2-((2-Chloro-5-(trifluoromethyl)pyrimidin-4-yl)amino)-N-methylbenzamide → Bis(2-hydroxyethyl)(3-methoxy-4-{[4-{[2-(methylcarbamoyl)phenyl]amino}-5-(trifluoromethyl)pyrimidin-2-yl]amino}benzyl)phosphonate

Participants

Reaction Steps

The title compound was prepared according to the procedure for Example 102 using bis(2-hydroxyethyl)(4-amino-3-methoxybenzyl)phosphonate (Compound 113A, 30 mg, 0.1 mmol) and 2-(2-chloro-5-(trifluoromethyl)pyrimidin-4-ylamino)-N-methylbenzamide (Compound 104A, 33 mg, 0.1 mmol). The reaction mixture was concentrated in vacuo and the residue was purified by HPLC to afford the title compound. 1H-NMR (DMSO-d6, 400 MHz): δ=2.83 (s, 3H), 3.35 (d, J=21.6 Hz, 2H), 3.60 (dd, J=5.2, 10.4 Hz, 4H), 3.84 (s, 3H), 3.99-4.03 (m, 4H), 4.95 (t, J=5.2 Hz, 2H), 6.92 (d, J=7.6 Hz, 1H), 7.11 (s, 1H), 7.16 (t, J=7.6 Hz, 1H), 7.45 (m, 1H), 7.61 (d, J=8.0 Hz, 1H), 7.73 (dd, J=1.2, 8.0 Hz, 1H), 8.43 (s, 1H), 8.48 (m, 1H), 8.80 (m, 2H), 11.49 (s, 1H). MS (ES+): m/z 600.11 [MH+]; HPLC: tR=2.80 min (ZQ3, polar—5 min).

Provenance & Evidence