他卡西醇的合成方法研究进展  

A Review for Synthesis Methods of Tacalcitol

作　　者：凌佳信 庄小慧 张兆康 孙彬[2] 金灿[1,2] LING Jiaxin;ZHUANG Xiaohui;ZHANG Zhaokang;SUN Bin;JIN Can(College of Pharmaceutical Sciences,Zhejiang University of Technology,Hangzhou,Zhejiang 310014,China;Collaborative Innovation Center 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3期29-36,共8页Zhejiang Chemical Industry

基　　金：国家自然科学基金项目(22478356,22108250)。

摘　　要：他卡西醇是一种活性维生素D3类似物,具有抑制表皮细胞增殖和诱导细胞分化作用,在治疗以银屑病为主的皮肤角化过度异常的临床上效果较好。与同类药物相比,他卡西醇的安全性更高、更温和、可应用的部位更广。本文系统综述了国内外他卡西醇的合成路线,分析了现有方法的优缺点,并提出优化建议,为改进他卡西醇的合成工艺及推动其工业化生产提供新的思路和可能性。Tacalcitol,an active vitamin D3 analogue,can inhibit the proliferation of epidermal cells and induce cell differentiation,and plays an important role in the treatment of abnormal skin hyperkeratosis mainly in psoriasis.Compared with similar drugs,tacalcitol has a higher safety profile,is milder,and can be used in a wider range of sites.In this review,the synthesis routes of tacalcitol at home and abroad were systematically reviewed,the advantages and disadvantages of the existing methods were analyzed,and the optimization suggestions were put forward,which provided new ideas and possibilities for improving the synthesis process of tacalcitol and promoting its industrial production.

关 键 词：他卡西醇 维生素D 半合成法 全合成法 

分 类 号：TQ460.4[化学工程—制药化工]