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-({6-[3-chloro-1-(3-hydroxypropyl)-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 1B using 3-amino-6-[3-chloro-1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-N-methylpyridine-2-carboxamide (Compound 49C, 365 mg, 1.18 mmol) to afford 480 mg of the title compound (59%). 1H NMR (400 MHz, CD3OD) δ 9.06 (br. s., 1H), 8.51 (s, 1H), 8.35 (s, 1H), 7.89 (d, J=9.1 Hz, 1H), 7.82 (d, J=8.1 Hz, 1H), 7.04 (t, J=2.0 Hz, 1H), 6.91 (td, J=2.3, 8.1 Hz, 1H), 4.26 (t, J=6.9 Hz, 2H), 4.00-4.11 (m, 4H), 3.89 (s, 3H), 3.59 (t, J=6.1 Hz, 2H), 3.35 (s, 1H), 3.23 (s, 1H), 2.98 (s, 3H), 2.11 (quin, J=6.5 Hz, 2H), 1.22-1.29 (m, 6H). MS (ESI): m/z=727.38/729.32 [M+H]+. UPLC: tR=1.35 min (UPLC-TOF: polar—2 min).

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