反应详情

A mixture of 2-chloro-4,6-di-morpholin-4-yl-[1,3,5]triazine (1.4 g, 4.9 mmoles), a catalytic amount of tetrakis(triphenylphosphine)palladium(0) (70 mg, 0.061 mmoles), sodium carbonate solution 2 M (3 mL), 4-aminophenylboronic acid pinacol ester (1.6 g, 7.3 mmoles) and DME (100 mL) was refluxed for 24 hours. The solvent was evaporated, and the residue was dissolved in methylene chloride and filtered through Celite™. The filtrate was washed with water (200 mL) and the organic layer was dried with magnesium sulfate. This was filtered and the solvent was evaporated. The residue was purified by Silica gel column chromatography and eluted with Ethyl acetate/hexanes (1:1) to give 1.40 g, (83% yield) of 4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)aniline as an amorphous solid. (M+H) 343.

1. customThe solvent was evaporated
2. dissolutionthe residue was dissolved in methylene chloride
3. filtrationfiltered through Celite™
4. washThe filtrate was washed with water (200 mL)
5. dry with materialthe organic layer was dried with magnesium sulfate
6. filtrationThis was filtered
7. customthe solvent was evaporated
8. customThe residue was purified by Silica gel column chromatography
9. washeluted with Ethyl acetate/hexanes (1:1)