Methylamine → HCID 69297474, compound

Participants

Reaction Steps

Using a procedure analogous to Example A1, 1-(1-tert-butyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)-3-(4-chloro-2-fluoro-5-(8-methyl-2-(methylthio)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (230 mg, 0.394 mmol), MCPBA (126 mg, 0.512 mmol) and 2.0N methylamine in THF (1.97 mL, 3.94 mmol) were combined to afford 1-(1-tert-butyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)-3-(4-chloro-2-fluoro-5-(8-methyl-2-(methylamino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (127 mg, 56% yield). 1H NMR (300 MHz, DMSO-d6), δ 1.59 (s, 9H), 2.92 (s, 3H), 3.53-3.62 (m, 3H), 7.55-7.65 (m, 1H), 7.78 (s, 1H), 7.80-7.90 (m, 1H), 7.93 (s, 1H), 8.15-8.25 (m, 1H), 8.45-8.70 (m, 2H), 9.25 (s, 1H); MS (ESI) m/z: 567.0 (M+H+).

Provenance & Evidence