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-({3-chloro-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 3A using diethyl (4-{[4-({3-chloro-4-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-2-(methylcarbamoyl)phenyl}amino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (Compound 28B, 18 mg, 24.8 μmol) to afford 19.4 mg of the title compound. 1H NMR (400 MHz, CD3OD) δ=8.29 (s, 1H), 8.21 (s, 1H), 7.99 (d, J=8.6 Hz, 1H), 7.95 (d, J=1.8 Hz, 1H), 7.81 (d, J=8.1 Hz, 1H), 7.74 (t, J=8.6 Hz, 1H), 7.05 (s, 1H), 6.76 (d, J=8.3 Hz, 1H), 4.33 (t, J=6.8 Hz, 2H), 3.89 (s, 3H), 3.82 (s, 2H), 3.58 (t, J=6.1 Hz, 2H), 2.96 (s, 1H), 2.92 (s, 4H), 2.10 (quin, J=6.51 Hz, 2H), 1.13 (t, J=6.95 Hz, 3H). MS (ESI): m/z=698.19 [M+H]+. UPLC: tR=1.06 min (UPLC-TOF: polar—3 min).

Provenance & Evidence