反应详情

To a solution of 2-[2-Phthalimido-1-(2,3,5,6-tetrahydropyran-2-yl)oxyethyl]-7-azaindole (10.2 g, 26 mmol) in EtOH (630 ml) NH2NH2.H2O (1.53 ml, 31 mmol) was added. The mixture was refluxed for 3 h. The solvent was evaporated, the residue dissolved in CH2Cl2 and washed with saturated aq. NaHCO3. The aqueous layer was extracted three times with CH2Cl2. The organic solutions were evaporated together to obtain a diastereomeric mixture (1:1) of 9a (6.72 g, 100%) as a light orange solid.

1. temperatureThe mixture was refluxed for 3 h
2. customThe solvent was evaporated
3. dissolutionthe residue dissolved in CH2Cl2
4. washwashed with saturated aq. NaHCO3
5. extractionThe aqueous layer was extracted three times with CH2Cl2
6. customThe organic solutions were evaporated together