反应详情

温度

120 °C

A mixture of 1-bromo-4-hydroxy-6-(4-propoxy-phenoxy)-isoquinoline-3-carboxylic acid butyl ester (315 mg, 0.664 mmol), CuCN (66 mg, 0.730 mmol), and N-methylpyrrolidinone (2 mL) was stirred at 120° C. for 4 h. After cooling to room temperature the mixture was poured into EtOAc (20 mL) and saturated ammonium hydroxide solution (˜1 mL) was added. The mixture was rapidly stirred for 2 min. Then it was acidified with concentrated HCl, washed with water, and saturated NaCl solution before it was dried over anhydrous sodium sulfate, and concentrated in vacuo. The residue was purified by column chromatography to give title compound (206 mg). ESI MS (m/z): 421 (M+H+).

1. temperatureAfter cooling to room temperature the mixture
2. additionwas added
3. stirringThe mixture was rapidly stirred for 2 min
4. washwashed with water, and saturated NaCl solution before it
5. dry with materialwas dried over anhydrous sodium sulfate
6. concentrationconcentrated in vacuo
7. customThe residue was purified by column chromatography