tert-butyl N-(2-fluoro-5-hydroxyphenyl)carbamate

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

実験手順: In the same manner as in Reference Example 33 and using tert-butyl (2-fluoro-5-hydroxyphenyl)carbamate (22.4 g, 98.4 mmol), 5-bromo-2-nitropyridine (16.7 g, 82.0 mmol), cesium carbonate (40.1 g, 123 mmol) and N,N-dimethylformamide (140 mL) as starting materials, the title compound (14.2 g, 50%) was obtained as a yellow oil.

反応条件: temp:40.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: A mixture of 3-[(tert-butoxycarbonyl)amino]-4-fluorophenyl tert-butyl carbonate (33.1 g, 101 mmol), sodium methoxide (6.55 g, 121 mmol) and methanol (500 mL) was stirred at 40° C. for 15 hr. The reaction mixture was concentrated under reduced pressure, and ethyl acetate and water were added to the residue. The organic layer was separated, washed with water and saturated brine, dried over anhydrous magnesium sulfate and filtrated. The filtrate was concentrated under reduced pressure, and the residue was dried to give the title compound (22.8 g, quant.) as a yellow oil. The reaction mixture was concentrated under reduced pressure, and ethyl acetate and water were added to the residue The organic layer was separated washed with water and saturated brine dried over anhydrous magnesium sulfate filtrated The filtrate was concentrated under reduced pressure the residue was dried