反应详情

To a solution of diethyl 1-{4-[(tert-butoxycarbonyl)amino]butan-2-yl}-1H-indole-2,6-dicarboxylate (1.04 g, 1.8 mmol) in CH2Cl2 (4 mL) is added TFA (4 mL). The reaction mixture is stirred for 1 h and the solvent is removed under vacuum. To a solution of the residue in ethanol (10 mL) is added triethylamine (0.75 mL, 5.4 mmol) and K2CO3 (742 mg, 5.4 mmol). The reaction mixture is refluxed for 3 h. Then the solvent is evaporated, the residue is partitioned between EtOAc and water. The organic layer is then separated, dried (MgSO4) and concentrated to afford crude compound which is purified by flash column chromatography to afford the title compound (300 mg, 59% for two steps).

1. customthe solvent is removed under vacuum
2. temperatureThe reaction mixture is refluxed for 3 h
3. customThen the solvent is evaporated
4. customthe residue is partitioned between EtOAc and water
5. customThe organic layer is then separated
6. dry with materialdried (MgSO4)
7. concentrationconcentrated
8. customto afford crude compound which
9. customis purified by flash column chromatography