反应详情

To a solution of 0.7 g (1.85 mmol) 3-[3-(4-fluoro-phenyl)-5-methyl-isoxazole-4-carbonyl]-1H-indole-6-carboxylic acid methyl ester in 12 mL of THF and 6 mL of H2O, was added 0.39 g (9.25 mmol) LiOH.H2O in one portion. The reaction mixture was heated under reflux for 16 h. After the evaporation the mixture was extracted with Et2O (10 mL), and acidified to pH=2-3 with 2 N HCl. The resulting solid was filtered off, washed with water and dried to give 0.65 g of the title compound (intermediate 1) in 97% yield as a white solid. (m/e): 365.1 (MH+; 100%).

1. temperatureThe reaction mixture was heated
2. temperatureunder reflux for 16 h
3. customAfter the evaporation the mixture
4. extractionwas extracted with Et2O (10 mL)
5. filtrationThe resulting solid was filtered off
6. washwashed with water
7. customdried