Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 18, Issue 4, Pages 552-554Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op500038s
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Funding
- Hubei Novel Reactor and Green Chemical Technology Key Laboratory Open Fund [RGCT201201]
- Wuhan Institute of Technology Scientific Research Fund [10128301]
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A practical and scalable one-pot process for the preparation of florfenicol phosphodiester (3), a new water-soluble prodrug of florfenicol (1), has been developed by adopting the phosphorylating system of POCl3/pyridine/CH3CN. The yield of 3 was 80.72%, and its HPLC purity reached as high as 99.20%, while the content of the maximum impurity was reduced to 0.28% under the optimum conditions. The present process has proven to be reliable on 500-g and 4-kg scale in the pilot plant.
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