反应详情

温度

100 °C

A mixture of 6-(benzenesulphonylmethyl)-3-bromo-2-methoxybenzoic acid (Intermediate 133, 0.1 g), copper (II) oxide (0.004 g), cesium carbonate (0.254 g) and pyrazole (0.018 g) in DMF (2 ml) was sealed in a microwave vial in an atmosphere of nitrogen and heated at 100° C. for 18 hours. After cooling, ethyl acetate was added, and the mixture was filtered through celite. The filtrate was evaporated to dryness and the residue was purified by HPLC, eluting with a mixture of acetonitrile and water containing 0.1% formic acid with a gradient of 40-60% to give 6-(benzenesulphonylmethyl)-2-methoxy-3-(pyrazol-1-yl)benzoic acid (0.026 g) as a white solid.

1. customwas sealed in a microwave vial in an atmosphere of nitrogen
2. temperatureAfter cooling
3. filtrationthe mixture was filtered through celite
4. customThe filtrate was evaporated to dryness
5. customthe residue was purified by HPLC
6. washeluting with a mixture of acetonitrile and water containing 0.1% formic acid with a gradient of 40-60%