A Scalable One-Pot Process for the Synthesis of Florfenicol Phosphodiester

详细信息    查看全文

• 作者：Shuang-Xi Gu ; Jia-Wen Du ; Xiu-Lian Ju ; Qing-Ping Chen
• 刊名：Organic Process Research & Development
• 出版年：2014
• 出版时间：April 18, 2014
• 年：2014
• 卷：18
• 期：4
• 页码：552-554
• 全文大小：178K
• 年卷期：v.18,no.4(April 18, 2014)
• ISSN：1520-586X

文摘

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.