反应详情

To a stirred solution of (2-(6-cyano-1-methyl-1H-indazol-3-yl)-7-(1-hydroxy-2-methylpropan-2-ylcarbamoyl)-5H-pyrrolo[2,3-b]pyrazin-5-yl)methyl pivalate (45 mg, 0.089 mmol) in 2 mL of THF was added a solution of 10% NaOH (2 mL) at room temperature and the reaction mixture was stirred for 15 hours. The solvent was evaporated under reduced pressure. The residue was diluted with water and adjusted to pH 5-6. The mixture was filtered and the filter cake washed with DMSO (3 mL), MeOH (3 mL) and then dried to give 2-(6-cyano-1-methyl-1H-indazol-3-yl)-N-(1-hydroxy-2-methylpropan-2-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide (4.5 mg, 12%) as white solid. MS: (M+H)+=390; 1H NMR (300 MHz, DMSO): δ 12.95 (brs, 1H), 9.14 (s, 1H), 8.79 (d, 1H, J=8.1 Hz), 8.54 (s, 1H), 8.42 (s, 1H), 7.91 (s, 1H), 7.62 (d, 1H, J=8.4 Hz), 5.15 (brs, 1H), 4.27 (s, 3H), 3.64 (d, 2H, J=5.4 Hz), 1.47 (s, 6H).

1. customThe solvent was evaporated under reduced pressure
2. additionThe residue was diluted with water
3. filtrationThe mixture was filtered
4. washthe filter cake washed with DMSO (3 mL), MeOH (3 mL)
5. customdried