反应详情

To a solution of N-(2-oxo-2-phenyl-1-(pyridin-4-yl)ethyl)benzamide, 67 (1.6 g) and acetic acid (1.5 mL) in ethanol (50 mL) is added tert-butyl 2-((4R,6R)-6-(2-aminoethyl)-2-phenyl-1,3,2-dioxaborinan-4-yl)acetate (7.9 g). Upon heating under reflux for 16 h, the solution is cooled to room temperature and the solvent is evaporated. The residue is partitioned between saturated aqueous sodium hydrogen carbonate and dichloromethane, the layers separated and the organic phase washed with brine, dried (magnesium sulfate), filtered and concentrated. Purification of the residue via chromatography affords the title compound, 68 (0.35 g).

1. temperatureUpon heating
2. temperatureunder reflux for 16 h
3. customthe solvent is evaporated
4. customThe residue is partitioned between saturated aqueous sodium hydrogen carbonate and dichloromethane
5. customthe layers separated
6. washthe organic phase washed with brine
7. dry with materialdried (magnesium sulfate)
8. filtrationfiltered
9. concentrationconcentrated
10. customPurification of the residue via chromatography