反应详情

The following was added sequentially to anhydrous DMF (5 mL): 1-(4-fluorobenzyl)-1H-indole-2-carboxylic acid (0.119 g, 0.443 mmol), Hunig's Base (0.232 ml, 1.329 mmol), EDC (0.093 g, 0.487 mmol), HOBT (0.075 g, 0.487 mmol), and phenyl(piperidin-4-yl)methanol (0.085 g, 0.443 mmol). The solution was stirred at room temperature for 30 h, at which time a 1:1 solution of EtOAc:Et2O was added and washed with 10% aq. Na2CO3. The organic solution was dried with MgSO4 and concentrated in vacuo to give a residue that was purified by silica gel chromatography (45 g silica, 80% EtOAc/Hexanes) to give 67 mg of the title compound.

1. washwashed with 10% aq. Na2CO3
2. dry with materialThe organic solution was dried with MgSO4
3. concentrationconcentrated in vacuo
4. customto give a residue that
5. customwas purified by silica gel chromatography (45 g silica, 80% EtOAc/Hexanes)