基于酯化水解一步法的甲泼尼龙合成研究  

Synthesis of Methylprednisolone Based on the Esterification-hydrolysis One Step Method

作　　者：刘娜娜[1] 李合兴 王海波 谢涵 曾庆蕾 李孟雅 刘杰 章冰馨 赵壹民 LIU Nana;LI Hexing;WANG Haibo;XIE Han;ZENG Qinglei;LI Mengya;LIU Jie;ZHANG Bingxin;ZHAO Yimin(The Key Laboratory of Subcritical High-Efficiency Extraction of Henan Province,Department of Chemistry&Environmental Engineering,Anyang Institute of Technology,Anyang 455000,China;Henan Engineering Research Center of Steroid Hormone Pharmaceutical,Henan Lihua Pharmaceutical Co.,Ltd,Anyang 455000,China)

机构地区：[1]安阳工学院化学与环境工程学院,河南省亚临界高效萃取重点实验室,河南安阳455000 [2]河南利华制药有限公司,河南省留体激素药物工程研究中心,河南安阳455000

出　　处：《安阳工学院学报》2025年第2期47-52,共6页Journal of Anyang Institute of Technology

基　　金：河南省科技攻关项目(222102310635)。

摘　　要：甲泼尼龙是一种糖皮质激素类药物,具有影响糖代谢、抗炎、抗过敏、抗毒素等作用,在治疗红斑狼疮、肺炎、哮喘、脑水肿等疾病方面疗效显著。针对现有甲泼尼龙合成工艺成本较高、收率低、后处理麻烦等问题,开展了以甲酸钾为酯化剂,将甲泼尼龙碘代物经酯化水解进一步合成甲泼尼龙的方法研究。分别比较了乙腈体系、丙酮体系、甲醇体系下,甲酸钾投料量、反应时间和反应温度对甲泼尼龙碘代物经酯化水解转化为甲泼尼龙的影响。结果表明最佳反应条件为甲泼尼龙碘代物投料量为10g、甲酸钾投料量为17.32g、甲醇投料量为80mL、反应温度为70℃、反应时间为24h,甲泼尼龙的收率为80%。Methylprednisolone,as a kind of glucocorticoid,exhibits the properties of affecting glucose metabolism,anti-inflammation,anti-allergy,and antitoxin.It shows remarkable efficacy in treating lupus erythematosus,pneumonia,asthma,cerebral edema,and other diseases.Aiming at the existing problems of the current synthetic routes for methylprednisolone,such as troublesome post-treatment,low yield,and high cost,a simple and efficient method for the synthesis of methylprednisolone was developed.This study investigated the one-step synthesis of methylprednisolone from methylprednisolone iodide through esterification and hydrolysis using potassium formate as the esterification agent.Specifically,in the acetonitrile,acetone,and methanol systems,the effects of the amount of potassium formate,reaction time,and reaction temperature on the conversion of methylprednisolone iodide to methylprednisolone were examined.Among the tested conditions,the optimal reaction conditions were determined as follows:the amount of methylprednisolone iodide was 10 g,the amount of potassium formate was 17.32 g,the amount of methanol was 80 mL,the reaction temperature was 70℃,and the reaction time was 24 h,resulting in a yield of 80%for methylprednisolone.

关 键 词：甲泼尼龙 糖皮质激素 酯化 水解 

分 类 号：O624.31[理学—有机化学]