反应详情

温度

100 °C

(S)-2-(1-((6-Amino-5-iodopyrimidin-4-yl)amino)ethyl)-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4(3H)-one (200 mg, 0.3 mmol) was treated with (3,4-difluoro-5-methoxyphenyl)boronic acid (93 mg, 0.49 mmol), 1,1-bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex (29 mg, 0.03 mmol) and aqueous solution of sodium carbonate (2M, 492 μl, 0.98 mmol) in dioxane. The reaction mixture was submitted at vacuum-argon cycles and heated at 100° C. overnight. The solvent was cooled at room temperature and diluted with ethyl acetate. The organic phase was dried over sodium sulphate, filtered and evaporated under reduced pressure. The residue was purified by reverse phase using SP1® Purification System to obtain 87 mg (53% yield) of the title compound.

1. temperatureThe solvent was cooled at room temperature
2. dry with materialThe organic phase was dried over sodium sulphate
3. filtrationfiltered
4. customevaporated under reduced pressure
5. customThe residue was purified by reverse phase
6. custom® Purification System