反应详情

温度

110 °C

Tert-butyl 2-(7-bromo-2-hydroxy-1,1-dimethyl-4-oxo-1,4-dihydronaphthalene-3-carboxamido)acetate (125 mg, 295 μmol, Example 53A-E), palladium acetate (7 mg, 29 μmol), racemic-2,2-bis(diphenylphosphino)-1,1-binaphthyl (18 mg, 29 μmol), and sodium tert-butoxide (42 mg, 442 μmol) were added to toluene (5892 μL) followed by 2-morpholinoethylamine (77 μL, 589 μmol). The reaction was then stirred at 110° C. for 3 hours. The reaction mixture was diluted with 100 mL of EtOAc, washed 2 times with 50 mL of 3 N HCl (aqueous), and separated. The organic layer was dried over sodium sulfate and concentrated to give crude product which was purified via HPLC to give the title compound.

1. washwashed 2 times with 50 mL of 3 N HCl (aqueous)
2. customseparated
3. dry with materialThe organic layer was dried over sodium sulfate
4. concentrationconcentrated
5. customto give crude product which
6. customwas purified via HPLC