反应详情

Prepared analogously to Compound 3A with diethyl (4-{[4-({4-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-2-(methylcarbamoyl)phenyl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (234 mg, 338 μmol) to yield 156 mg of the desired product (70%). 1H NMR (400 MHz, CD3OD) δ 8.30-8.36 (m, 1H), 8.26 (s, 1H), 8.14 (s, 1H), 7.92 (s, 1H), 7.86 (d, J=8.08 Hz, 1H), 7.83 (d, J=2.02 Hz, 1H), 7.63 (dd, J=2.02, 8.59 Hz, 1H), 7.04 (s, 1H), 6.80 (s, 1H), 4.30 (t, J=6.82 Hz, 2H), 3.88 (s, 3H), 3.84 (t, J=6.95 Hz, 2H), 3.58 (t, J=6.19 Hz, 2H), 2.92-3.02 (d, J=21.9 Hz, 2H), 2.91 (s, 3H), 2.10 (t, J=6.44 Hz, 2H), 1.15 (t, J=6.95 Hz, 3H). MS (ESI): m/z 664.21 [M+H]+. UPLC: tR=1.13 min (UPLC-TOF: polar—3 min).