Diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-ethoxybenzyl)phosphonate → HCID 178466847, compound

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Reaction Steps

The title compound was prepared according to the procedure for Example 102 using of diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-ethoxybenzyl)phosphonate (Compound 244A, 29.84 mg, 0.064 mmol) and ethyl trans-4-(7-amino-2-methyl-1-oxo-2,3-dihydro-1H-isoindol-4-yl)cyclohexanecarboxylate (22.2 mg, 0.070 mmol). 31.2 mg (65%) of the desired product was isolated after work-up/chromatography. 1H NMR (400 MHz, MeOD) δ ppm 8.48 (d, J=7.83 Hz, 1 H), 8.35 (s, 1 H), 7.87 (d, J=8.08 Hz, 1 H), 7.38 (d, J=8.84 Hz, 1 H), 7.05 (s, 1 H), 6.94 (dt, J=8.08, 2.27 Hz, 1 H), 4.52 (s, 2 H), 4.04-4.22 (m, 8 H), 3.28 (s, 2 H), 3.19 (s, 3 H), 2.63 (t, J=11.62 Hz, 1 H), 2.42-2.54 (m, 1 H), 2.13 (d, J=14.15 Hz, 2 H), 1.90-1.99 (m, 2 H), 1.54-1.77 (m, 4 H), 1.41 (t, J=6.95 Hz, 3 H), 1.24-1.33 (m, 9 H). MS (ES+): m/z 748.26/749.29 (100/98) [MH+]. HPLC: tR=1.80 min (Micromass TOF: polar—3 min).

Provenance & Evidence