反应详情

To 2-propenyl-carbamic acid 1,1-dimethylethyl ester under nitrogen was added 9-borabicyclo[3.3.1]nonane (0.5M in tetrahydrofuran, 7.1 mL) and the mixture refluxed for 2 hours. The reaction was allowed to cool to room temperature and potassium phosphate (1.02 g) in water (1.8 mL) added. The resultant mixture was stirred for 15 minutes. N-(2,6-Dichloro-5-quinolinyl)-cyclohexaneacetamide (prepared as described in Example 1a) (0.5 g) was added followed by tetrakis(triphenylphosphine)palladium(0) (17 mg) in dimethylformamide (2.8 mL). The reaction was heated at 70° C. under nitrogen for 4 hours. To the cooled solution was added brine (30 mL) and the mixture extracted with ethyl acetate (3×30 mL). The combined organics were dried, filtered and concentrated to give the sub-title compound (0.9 g).

1. temperaturethe mixture refluxed for 2 hours
2. temperatureThe reaction was heated at 70° C. under nitrogen for 4 hours
3. extractionthe mixture extracted with ethyl acetate (3×30 mL)
4. customThe combined organics were dried
5. filtrationfiltered
6. concentrationconcentrated