泰拉霉素的合成工艺研究

摘要

以二氢高红霉素(去甲基阿奇霉素)为原料,经CbzCl保护、Swem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——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 (deraethylazithromycin) as initial material,undergoes five step reactions:CbzCl protection,Swem 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 solution 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 sodium hydrogen as inorganic base and TFA salt conditions reduced side reactions, improved the yield and product purity.