反应详情

温度

80 °C

3-Bromo-N-cyclopropyl-5-fluoro-4-methylbenzamide (Intermediate 1, 40 mg, 0.15 mmol), N-cyclopropylmethyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)benzamide (45 mg, 0.15 mmol) and tetrakis(triphenylphosphine)palladium (17 mg, 0.015 mmol) were dissolved in DME (3 ml) and aqueous sodium carbonate (1M, 150 μl) was added. The mixture was refluxed at 80° C. for 16 hours. Solvent was removed in vacuo and the residue was purified by silica biotage chromatography, eluting with ethyl acetate:cyclohexane (2:) then 100% ethyl acetate to give N3-cyclopropyl-N4′-(cyclopropylmethyl)-5-fluoro-6-methyl-1,1′-biphenyl-3,4′-dicarboxamide (34 mg, 62%)

1. customSolvent was removed in vacuo
2. customthe residue was purified by silica biotage chromatography
3. washeluting with ethyl acetate