Methylamine → HCID 69037538, compound

Participants

Reaction Steps

Using a procedure analogous to Example A1, 1-(1-tert-butyl-5-(trifluoromethyl)-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 (148 mg, 0.263 mmol), MCPBA (81 mg, 0.328 mmol) and 2.0N methylamine in THF (1.3 mL) were combined to afford 1-(1-tert-butyl-5-(trifluoromethyl)-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 (103 mg, 71% yield). 1H NMR (300 MHz, DMSO-d6): δ 1.59 (s, 9H), 2.08 (s, 3H), 2.92 (s, 3H), 3.55-3.62 (m, 3H), 7.25-7.30 (m, 1H), 7.69 (s, 1H), 7.70-7.80 (m, 1H), 7.93 (s, 1H), 7.95-8.05 (m, 1H), 8.51 (s, 1H), 8.20-8.25 (m, 1H), 9.04 (s, 1H); MS (ESI) m/z: 547.2 (M+H+).

Provenance & Evidence