Synthesis of Methylprednisolone Based on the Esterification-hydrolysis One Step Method
LIU Nana
LI Hexing
WANG Haibo
XIE Han
ZENG Qinglei
LI Mengya
LIU Jie
ZHANG Bingxin
ZHAO Yimin
Abstract：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.
Keywords：methylprednisoloneglucocorticoidesterificationhydrolysis
Publication Date：2025-03-20
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：6( 47-52 )