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}benzyl)phosphonate (Compound 10B, 589 mg, 872 μmol) to afford 296 mg of the title compound (53%). 1H NMR (400 MHz, CD3OD) δ 8.41 (br. s., 1H), 8.27 (s, 1H), 8.16 (s, 1H), 7.93 (s, 1H), 7.82 (d, J=1.5 Hz, 1H), 7.67 (d, J=8.6 Hz, 1H), 7.46 (d, J=8.1 Hz, 2H), 7.24 (d, J=7.6 Hz, 2H), 4.31 (t, J=6.8 Hz, 2H), 3.84 (t, J=6.9 Hz, 2H), 3.58 (t, J=6.1 Hz, 2H), 3.40 (q, J=7.1 Hz, 2H), 2.90-3.03 (m, 2H), 2.10 (t, J=6.3 Hz, 2H), 1.22 (t, J=7.2 Hz, 3H), 1.14 (t, J=6.9 Hz, 3H). MS (ESI): m/z 648.70 [M+H]+. UPLC: tR=1.04 min (UPLC-SQD: analytical—2 min).