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)-1H-pyrazol-4-yl]-2-(methylcarbamoyl)pyridin-3-yl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methylbenzyl)phosphonate

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Prepared analogously to Compound 3A using diethyl (4-{[4-({6-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-2-(methylcarbamoyl)pyridin-3-yl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methylbenzyl)phosphonate (Compound 33B, 345 mg, 510 μmol) to afford 330 mg of the title compound (99.8%). 1H NMR (400 MHz, CD3OD) δ 8.71-8.96 (m, 1H), 8.60 (s, 1H), 8.28 (s, 1H), 8.23 (s, 1H), 7.63 (d, J=9.1 Hz, 1H), 7.34 (s, 1H), 7.22-7.28 (m, 2H), 4.32 (t, J=6.8 Hz, 2H), 3.88 (t, J=7.0 Hz, 2H), 3.59 (t, J=6.1 Hz, 2H), 3.06 (d, J=21.9 Hz, 2H), 2.98 (s, 3H), 2.23 (s, 3H), 2.11 (t, J=6.3 Hz, 2H), 1.12 (t, J=7.1 Hz, 3H). MS (ESI): m/z=649.65 [M+H]+. UPLC: tR=1.06 min (UPLC-SQD: analytical—2 min).

Provenance & Evidence