反应详情

485 mg (1.14 mmol) of 1-(2,4-difluorobenzyl)-N-(4-fluorophenyl)-5-nitro-1H-indole-2-carboxamide from Example XXIV are initially charged in ethyl acetate and ethanol. 287 mg (4.56 mmol) of ammonium formate and 49 mg of palladium on activated carbon (10%) are added. The mixture is heated to reflux, and at 50° C. gas evolves. To bring the reaction to completion, the same amounts of ammonium formate and palladium as above are added. After a further 3 hours at reflux, the mixture is cooled and filtered off through kieselguhr, which is washed with 500 ml of ethanol. The solvent is removed under reduced pressure and the residue is dried.

1. temperatureThe mixture is heated
2. temperatureto reflux
3. customat 50° C.
4. customthe reaction to completion
5. temperatureAfter a further 3 hours at reflux
6. temperaturethe mixture is cooled
7. filtrationfiltered off through kieselguhr, which
8. washis washed with 500 ml of ethanol
9. customThe solvent is removed under reduced pressure
10. customthe residue is dried