反应详情

Prepared analogously to Compound 3A using diethyl (4-{[4-({2-(ethylcarbamoyl)-4-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]phenyl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (Compound 9B, 570 mg, 808 μmol) to afford the title compound as 349 mg of a white solid (65%). 1H NMR (400 MHz, CD3OD) δ 8.30 (d, J=8.6 Hz, 1H), 8.27 (s, 1H), 8.16 (s, 1H), 7.93 (s, 1H), 7.85 (d, J=8.1 Hz, 1H), 7.82 (d, J=2.0 Hz, 1H), 7.66 (dd, J=2.0, 8.6 Hz, 1H), 7.05 (s, 1H), 6.80 (d, J=8.3 Hz, 1H), 4.31 (t, J=6.8 Hz, 2H), 3.89 (s, 3H), 3.83 (quin, J=6.9 Hz, 2H), 3.58 (t, J=6.1 Hz, 2H), 3.40 (q, J=7.2 Hz, 2H), 2.91-3.01 (m, 2H), 2.10 (quin, J=6.4 Hz, 2H), 1.22 (t, J=7.2 Hz, 3H), 1.12-1.17 (m, 3H). MS (ESI): m/z 678.74 [M+H]+. UPLC: tR=1.07 min (UPLC-SQD: analytical—2 min).