反应详情

To a solution of N-(2,6-diethylphenyl)-1-methyl-8-(piperidin-4-ylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide hydrochloride (40 mg, 0.075 mmol) in dimethylformamide (1 mL), DIPEA (0.2 mL, 1.1 mmol), N-ethyl-N′,N′-diisopropyl carbodiimide hydrochloride (EDCI) (22 mg, 0.113 mmol), 1-hydroxy-benzotriazole (18 mg, 0.113 mmol) and acetic acid (0.005 mL, 0.009 mmol) were added. The mixture was stirred at room temperature for 6 h. Water was added and the mixture extracted with ethylacetate. The organic layer was washed with brine then dried over Na2SO4 and the solvent evaporated to dryness. The crude solid was purified by flash chromatography on silica gel (eluant: dichloromethane/methanol: 97/3) to 29 mg of the title compound. (77% yield)

1. extractionthe mixture extracted with ethylacetate
2. washThe organic layer was washed with brine
3. dry with materialthen dried over Na2SO4
4. customthe solvent evaporated to dryness
5. customThe crude solid was purified by flash chromatography on silica gel (eluant: dichloromethane/methanol: 97/3) to 29 mg of the title compound