反应详情

温度

175 °C

A mixture of methyl 2-benzenesulphonylmethyl-5-bromobenzoate (Intermediate 63, 0.2 g), furan-3-yl boronic acid (0.091 g), tetrakis-(triphenylphosphine) palladium (0.063 g), potassium fluoride monohydrate (0.0.23 g) and sodium bromide (0.1 g) in α,α,α-trifluorotoluene (2.5 ml) was sealed in a microwave vial and the mixture was degassed then heated in the microwave at 175° C. for 30 minutes. After cooling, the mixture was diluted with DCM and filtered. The filtrate was evaporated to dryness and the residue was purified by chromatography on silica, eluting with a mixture of ethyl acetate and cyclohexane with a gradient of 0-40% to give methyl 2-(benzenesulphonylmethyl)-5-(furan-3-yl)benzoate (0.149 g) as a white solid.

1. customwas sealed in a microwave vial
2. customthe mixture was degassed
3. temperatureAfter cooling
4. additionthe mixture was diluted with DCM
5. filtrationfiltered
6. customThe filtrate was evaporated to dryness
7. customthe residue was purified by chromatography on silica
8. washeluting with a mixture of ethyl acetate and cyclohexane with a gradient of 0-40%