2-Amino-5-fluoro-N-methylbenzamide → ethyl[5-{[2-({4-[(diethoxyphosphoryl)methyl]-2-methoxyphenyl}amino)-5-(trifluoromethyl)pyrimidin-4-yl]amino}-3-methyl-4-oxoquinolin-1(4H)-yl]acetate

Participants

Reaction Steps

The title compound was prepared according to Compound 102A using diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (50.0 mg, 0.110 mmol) and ethyl (5-amino-3-methyl-4-oxoquinolin-1(4H)-yl)acetate (Example 301A, 31.5 mg, 0.121 mmol). 1H NMR (CD3OD, 400 MHz): δ=1.24-1.32 (m, 9H), 2.12 (s, 3H), 3.29 (d, J=21.2 Hz, 2H), 4.05-4.16 (m, 6H), 4.84 (s, 2H), 6.91 (dt, J=2.8, 8.4 Hz, 1H), 7.04 (t, J=2.0 Hz, 1 H), 7.40 (d, J=8.8 Hz, 1H), 7.60 (t, J=8.4 Hz, 1H), 7.89 (s, 1H), 7.98 (d, J=8.0 Hz, 1H), 8.37 (s, 1H), 8.66 (d, J=7.6 Hz, 1H). MS (ES+): m/z 678.17 [MH+]. HPLC: tR=1.50 min (UPLC TOF, polar—3 min).

Provenance & Evidence