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 triethylamine (2.05 g, 0.02 mole) and stirred at room temperature for 18 hours. After completion of reaction, methanol was distilled off from the 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 title compound having purity 99.20% by HPLC.

1. distillationwas distilled off from the reaction mass, toluene (25 ml) and water (5 ml)
2. additionwere added
3. customThe product thus precipitated
4. filtrationwas filtered
5. washwashed with methylene chloride (20 ml)
6. customcrystallized from 2-propanol/water (5:1)