菜籽甾醇关键中间体合成工艺研究  

Research on Synthesis Process of Key Intermediates of Brassicasterol

作　　者：王忆莹 孙彬 金灿[1,2] WANG Yiying;SUN Bin;JIN Can(College of Pharmaceutical Science,Zhejiang University of Technology,Hangzhou,Zhejiang 310014,China;Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals,Zhejiang University of Technology,Hangzhou,Zhejiang 310014,China)

机构地区：[1]浙江工业大学药学院,浙江杭州310014 [2]浙江工业大学长三角绿色制药协同创新中心,浙江杭州310014

出　　处：《浙江化工》2025年第4期7-14,共8页Zhejiang Chemical Industry

基　　金：国家自然科学基金项目(22478356,22108250)。

摘　　要：菜籽甾醇是一种天然的植物性甾体化合物,具有多种药理活性,是一种重要的医药中间体。针对原菜籽甾醇合成工艺收率低、成本高等问题,本研究以廉价甾体化合物双降醇为原料,通过磺酰化、烯醇酯化、还原、乙酰化、溴代、季鏻盐等6步反应,以总收率60.2%合成菜籽甾醇关键中间体17,避免高成本、高污染试剂的使用,为菜籽甾醇合成工艺研究提供了新思路。产物结构经^(1)H NMR、^(13)C NMR及HRMS确证。Brassicasterol is a natural plant steroidal compound with multiple pharmacological activities and serves as an important pharmaceutical intermediate.In response to the problems of low yield and high process cost in the traditional synthesis of brassicasterol,this study developed a novel synthetic route using the inexpensive steroidal compound bisnoralcohol as the starting material.Through six sequential reactions,including sulfonylation,enol esterification,reduction,acetylation,bromination,and quaternary phosphonium salt formation,the key intermediate 17 of brassicasterol was successfully synthesized with an overall yield of 60.2%.This approach avoided the use of costly and environmentally harmful reagents,offering a promising alternative for optimizing the synthesis process of brassicasterol.The structure of the final product was confirmed by ^(1)H NMR,^(13)C NMR and HRMS.

关 键 词：菜籽甾醇 关键中间体 植物甾醇 合成工艺 

分 类 号：TQ464.8[化学工程—制药化工]