3-(3-Aminophenyl)-1,4-dimethylpiperazin-2-one → 3-{3-[7-(3-Methanesulfonyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino]-phenyl}-1,4-dimethyl-piperazin-2-one

Participants

Reaction Steps

3-{3-[7-(3-Methanesulfonyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino]-phenyl}-1,4-dimethyl-piperazin-2-one was prepared from 7-(3-methanesulfonyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-ol and 3-(3-amino-phenyl)-1,4-dimethyl-piperazin-2-one in an analogous manner to Example 1052a. Product isolated as an orange foam (69 mg, 46%). LCMS (m/e) 491 (M+H); 1H-NMR (CDCl3, 400 MHz) δ 8.75 (s, 1H), 8.59 (d, 1H, J=8.0 Hz), 8.52 (s, 1H), 7.91 (d, 1H, J=7.8 Hz), 7.84 (d, 1H, J=8.1 Hz), 7.75-7.66 (m, 1H), 7.41-7.33 (m, 1H), 7.10 (s, 1H), 7.12-7.04 (m, 2H), 6.89-6.81 (m, 2H) 3.76-3.66 (m, 2H), 3.27-3.18 (m, 1H), 3.09 (s, 3H), 3.06-2.96 (m, 1H), 2.98 (s, 3H), 2.74-2.62 (m, 1H), 2.19 (s, 3H).

Provenance & Evidence