反应详情

The title product was prepared according to the procedure for Example 102 2-{[2-chloro-5-(trifluoromethyl)pyrimidin-4-yl]amino}-N-methylbenzamide (Compound 104A, 40.0 mg, 0.12 mmol) and diethyl[(4-aminophenyl)(difluoro)methyl]-phosphonate (Compound 188A, 40.5 mg, 0.15 mmol). The crude product was purified by silica gel chromatography (5% 7 N NH3 in MeOH in DCM) to afford the desired product as a white solid (4.1 mg, yield: 6%). 1H NMR (CD3OD, 400 MHz): δ=1.32 (t, J=7.2 Hz, 6H), 2.90 (s, 3H), 4.14-4.25 (m, 4H), 7.22 (t, J=8.4 Hz, 1H), 7.45 (d, J=8.4 Hz, 2H), 7.51 (dt, J=1.2, 7.2 Hz, 1H), 7.66 (dd, J=1.2, 7.6 Hz, 1H), 7.79 (d, J=8.8 Hz, 2), 8.39 (s, 1H), 8.47 (d, J=8.4 Hz, 1H). MS (ES+): m/z 574.12 [MH+]. HPLC: tR=4.13 min (OpenLynx, polar—5 min).

1. customThe title product was prepared
2. customThe crude product was purified by silica gel chromatography (5% 7 N NH3 in MeOH in DCM)