反应详情

In a similar manner as described for Example 9, methyl 4-{[(1-{3-[(3,4,5-trimethoxyphenyl)amino]-1,2,4-triazin-6-yl}ethyl)amino]carbonyl}benzoate (Intermediate 30) (56 mg, 0.12 mmol), and 1,2,4-triazole (55 mg, 0.80 mmol) in pyridine (2 mL) and phosphorous oxychloride (0.037 mL, 0.40 mmol) gave methyl 4-{5-methyl-2-[(3,4,5-trimethoxyphenyl)amino]imidazo[5,1-f][1,2,4]triazin-7-yl}benzoate (11 mg, 20%) as a yellow solid. 1H NMR (CD3OD): δ9.06 (s, 1H), 9.01 (s, 1H), 8.58 (d, J=7.87 Hz, 1H), 8.08 (d, J=7.87 Hz, 1H), 7.62 (t, J=7.87 Hz, 1H), 7.04 (s, 2H), 5.48 (s, 1H), 3.87 (s, 3.75 (s, 3H), 3.71 (s, 6H), 2.59 (s, 3H). MS m/z 449 (M+1).