Methylamine → HCID 69096056, compound

Participants

Reaction Steps

Using a procedure analogous to Example A1, 1-(1-tert-butyl-5-methyl-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 (80 mg, 0.151 mmol), MCPBA (47 mg, 0.189 mmol) and 2.0N methylamine in THF (0.8 mL) were combined to afford 1-(1-tert-butyl-5-methyl-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 (48 mg, 62% yield). 1H NMR (300 MHz, DMSO-d6): δ 1.49 (s, 9H), 2.27 (s, 3H), 2.89 (s, 3H), 3.49-3.56 (m, 3H), 7.39 (s, 1H), 7.49 (d, 1H), 7.74 (s, 1H), 7.94 (br. s, 1H), 8.17 (d, 1H), 8.29 (s, 1H), 8.62-8.74 (m, 2H); MS (ESI) m/z: 513.0 (M+H+).

Provenance & Evidence