苯磺酸美洛加巴林关键中间体的合成研究进展  

Advances in Synthesis of Key Intermediates of Mirogabalin Besylate

作　　者：褚海龙 陈丽娜[2] Chu Hailong;Chen Lina(Lesheng Pharmaceutical Shijiazhuang Co.,Ltd.,Shijiazhuang 050000,China;Hebei Provincial Hospital of Traditional Chinese Medicine,Shijiazhuang 050000,China)

机构地区：[1]乐声药业石家庄有限公司,河北石家庄050000 [2]河北省中医院药学部,河北石家庄050000

出　　处：《炼油与化工》2025年第2期8-12,共5页Refining And Chemical Industry

基　　金：2021年度河北省中医药管理局科研计划项目(2021033)。

摘　　要：(1R,5S)-3-乙基双环[3.2.0]庚-3-烯-6-酮是苯磺酸美洛加巴林合成的重要中间体。文中主要对苯磺酸美洛加巴林重要中间体的不同合成方法展开综述,通过对多种合成路线的对比分析研究,从收率、中间体纯度以及工艺难易程度等多方面进行深入分析,评价各路线的优劣之处,最终筛选出反应条件温和、后处理简单且具有较大工业化生产价值的合成路线。此综述旨在为苯磺酸美洛加巴林及其中间体的合成研究与实际生产提供有价值的参考依据,以期推动相关领域的发展与进步,为进一步优化合成工艺和提高生产效率提供指导方向。(1R,5S)-3-Ethylbicyclo[3.2.0]hept-3-en-6-one is an important intermediate in the synthesis of milobarin benzene sulfonate.This article mainly reviews different synthetic methods of the key intermediate of milobarin benzenesulfonate.Through the comparative analysis of multiple synthetic routes,an in-depth analysis is conducted from multiple aspects such as yield,purity of intermediates,and the difficulty of the process to evaluate the advantages and disadvantages of each route.Ultimately,a synthetic route with mild reaction conditions,simple post-treatment,and significant industrial production value is selected.This review aims to provide valuable reference for the synthesis research and actual production of milobarin benzenesulfonate and its intermediates,with the expectation of promoting the development and progress in related fields and providing guidance for further optimization of the synthesis process and improvement of production efficiency.

关 键 词：美洛加巴林 中间体 合成路线 综述 

分 类 号：R924.5[医药卫生—药学]