反应详情

To a solution of N-(1-(tert-butyldimethylsilyloxy)-2-methylpropan-2-yl)-2-(1-(2-(dimethylamino)ethyl)-6-methyl-1H-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide (127 mg, 0.23 mmol) in 5 mL of methanol and 1 mL of THF was added 1 mL of concentrated HCl, then stirred for 3 hours. The precipitate was filtered and filter cake was washed with 2-methoxy-2-methylpropane (5 mL) to give 25 mg of 2-(1-(2-(dimethylamino)ethyl)-6-methyl-1H-indazol-3-yl)-N-(1-hydroxy-2-methylpropan-2-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide hydrochloride. LCMS: (M+H)+=436; 1H NMR (300 MHz, DMSO): δ 12.85 (s, 1H), 10.19 (s, 1H), 9.18 (s, 1H), 8.47 (d, 1H, J=8.1 Hz), 8.37 (s, 1H), 7.92 (s, 1H), 7.68 (s, 1H), 7.17 (d, 1H, J=8.4 Hz), 4.93 (s, 2H), 3.70-3.63 (m, 4H), 2.89 (s, 6H), 2.50 (s, 3H), 1.45 (s, 6H).

1. filtrationThe precipitate was filtered
2. filtrationfilter cake
3. washwas washed with 2-methoxy-2-methylpropane (5 mL)