反应详情

To a mixture of 3.16 g (E)-3-[1-(4-Bromo-benzenesulfonyl)-1H-pyrrol-3-yl]-acrylic acid and 170 ml DMF are added 1.06 g HOBtxH2O and 7.02 g Et3N. This mixture is stirred for 70 min at ambient temperature. 3.99 g EDCxHCl are added and the reaction mixture is stirred for additional 45 min. 0.812 g O-(tetrahydro-2H-pyran-2-yl)-hydroxylamin are added and the reaction mixture is stirred overnight. The solvent is evaporated and the residue is partitioned between ethyl acetate and water. The organic phase is dried, evaporated and the crude product is purified by silica gel flash chromatography.

1. addition3.99 g EDCxHCl are added
2. stirringthe reaction mixture is stirred for additional 45 min
3. stirringthe reaction mixture is stirred overnight
4. customThe solvent is evaporated
5. customthe residue is partitioned between ethyl acetate and water
6. customThe organic phase is dried
7. customevaporated
8. customthe crude product is purified by silica gel flash chromatography