反应详情

It was prepared according to the literature method (ZHAO Xiao-yu, et al., Improved synthesis of Linezolid, WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES, 2007, 22(2), 179-181). 36.2 g (0.16 mol) 3-fluoro-4-morpholinylnitrobenzene, 3.2 g 10% Pd/C, 30.4 g (0.49 mol) ammonium formate and 500 ml acetone were added into a 1000 ml four-necked bottle equipped with reflux condenser and dropping funnel, and stirred for 4 hours at 45˜50° C. After the completion of the reaction traced by TLC (developing solvent: ethyl acetate:petroleum ether=1:1), it was cooled to room temperature. After filtering by suction, solvents were evaporated from the filtrate under reduced pressure to obtain crude solid, which was recrystallized from toluene to obtain 28.1 g solid (89.5% yield). Structural confirmation:

1. customIt was prepared
2. customequipped
3. temperaturewith reflux condenser
4. filtrationAfter filtering by suction, solvents
5. customwere evaporated from the filtrate under reduced pressure
6. customto obtain crude solid, which
7. customwas recrystallized from toluene