甲泼尼龙合成工艺研究进展  

Progress in Synthesis of Methylprednisolone

作　　者：尹琳琳 隋志红 金旦妮 YIN Linlin;SUI Zhihong;JIN Danni(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》2022年第5期20-24,I0003,共6页Chemical Production and Technology

摘　　要：介绍了甲泼尼龙的药理特性及临床应用,叙述了目前已报道的多种甲泼尼龙的合成方法,总结了现有方法所存在的不足之处,指出了开发温和绿色甲泼尼龙合成工艺的重要性。对现有制备方法的分析表明,生物-化学耦合法技术的进步提升了甲泼尼龙制备工艺水平,若生物法能够在6α-甲基的引入中获得突破,将极大缩短合成路线,简化工艺操作;发温和高效、高选择性的21位卤代反应的工艺。通过新型卤代试剂或卤代体系方法学研究,实现廉价“氯取代”向“碘取代”的替代,可提高工艺的绿色及安全性、降低工艺成本。The pharmacological properties and clinical application of methylprednisolone were introduced. The synthesis methods of methylprednisolone reported at present were described. The shortcomings of the existing methods were summarized. The importance of developing mild and green synthesis process of methylprednisolone was pointed out. The analysis of the existing preparation methods shows that the progress of bio-chemical coupling technology has improved the level of methylprednisolone preparation process. If the biological method can make a breakthrough in the introduction of 6α-methyl, it will greatly shorten the synthesis route and simplify the process operation. A mild, efficient and highly selective 21-position halogenation reaction process.Through the study of new halogenated reagents or halogenated system methodology to achieve cheap ’chlorine substitution’ to’iodine substitution’ alternative, can improve the process of green and safety, reduce process costs.

关 键 词：4甲泼尼龙 甾体类药物 皮质激素 合成工艺 

分 类 号：TQ467.5[化学工程—制药化工]