5-Aminobenzimidazole → HCID 66712588, compound

Participants

Reaction Steps

Following the synthetic and purification procedures described in Example 1293d, 2-methanesulfinyl-7-(2-methoxy-phenyl)-pyrrolo[2,1-f][1,2,4]triazine (75.4 mg, 0.262 mmol) was coupled to 3H-benzimidazol-5-ylamine (60.0 mg, 0.45 mmol) at 105° C. for 86 h to afford the title compound. Yield of TFA salt: 62 mg (50%) of brown powder. LC/MS: 357 (M+H); HPLC: 95% pure, RT=2.38 min; 1H NMR: (DMSO, δ) 9.77 (s, 1H), 9.38 (s, 1H), 9.02 (s, 1H), 8.04 (s, 1H), 7.93 (d, J=9.2, 1H), 7.85 (d, J=7.5, 1H), 7.65 (d, J=9.2, 1H), 7.47 (t, J=8.2, 1H), 7.25 (d, J=8.2, 1H), 7.17 (t, J=7.5, 1H), 7.01 (d, J=4.8, 1H), 6.98 (d, J=4.8, 1H), 3.81 (s, 3H)-benzimidazole NH presumably underwent rapid exchange with residual water.

Provenance & Evidence