反应详情

4-(tert-Butyl-dimethyl-silanyloxy)-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester (0.673 g, 1.94 mmol), 2-fluoro-4-iodoaniline (0.46 g, 1.94 mmol), EEDQ (0.575 g, 2.32 mmol) and triethylamine (0.408 mL, 2.91 mmol) were heated at reflux in CHCl3 (10 mL) for 22 h. The solution was concentrated and resulting oil partitioned between EtOAc and water. The organic layer was washed with brine and dried over MgSO4. The product was purified by mplc to produce the product as a clear oil (1.0 g, 90% ). MS: APCI (AP−): 563.2 (M)−.

1. concentrationThe solution was concentrated
2. customresulting oil
3. custompartitioned between EtOAc and water
4. washThe organic layer was washed with brine
5. dry with materialdried over MgSO4
6. customThe product was purified by mplc