Ethyl hydrogen (4-{[4-({2-(diethylcarbamoyl)-4-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]phenyl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate → Ethyl hydrogen (4-{[4-({6-[1-(3-hydroxypropyl)-3-methoxy-1H-pyrazol-4-yl]-2-(methylcarbamoyl)pyridin-3-yl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate

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Prepared analogously to Compound 3A using diethyl (4-{[4-({6-[1-(3-hydroxypropyl)-3-methoxy-1H-pyrazol-4-yl]-2-(methylcarbamoyl)pyridin-3-yl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (Compound 48B, 286 mg, 0.395 mmol) affording 132 mg of the title compound (48%). 1H NMR (400 MHz, CD3OD) δ 8.86 (br. s., 1H), 8.29 (br. s., 2H), 7.63-7.77 (m, 2H), 7.12 (s, 1H), 6.88 (d, J=8.1 Hz, 1H), 4.14 (t, J=6.7 Hz, 2H), 4.07 (s, 3H), 3.80-3.90 (m, 5H), 3.59 (t, J=6.1 Hz, 2H), 2.99-3.08 (m, 2H), 2.96 (s, 3H), 2.07 (quin, J=6.4 Hz, 2H), 1.17 (t, J=7.1 Hz, 3H). MS (ESI): m/z=695.56 [M+H]+. UPLC: tR=1.15 min (UPLC-TOF: polar—2 min).

Provenance & Evidence