反应详情

Prepared analogously to Compound 3A using diethyl (4-{[4-({2-(dimethylcarbamoyl)-4-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]phenyl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (Compound 12B, 72 mg, 102 μmol) to afford 39 mg of the title compound (56%). 1H NMR (400 MHz, CD3OD) δ 8.26 (s, 1H), 8.18 (s, 1H), 7.93 (s, 1H), 7.79-7.86 (m, 1H), 7.70-7.79 (m, 2H), 7.59 (d, J=2.0 Hz, 1H), 7.01 (s, 1H), 6.61 (br. s., 1H), 4.32 (t, J=6.8 Hz, 2H), 3.88 (s, 3H), 3.76 (quin, J=6.9 Hz, 2H), 3.59 (t, J=6.1 Hz, 2H), 3.04 (s, 3H), 2.90 (d, J=3.8 Hz, 4H), 2.85 (s, 1H), 2.04-2.17 (m, 2H), 1.11 (t, J=7.1 Hz, 3H). MS (ESI): m/z 678.70 [M+H]+. UPLC: tR=0.95 min (UPLC-SQD: analytical—2 min).