1H), 8.70-8.80 (m, 1H); MS (ESI) m/z: 493.0 (M+H+).

Provenance & Evidence