反应详情

温度

80 °C

A mixture of 6-(benzenesulphonylmethyl)-3-bromo-2-methoxybenzoic acid (Example 7, 0.1 g), 2-furylboronic acid (0.031 g), tri-tert-butylphosphinium tetrafluoroborate (0.0074 g), cesium carbonate (0.253 g) and tris-(dibenzylideneacetone)dipalladium (0.012 g) in dioxane (3 ml) and water (0.4 ml) was sealed in a vial under nitrogen and heated at 80° C. for 2 hours. After cooling, the mixture was diluted with t-butyl methyl ether, dried (MgSO4) and filtered. The filtrate was evaporated to dryness and the residue was purified twice by preparative HPLC (C18), eluting with a mixture of methanol and water containing 0.1% formic acid with a gradient of 25-98% to give 6-(benzenesulphonylmethyl)-3-(furan-2-yl)-2-methoxybenzoic acid (0.032 g) as a white solid.

1. customwas sealed in a vial under nitrogen
2. temperatureAfter cooling
3. dry with materialdried (MgSO4)
4. filtrationfiltered
5. customThe filtrate was evaporated to dryness
6. customthe residue was purified twice by preparative HPLC (C18)
7. washeluting with a mixture of methanol and water containing 0.1% formic acid with a gradient of 25-98%