反应详情

Using a procedure analogous to Example A1, 1-(1-tert-butyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)-3-(2-fluoro-5-(8-methyl-2-(methylthio)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (247 mg, 0.449 mmol) and 2.0N methylamine in THF (2.25 mL, 4.49 mmol) were combined to afford 1-(1-tert-butyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)-3-(2-fluoro-5-(8-methyl-2-(methylamino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (152 mg, 63% yield). 1H NMR (300 MHz, acetone-d6) δ 1.64 (s, 9H), 2.82 (s, 3H), 3.06 (m, 3H), 6.80-6.95 (m, 1H), 7.14-7.19 (m, 1H), 7.38-7.42 (m, 1H), 7.85 (s, 1H), 8.06 (s, 1H), 8.11 (br. s, 1H), 8.50 (br. s, 1H), 8.57-8.59 (m, 1H), 8.60-8.63 (m, 1H); MS (ESI) m/z: 533.3 (M+H+).