反应详情

tert-Butyl 4-(2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamido)-4-methylpiperidine-1-carboxylate (100 mg, 0.20 mmol) was dissolved in 30 mL of a saturated solution of HCl (g) in dioxane and the solution was stirred at room temperature for 16 hours. The reaction mixture was filtered, washed with dichloromethane (20 mL), diethyl ether (30 mL) and dried to give 2-(6-fluoro-1-methyl-1H-indazol-3-yl)-N-(4-methylpiperidin-4-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide hydrochloride (29 mg, 33.2%) as a white solid. MS: (M+H)+=408; 1H NMR (300 MHz, DMSO): δ 9.16 (s, 1H), 8.57-8.41 (m, 4H), 7.92 (s, 1H), 7.75 (d, 1H, J=10.5 Hz), 7.32-7.26 (m, 1H), 6.98-6.93 (m, 1H), 5.75 (d, 2H, J=6.9 Hz), 4.19 (s, 3H), 3.16 (brs, 5H), 1.96 (brs, 3H), 1.61 (s, 3H).

1. filtrationThe reaction mixture was filtered
2. washwashed with dichloromethane (20 mL), diethyl ether (30 mL)
3. customdried