反应详情

温度

150 °C

A stirred mixture of 6-iodo-1H-indazole (0.45 g), N-ethyl-4-methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide (Intermediate 10, 0.54 g) tetrakis(triphenylphosphine)palladium(0) (0.05 g) and aqueous sodium hydrogen carbonate (1M, 1 ml) in isopropanol (10 ml) was heated at 150° C. for 30 min in a microwave oven. The reaction mixture was poured into water (50 ml) and extracted with ethyl acetate (3×25 ml). The extracts were washed with water (25 ml) dried (Na2SO4) and concentrated under vacuum. The residual oil was purified by column chromatography on silica (50 g) eluting with ether/ethyl acetate (7:3) to give the title compound as a pale yellow foam (0.25 g).

1. extractionextracted with ethyl acetate (3×25 ml)
2. washThe extracts were washed with water (25 ml)
3. dry with materialdried (Na2SO4)
4. concentrationconcentrated under vacuum
5. customThe residual oil was purified by column chromatography on silica (50 g)
6. washeluting with ether/ethyl acetate (7:3)