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-(4-hydroxy-2-methylbutan-2-yl)-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-(4-hydroxy-2-methylbutan-2-yl)-1H-pyrazol-4-yl]-2-(methylcarbamoyl)pyridin-3-yl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (Compound 50B, 117 mg, 0.163 mmol) to afford 88.6 mg of the title compound (79%). 1H NMR (400 MHz, CD3OD) δ 8.76 (s, 1H), 8.35 (s, 1H), 8.11 (d, J=8.6 Hz, 1H), 7.83 (d, J=8.6 Hz, 1H), 7.50 (d, J=8.1 Hz, 1H), 6.85 (s, 1H), 6.52 (d, J=8.1 Hz, 2H), 3.72-3.98 (m, 7H), 3.15-3.25 (m, 2H), 2.94 (s, 3H), 2.30-2.43 (m, 2H), 1.77 (s, 6H), 1.11 (t, J=7.1 Hz, 3H). MS (ESI): m/z=693.61 [M+H]+. UPLC: tR=1.18 min (UPLC-TOF: polar—2 min).

Provenance & Evidence