艾沙康唑合成工艺的优化

Optimization of synthetic process of Isavuconazonium

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.