反应详情

2-Methanesulfinyl-7-(1-methyl-1H-pyrazol-4-yl)-pyrrolo[2,1-f][1,2,4]triazine (100.0 mg, 0.3827 mmol) was dissolved in 1-Methoxy-2-propanol (374.1 uL, 3.827 mmol) and added to 4-(3-Amino-phenoxy)-piperidine-1-carboxylic acid tert-butyl ester (223.8 mg, 0.7654 mmol) and N,N-Diisopropylethylamine (200.0 uL, 1.148 mmol). The substance was microwaved at 200 C for 15 min. The reaction was concentrated, dissolved in 1 mL of DMSO and placed onto the Gilson. Lyophilized overnight to give 3-{1-[7-(1-Methyl-1H-pyrazol-4-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-piperidin-4-yloxy}-phenylamine as a yellow solid (4 mg, 3%). LCMS (E/I+) 417 (M+H). NMR 1H (DMSO-d6)-8.82 (s, 1H), 8.39 (s, 1H), 8.16 (s, 1H), 7.24 (t, 1H, J=8.05 Hz), 7.05 (d, 1H, J=4.71 Hz), 6.87 (d, 1H, J=4.76 Hz), 6.77 (d, 1H, J=8.04 Hz), 6.69 (s, 1H), 6.65 (d, 1H, J=8.04 Hz), 4.62-4.68 (m, 1H), 4.08-4.16 (m, 2H), 3.93 (s, 3H), 3.50-3.6 (m, 2H), 2.04-2.12 (m, 2H), 1.66-1.76 (m, 2H).

1. customThe substance was microwaved at 200 C for 15 min
2. concentrationThe reaction was concentrated
3. dissolutiondissolved in 1 mL of DMSO