1H-1,2,4-Triazole → HCID 11200247, compound

Participants

Reaction Steps

In a similar manner as described for Example 9, 1-methyl-N-(1-{3-[(3,4,5-trimethoxyphenyl)amino]-1,2,4-triazin-6-yl}ethyl)-1H-pyrrole-2-carboxamide (Intermediate 35) (222 mg, 0.54 mmol), and 1,2,4-triazole (220 mg, 3.2 mmol) in pyridine (10 mL) and phosphorous oxychloride (0.15 mL, 1.6 mmol) gave 5-methyl-7-(1-methyl-1H-pyrrol-2-yl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine (52 mg, 25%) as a yellow solid. 1H NMR (DMSO-d6): δ9.54 (s, 1H), 9.18 (s, 1H), 7.19 (d, J=2.01 Hz, 1H), 7.16 (s, 2H), 6.98 (s, 1H), 6.14 (t, J=3.02 Hz, 1H), 3.96 (s, 3H), 3.74 (s, 6H), 3.61 (s, 3H), 2.51 (s, 3H). MS m/z 394 (M+1).

Provenance & Evidence