16α-羟基泼尼松龙合成方法综述  

Review of Synthetic Method of 16α-hydroxprednisolone

作　　者：蒋建武 江海 尹琳琳 林建东 JIANG Jianwu;JIANG Hai;YIN Linlin;LIN Jiandong(Taizhou Xianju Pharmaceutical Co.,Ltd.,Taizhou,Zhejiang,317016)

机构地区：[1]台州仙琚药业有限公司,浙江台州317016

出　　处：《化工生产与技术》2023年第5期19-24,I0003,共7页Chemical Production and Technology

摘　　要：归纳了目前已报道的16α-羟基泼尼松龙相关合成路线,并作初步分析评价。化学合成法以泼尼松龙、醋酸泼尼松和甾体化合物为原料,存在选择性较差、收率低及路线设计不够绿色环保等缺点;生物发酵法存在现有菌种活性差、发酵液有效物含量低和提取成本高等缺点。展望了未来工艺改进方向,通过光催化等技术避免高锰酸钾、铬等重金属试剂的使用,如以廉价甾体化合物为原料,采用生物发酵降解技术可将大幅度降低生产成本,实现16α-羟基泼尼松龙制备工艺的变革。The reported synthetic routes of 16α-hydroxyprednisolone are summarized and evaluated in this paper.The chemical synthesis using prednisolone,prednisolone acetate and steroidal compounds as raw materials,which has some disadvantages such as poor selectivity,low yield and the route design is not green enough.The biological fermentation method has the disadvantages of poor activity of existing strains,low content of effective substances in fermentation solution and high extraction cost.The future direction of the process improvement is prospected,and the use of heavy metal reagents such as potassium permanganate and chromium can be avoided by photocatalysis.For example,the production cost can be greatly reduced by using cheap steroid compounds as raw materials and biological fermentation degradation technology,which achieves the change of the preparation process of 16α-hydroxyprednisone.

关 键 词：16α-羟基泼尼松龙 合成方法 生物发酵 

分 类 号：TQ224.6[化学工程—有机化工]