反应详情

温度

75 °C

A 5M solution of hydrogen chloride in isopropanol (0.773 ml) was added to tert-butyl 4-[4-[6-amino-5-[7-(methylcarbamoyl)-1,3-benzoxazol-2-yl]-3-pyridyl]pyrazol-1-yl]piperidine-1-carboxylate (200 mg) dissolved in isopropanol (5 ml). The resulting solution was heated at 75° C. for 2 hours. The mixture was evaporated to dryness, diisopropylethyamine (1 ml) was added and the mixture was adsorbed on silica gel with 7N methanolic ammonia and dichloromethane. The crude product was purified by flash chromatography on silica gel eluting with 2 to 8% methanolic ammonia (7 N) in dichloromethane. The solvent was evaporated to dryness to afford 2-[2-amino-5-[1-(4-piperidyl)pyrazol-4-yl]-3-pyridyl]-N-methyl-1,3-benzoxazole-7-carboxamide (92 mg) as a solid.

1. customThe mixture was evaporated to dryness, diisopropylethyamine (1 ml)
2. additionwas added
3. customThe crude product was purified by flash chromatography on silica gel eluting with 2 to 8% methanolic ammonia (7 N) in dichloromethane
4. customThe solvent was evaporated to dryness