艾沙康唑合成工艺的优化  

Optimization of synthetic process of Isavuconazonium

作　　者：陆宏龙 陈海燕[1] 覃艺群 LU Honglong;CHEN Haiyan;QIN Yiqun(Guangxi Medical College,Nanning,Guangxi,530023 P.R.China)

机构地区：[1]广西卫生职业技术学院,广西南宁530023

出　　处：《华西药学杂志》2021年第4期375-377,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的优化艾沙康唑的合成工艺。方法以化合物Ⅳ为起始原料,经环氧化、亲核取代、脱保护、分子内取代关环、氰基化取代、硫代、缩合等反应步骤,制备艾沙康唑。结果以44%的总收率实现了艾沙康唑的制备,HPLC纯度为98%。结论优化后的工艺避免了剧毒品、危化品的应用,操作更简便,反应条件温和,有较好的工业化基础。OBJECTIVE To optimize the synthetic process of antifungal agent drug Isavuconazonium.METHODS CompoundⅣwas employed to synthesize Isavuconazonium via multi-step reactions including epoxidation,nucleophilic substitution,condensation,and so on.RESULTS The target product was obtained with 98%HPLC purity,and the total yield was 44%.CONCLUSION Toxic and hazardous materials are avoided,and the optimized synthetic process with mild reaction conditions,simple operation and commercially available materials is suitable for industrial production.

关 键 词：抗真菌药 艾沙康唑 工艺优化 缩合关环反应 叠缩工艺 一锅法工艺 工业化生产 

分 类 号：R914[医药卫生—药物化学]