反应详情

温度

85 °C

To a solution of tert-butyl 4-(bromo(3-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)methylene)piperidine-1-carboxylate (Example 71, step 2) (420 mg, 0.818 mmol) in toluene (10 mL), under N2 was added methyl boronic acid (54 mg, 0.900 mmol), dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) (60 mg, 0.0818 mmol), potassium carbonate (226 mg, 1.64 mmol) and silver oxide (379 mg, 1.64 mmol). The reaction was heated to 85° C. overnight. The reaction was cooled down and filtered. The filtrate was washed with water and dried over MgSO4. Purification by silica gel column chromatography (0-5% MeOH/CH2Cl2) gave the title compound (291 mg, 79% yield).

1. temperatureThe reaction was cooled down
2. filtrationfiltered
3. washThe filtrate was washed with water
4. dry with materialdried over MgSO4
5. customPurification by silica gel column chromatography (0-5% MeOH/CH2Cl2)