青霉素G亚砜的新合成工艺  

Study on the new preparation process of penicillin G sulfoxide

作　　者：王立强 闫峰 关奇[1] 包凯[1] 张为革[1] WANG Liqiang;YAN Feng;GUAN Qi;BAO Kai;ZHANG Weige(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China;NCPC Hebei Huamin Pharmaceutical Co.,Ltd.,Shijiazhuang 052165,China)

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]华北制药河北华民药业有限责任公司,河北石家庄052165

出　　处：《沈阳药科大学学报》2020年第3期231-235,274,共6页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(81673293);863计划“面向工业过程的特种分离膜应用技术”(2012AA03A609).

摘　　要：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.

关 键 词：青霉素G亚砜 青霉素G发酵液 氧化 过氧乙酸 

分 类 号：TQ465.1[化学工程—制药化工]