泰拉霉素的合成工艺研究

Study on the synthesis of Tulathromycin

以二氢高红霉素(去甲基阿奇霉素)为原料,经CbzCl保护、Swern氧化、环氧化、烯丙基胺开环氧和钯碳催化加氢五步反应以46%的总收率合成了泰拉霉素(纯度97%),其结构经液相色谱与标准品对比确认。烯丙基胺乙醇溶液开环氧与催化加氢两步反应实现一锅法,简化了工艺操作,降低了分离难度,加之采用钠氢作无机碱和TFA成盐条件,减少了副反应的发生,提高了收率和产品纯度。

By using dihydroerythromycin （demethylazithromycin） as initial material, undergoes five step reactions： CbzC1 protection, Swern oxidation, epoxidation, opening the epoxide by allylamine, catalytic hy- drogenation by palladium carbon,Tulathromycin was synthesized in 46% total yield and 97% purity. The structure was confirmed by liquid chromatography with .standard contrast. The allylamine＇ s ethanol solu- tion to open the epoxy and catalytic hydrogenation two-step reactions were featured with one-pot reaction leads to simplify the process operation and reduce the difficulty of separation, which combined with sodi- um hydrogen as inorganic base and TFA salt conditions reduced side reactions, improved the yield and product purity