反应详情

A mixture of 6-bromo-3-(methylsulfonyl)-1-({[2-(trimethylsilyl)ethyl]oxy}methyl)-1H-indazole (Intermediate 76) (0.18 g) N-cyclopropyl-3-fluoro-4-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide (Intermediate 62) (0.14 g) aqueous sodium carbonate (1M, 1.32 ml) and tetrakis(triphenylphosphine)palladium(0) (0.01 g) in isopropanol (2 ml) was stirred at reflux under nitrogen for 18 h. The mixture was concentrated under vacuum and the residue was purified by column chromatography on silica eluting with cyclohexane:ethyl acetate (2:1) to give the title compound (0.15 g).

1. temperatureat reflux under nitrogen for 18 h
2. concentrationThe mixture was concentrated under vacuum
3. customthe residue was purified by column chromatography on silica eluting with cyclohexane:ethyl acetate (2:1)