反应详情

A mixture of 3-(4-chloro-6-morpholin-4-yl-1,3,5-triazin-2-yl)-8-oxa-3-azabicyclo[3.2.1]octane (2.0 g, 6.4 mmol), tetrakis(triphenylphosphine)palladium (0) in catalytic amount (100 mg), sodium carbonate solution 2 M (5 mL), 4-aminophenylboronic acid pinacol ester (1.5 g, 6.43 mmoles), DME (200 mL) was refluxed for 24 hours. The solvent was evaporated and the residue was dissolved in methylene chloride and filtered though Celite™. The organic layer was washed with water (200 mL) and dried over magnesium sulfate. It was filtered and the solvent was evaporated. The residue was chromatographed on silica gel column using Ethyl acetate/hexanes (1:1) as an eluent, to give 1.4 g, (59% yield) of the titled product. mp. 154; (M+H) 369.4.

1. temperaturewas refluxed for 24 hours
2. customThe solvent was evaporated
3. dissolutionthe residue was dissolved in methylene chloride
4. filtrationfiltered though Celite™
5. washThe organic layer was washed with water (200 mL)
6. dry with materialdried over magnesium sulfate
7. filtrationIt was filtered
8. customthe solvent was evaporated
9. customThe residue was chromatographed on silica gel column