反应详情

A solution of 5-(2-benzyl-2H-indazol-6-yl)-7-(4-benzylmorpholin-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (200 mg, 0.388 mmol) and 25 mg 10% by wt. palladium on carbon in acetic acid (5 mL) was stirred under an atmosphere of hydrogen for 52 h. The reaction was filtered through Celite® and concentrated in vacuo. The residue was purified by preparative RP-HPLC to provide 35.1 mg (27%) of the desired product. 1H NMR (300 MHz, DMSO-d6) δ 8.10 (s, 1 H), 7.92 (s, 1 H), 7.83 (d, 1 H, J=8 Hz), 7.52 (s, 1 H), 7.19 (d, 1 H, J=8 Hz), 6.73 (s, 1 H), 4.98 (dd, 1 H, J=10, 2 Hz) (m, 1 H), 3.81 (d, 1H, J=11 Hz), 3.55-3.66 (m, 2H), 3.31 (bs, 3H), 3.05 (dd, 1H, J=12, 3 Hz), 2.86 (dd, 1H, J=12, 10 Hz), 2.71-2.78 (m, 2H); ES-MS m/z 336.4 [M+H]+, HPLC RT (min) 1.10.

1. filtrationThe reaction was filtered through Celite®
2. concentrationconcentrated in vacuo
3. customThe residue was purified by preparative RP-HPLC