A Novel and Practical Synthesis of Isavuconazonium Sulfate via Anion Exchange Resin

Lei Huang, Yi Zhang, Hua Chen, Weiwei Wang, Jian-qi Li, Yu Liu
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Abstract

In this study, an efficient and practical process for the synthesis of isavuconazonium sulfate (compound 1), an antifungal agent, was described. Highlights in the synthesis route are the usage of the ion exchange resin instead of H2SO4 to introduce the HSO4 − anion in the formulation of quaternary ammonium salt (1), and the reaction condition was further optimized to facilitate the scale-up. The overall yield of the process was 57.0% and the high-performance liquid chromatography purity of product was 97.25%, which was higher than that of the reference-listed drug.
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阴离子交换树脂法合成硫酸异磺康唑的新方法
本文介绍了一种高效实用的合成抗真菌剂硫酸异武唑铵(化合物1)的工艺。该合成路线的亮点是采用离子交换树脂代替H2SO4,在季铵盐配方中引入HSO4−阴离子(1),并进一步优化了反应条件,便于规模化生产。该工艺的总得率为57.0%,产品的高效液相色谱纯度为97.25%,高于参比药。
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审稿时长
15 weeks
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