[3-(Hydroxymethyl)phenyl]boronic acid → (3-{2-[4-(4-Methyl-piperazin-1-yl)-phenylamino]-pyrrolo[2,1-f][1,2,4]triazin-7-yl}-phenyl)-methanol

Participants

Reaction Steps

Analogous to Example 1497, (7-Bromo-pyrrolo[2,1-f][1,2,4]triazin-2-yl)-[4-(4-methyl-piperazin-1-yl)-phenyl]-amine (0.125 g, 0.323 mmol) and (3-Hydroxymethylphenyl)-boronic acid (98.1 mg, 0.646 mmol) were reacted to afford (3-{2-[4-(4-Methyl-piperazin-1-yl)-phenylamino]-pyrrolo[2,1-f][1,2,4]triazin-7-yl}-phenyl)-methanol (109 mg; Yield=81.5%). LCMS (HPLC): 0.74 min, m/z=415 (M+H); 1H-NMR (DMSO-d6): 9.22 (s, 1H), 8.93 (s, 1H), 8.19 (s, 1H), 7.99 (d, 1H, J=7.8 Hz), 7.64 (d, 2H, J=9.0 Hz), 7.49 (m, 1H), 7.37 (d, 1H, J=7.6 Hz), 7.13 (d, 1H, J=4.7 Hz), 6.92 (m, 3H), 5.25 (t, 1H, J=5.8 Hz), 4.60 (d, 2H, J=5.8 Hz), 3.08 (m, 4H), 2.46 (m, 4H), 2.23 (s, 3H).

Provenance & Evidence