反应详情

温度

40 °C

To a solution of 3-bromo-7-methoxyquinolin-2(1H)-one (1.31 g, 5.17 mmol) and 1-tert-butyl 2-methyl (2S,4S)-4-{[(4-bromophenyl)sulfonyl]oxy}pyrrolidine-1,2-dicarboxylate (2.0 g, 4.31 mmol) in NMP (21.5 mL), Cs2CO3 (2.11 g, 6.46 mmol) was added, and the reaction mixture was stirred for 40 hours at 40° C. An additional portion of 1-t-butyl 2-methyl (2S,4S)-4-{[(4-bromophenyl)sulfonyl]oxy}pyrrolidine-1,2-dicarboxylate (1.0 g, 2.16 mmol) was added, and the reaction mixture was stirred at 40° C. for 16 hours. The reaction mixture was cooled and poured onto a mixture of EtOAc and H2O, and the layers were separated. The organic layer was washed with H2O (2×), NaHCO3 (2×) and brine, dried over Mg2SO4, filtered and concentrated. The product was used with no further purification. LRMS (M+H-Boc)+=381.2.

1. stirringthe reaction mixture was stirred at 40° C. for 16 hours
2. temperatureThe reaction mixture was cooled
3. customthe layers were separated
4. washThe organic layer was washed with H2O (2×), NaHCO3 (2×) and brine
5. dry with materialdried over Mg2SO4
6. filtrationfiltered
7. concentrationconcentrated
8. customThe product was used with no further purification