反应详情

To a mixture of methyl [6-chloro-2-[(5,6,7,8-tetrahydroisoquinolin-3-yl)carbonyl]-1H-indol-3-yl]acetate (Example 1) in MeOH (20 ml)-THF (20 ml) was added 2N aqueous NaOH (0.6 ml, 1.2 mmol) at room temperature and the resulting mixture was heated at reflux temperature for 8 h. The mixture was cooled and concentrated. The residue was dissolved in water (20 ml) and washed with diethyl ether (20 ml×3). The aqueous layer was acidified with 2N aqueous HCl and extracted with ethyl acetate (40 ml×3). The combined organic layers were dried (MgSO4) and concentrated. The residue was recrystallized from ethyl acetate to afford 23.3 mg (60.7%) of the title compound as yellow solids.

1. temperaturethe resulting mixture was heated
2. temperatureat reflux temperature for 8 h
3. temperatureThe mixture was cooled
4. concentrationconcentrated
5. dissolutionThe residue was dissolved in water (20 ml)
6. washwashed with diethyl ether (20 ml×3)
7. extractionextracted with ethyl acetate (40 ml×3)
8. dry with materialThe combined organic layers were dried (MgSO4)
9. concentrationconcentrated
10. customThe residue was recrystallized from ethyl acetate