反应详情

2-Methanesulfinyl-7-(3-methanesulfonyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazine (100 mg, 0.298 mmol), 4-(1,1-dioxo-1$1(6)-thiomorpholin-4-ylmethyl)-phenylamine (158 mg, 0.656 mmol), and N,N-diisopropylethylamine (114 μL, 0.656 mmol) were placed in 1-methoxy-2-propanol (728 μL). The reaction was microwaved on 300 watts, 170° C. for 8 hours. Purification by prep-HPLC using a gradient of 10-70% AcN/water both containing 0.1% TFA as the eluting solvent. The product was then free based to obtain the title compound as an orange foam (18 mg, 12%). LCMS (m/e) 512 (M+H); 1H-NMR (CDCl3, 400 MHz) δ 8.76 (s, 1H), 8.71 (s, 1H), 8.34 (d, 1H, J=7.9 Hz), 7.94 (d, 1H, J=7.8 Hz), 7.73-7.66 (m, 1H), 7.58 (d, 2H, J=8.3 Hz), 7.31 (d, 2H, J=8.3 Hz), 7.05 (d, 1H, J=4.8 Hz), 6.99 (s, 1H), 6.87 (d, 1H, J=4.8 Hz), 3.63 (s, 2H), 3.09 (s, 3H), 3.09-3.03 (m, 4H), 3.03-2.94 (m, 4H).

1. customThe reaction was microwaved on 300 watts, 170° C. for 8 hours
2. customPurification