Diethyl (4-{[4-({7-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-2-methyl-3-oxo-2,3-dihydro-1H-isoindol-4-yl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate → Diethyl (4-{[4-({3-fluoro-4-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-2-(methylcarbamoyl)phenyl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxy benzyl)phosphonate

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Prepared analogously to Compound 1B replacing compound 1C with 6-amino-2-fluoro-3-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-N-methylbenzamide (281 mg, 961 μmol) to afford 204 mg of the title compound (30%). 1H NMR (400 MHz, CD3OD) δ=8.32 (s, 1H), 8.15 (d, J=1.8 Hz, 1H), 7.94-8.01 (m, 2H), 7.89 (d, J=8.1 Hz, 1H), 7.73 (t, J=8.6 Hz, 1H), 6.98 (t, J=2.0 Hz, 1H), 6.77 (d, J=8.1 Hz, 1H), 4.32 (t, J=7.0 Hz, 2H), 3.97-4.07 (m, 4H), 3.89 (s, 3H), 3.55-3.60 (m, 2H), 3.24 (s, 1H), 3.19 (s, 1H), 2.91 (s, 3H), 2.10 (quin, J=6.5 Hz, 2H), 1.23 (t, J=7.1 Hz, 6H). MS (ESI): m/z=710.21 [M+H]+. UPLC: tR=1.39 min (UPLC-TOF: polar—3 min).

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