反应详情

Prepared analogously to Compound 3A using diethyl (4-{[4-({4-[1-(4-hydroxybutyl)-1H-pyrazol-4-yl]-2-(methylcarbamoyl)phenyl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (Compound 14B, 63.6 mg, 0.09 mmol) to afford 59 mg of the title compound (96%). 1H NMR (400 MHz, CD3OD) δ 8.34 (d, J=8.6 Hz, 1H), 8.28 (s, 1H), 8.15 (s, 1H), 7.91 (d, J=0.5 Hz, 1H), 7.87 (d, J=8.1 Hz, 1H), 7.83 (d, J=2.3 Hz, 1H), 7.65 (dd, J=2.15, 8.72 Hz, 1H), 7.06 (t, J=1.9 Hz, 1H), 6.80 (dd, J=1.9, 8.2 Hz, 1H), 4.23 (t, J=6.9 Hz, 2H), 3.90 (s, 3H), 3.83 (quin, J=7.0 Hz, 2H), 3.56-3.62 (m, 2H), 2.93-3.00 (m, 2H), 2.91 (s, 3H), 1.92-2.02 (m, 2H), 1.50-1.60 (m, 2H), 1.14 (t, J=7.1 Hz, 3H). MS (ESI): m/z 678.79 [M+H]+. UPLC: tR=1.02 min (UPLC-SQD: analytical—2 min).