反应详情

Water (5 mL) was added to a solution of 5-[3-(6-tert-butyl-1-oxo-1H-phthalazin-2-yl)-2-hydroxymethyl-phenyl]-1-methyl-1H-pyrrole-2-carboxylic acid methyl ester (150 mg, 0.337 mmol) in dioxane (5 mL). The mixture was stirred for 5 min and NaOH (40 mg) was added. The reaction mixture was stirred at room temperature for 16 h. The mixture was concentrated under reduced pressure. The residue was extracted with diethyl ether (5 mL×3). The combined organic layers were washed with brine, dried over Na2SO4 and concentrated under reduced pressure to give 5-[3-(6-tert-butyl-1-oxo-1H-phthalazin-2-yl)-2-hydroxymethyl-phenyl]-1-methyl-1H-pyrrole-2-carboxylic acid (113 mg, yield 78%) as a yellow solid. LC-MS calcd for C25H25N3O4 (m/e) 431.18, obsd 885 [2M+23]+.

1. stirringThe reaction mixture was stirred at room temperature for 16 h
2. concentrationThe mixture was concentrated under reduced pressure
3. extractionThe residue was extracted with diethyl ether (5 mL×3)
4. washThe combined organic layers were washed with brine
5. dry with materialdried over Na2SO4
6. concentrationconcentrated under reduced pressure