tert-butyl 3-(3-amino-4-fluorophenyl)propanoate

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 535 mg (2.00 mmol) of tert-butyl(2E)-3-(4-fluoro-3-nitrophenyl)prop-2-enoate were dissolved in 1 ml of ethanol and 1 ml of THF, and 21.3 mg of palladium (10% on carbon) were added. At RT, the mixture was hydrogenated under a hydrogen atmosphere at atmospheric pressure overnight. The reaction mixture was filtered off with suction through kieselguhr, the residue was washed with THF and the filtrate was concentrated. This gave 479 mg (100% of theory) of the title compound. At RT was hydrogenated under a hydrogen atmosphere at atmospheric pressure overnight The reaction mixture was filtered off with suction through kieselguhr the residue was washed with THF the filtrate was concentrated

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 535 mg (2.00 mmol) of tert-butyl(2E)-3-(4-fluoro-3-nitrophenyl)prop-2-enoate were dissolved in 1 ml of ethanol and 1 ml of THF, and 21.3 mg of palladium (10% on carbon) were added. At RT, the mixture was hydrogenated under a hydrogen atmosphere at atmospheric pressure overnight. The reaction mixture was filtered off with suction through kieselguhr, the residue was washed with THF and the filtrate was concentrated. This gave 479 mg (100% of theory) of the title compound. At RT was hydrogenated under a hydrogen atmosphere at atmospheric pressure overnight The reaction mixture was filtered off with suction through kieselguhr the residue was washed with THF the filtrate was concentrated

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: A solution of 81.0 g (303 mmol) of tert-butyl (2E)-3-(4-fluoro-3-nitrophenyl)acrylate in a mixture of 810 ml of THF and 810 ml of ethanol was inertized with argon, and 8.1 g of 10% palladium on carbon were added. The suspension was stirred at RT under a hydrogen atmosphere at standard pressure for 9 h. The reaction mixture was then filtered off with suction through kieselguhr, and the filtrate was concentrated. The crude product was purified by chromatography on silica gel (mobile phase petroleum ether/ethyl acetate 4:1). This gave 66.0 g (91% of theory) of the title compound. were added The reaction mixture was then filtered off with suction through kieselguhr the filtrate was concentrated The crude product was purified by chromatography on silica gel (mobile phase petroleum ether/ethyl acetate 4:1)

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 535 mg (2.00 mmol) of tert-butyl (2E)-3-(4-fluoro-3-nitrophenyl)prop-2-enoate were dissolved in 1 ml of ethanol and 1 ml of THF, and 21.3 mg of palladium on carbon (10%) were added. At RT, the mixture was hydrogenated under an atmosphere of hydrogen at atmospheric pressure overnight. The reaction mixture was then filtered off with suction through kieselguhr, the residue was washed with THF and the filtrate was concentrated. This gave 479 mg (100% of theory) of the title compound. At RT was hydrogenated under an atmosphere of hydrogen at atmospheric pressure overnight The reaction mixture was then filtered off with suction through kieselguhr the residue was washed with THF the filtrate was concentrated

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 535 mg (2.00 mmol) of tert-butyl(2E)-3-(4-fluoro-3-nitrophenyl)prop-2-enoate were dissolved in 1 ml of ethanol and 1 ml of THF, and 21.3 mg of palladium (10% on carbon) were added. At RT, the mixture was hydrogenated under a hydrogen atmosphere at atmospheric pressure overnight. The reaction mixture was filtered off with suction through kieselguhr, the residue was washed with THF and the filtrate was concentrated. This gave 479 mg (100% of theory) of the title compound. At RT was hydrogenated under a hydrogen atmosphere at atmospheric pressure overnight The reaction mixture was filtered off with suction through kieselguhr the residue was washed with THF the filtrate was concentrated

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: A solution of 81.0 g (303 mmol) of tert-butyl (2E)-3-(4-fluoro-3-nitrophenyl)acrylate in a mixture of 810 ml of THF and 810 ml of ethanol was inertized with argon, and 8.1 g of 10% palladium on carbon were added. The suspension was stirred at RT under a hydrogen atmosphere at standard pressure for 9 h. The reaction mixture was then filtered off with suction through kieselguhr, and the filtrate was concentrated. The crude product was purified by chromatography on silica gel (mobile phase petroleum ether/ethyl acetate 4:1). This gave 66.0 g (91% of theory) of the title compound. were added The reaction mixture was then filtered off with suction through kieselguhr the filtrate was concentrated The crude product was purified by chromatography on silica gel (mobile phase petroleum ether/ethyl acetate 4:1)