反应详情

To a solution of (1R,2S)-1-[4-(methylsulfonyl)phenyl]-2-amino-3-fluoro-1-propanol (5 g, 0.02 moles) in methanol (50 ml) was added methyl dichloroacetate (14.5 g; 0.10 g) and heated to reflux at 60° C. to 65° C. for 18 hours. After completion of reaction, methanol was distilled off from reaction mass, toluene (25 ml) and water (5 ml) were added. The product thus precipitated was filtered, washed with methylene chloride (20 ml) and crystallized from 2-propanol/water (5:1) to give 5 g of Florfenicol with 99% HPLC purity.

1. temperatureheated
2. temperatureto reflux at 60° C. to 65° C. for 18 hours
3. distillationwas distilled off from reaction mass, toluene (25 ml) and water (5 ml)
4. additionwere added
5. customThe product thus precipitated
6. filtrationwas filtered
7. washwashed with methylene chloride (20 ml)
8. customcrystallized from 2-propanol/water (5:1)