反应详情

To a stirred solution of (RS) ethyl (2-hydroxy-1-tert-butoxycarbonyl-7-azaindoline-2-carboxylate) (0.6 g, 1.9 mmol) in ethanol (20 mL) was added dropwise concentrated hydrochloric acid (0.6 mL). The mixture was heated under reflux for 2 h, cooled to room temperature and partitioned between ether (30 mL) and aqueous sodium hydrogen carbonate solution (30 mL). The organic layer was washed (water, brine), dried (sodium sulfate) and concentrated in vacuo to give ethyl 7-azaindole-2-carboxylate as a white solid (0.26 g, 70%). mp 153–6° C. Found: C, 62.84; H, 5.34; N, 14.50%. C10H10N2O2 requires: C, 63.15; H, 5.30; N, 14.72%.

1. temperatureThe mixture was heated
2. temperatureunder reflux for 2 h
3. custompartitioned between ether (30 mL) and aqueous sodium hydrogen carbonate solution (30 mL)
4. washThe organic layer was washed (water, brine)
5. dry with materialdried (sodium sulfate)
6. concentrationconcentrated in vacuo