青霉素G亚砜的新合成工艺

Study on the new preparation process of penicillin G sulfoxide

目的开发直接氧化青霉素G发酵液生成青霉素G亚砜的新工艺。方法以青霉素G发酵液为原料、以质量分数为34%的过氧乙酸为氧化剂直接进行氧化,经陶瓷膜滤除菌丝和超滤膜提纯得到滤液,使用浓硫酸调滤液pH值至1.0进行结晶得到粗品,粗品用甲醇溶剂化提纯,脱醇后制得青霉素G亚砜。结果总摩尔收率为87.09%,纯度为99.8%,425 nm吸光小于0.01。结论直接氧化青霉素G发酵液制备青霉素G亚砜,简化了操作过程,避免了青霉素G降解损失,具有较好的工业化应用前景。

Objective To develop a new process for the preparation of penicillin G sulfoxide by directly oxidizing penicillin G in fermentation broth.Methods The penicillin G in the fermentation broth was directly oxidized by using 34%(w)peracetic acid as an oxidant.The filtrate was obtained by removing the hyphae through a ceramic membrane and purifying with ultrafiltration membrane,and then was adjusted to pH 1.0 by using concentrated sulfuric acid to obtain the crude penicillin G sulfoxide.The crude product above was purified by solvation with methanol,which was then removed to obtain penicillin G sulfoxide.Results The molar yield of penicillin G sulfoxide was 87.09%,the purity was 99.8%,and the absorbance at 425 nm was less than 0.01.Conclusion The process of preparing penicillin G sulfoxide by directly oxidizing penicillin G potassium in fermentation broth,which simplifies the operation process and avoids the degradation loss of penicillin G,hence having a good industrial application potential.