1H-1,2,4-Triazole → HCID 135507498, compound

Participants

Reaction Steps

In a similar manner as described for Example 9, 5-nitro-N-(1-{3-[(3,4,5-trimethoxyphenyl)amino]-1,2,4-triazin-6-yl}ethyl)-1H-pyrrole-2-carboxamide (Intermediate 34) (201 mg, 0.45 mmol), and 1,2,4-triazole (190 mg, 2.72 mmol) in pyridine (10 mL) and phosphorous oxychloride (0.13 mL, 1.36 mmol) gave 5-methyl-7-(5-nitro-1H-pyrrol-2-yl)-N-(3,4,5-trimethoxyphenyl)-imidazo[5,1-f][1,2,4]triazin-2-amine (95 mg, 49%) as a yellow solid. 1H NMR (DMSO-d6): δ13.04 (s, 1H), 9.63 (s, 1H), 9.25 (s, 1H), 7.98 (dd, J=3.30 and 1.65 Hz, 1H), 7.57 (t, J=2.01 Hz, 1H), 7.05 (s, 2H), 3.74 (s, 6H), 3.65 (s, 3H), 2.54 (s, 3H). MS m/z 425 (M+1).

Provenance & Evidence