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

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 qua...

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Main Authors: Lei Huang (Author), Yi Zhang (Author), Hua Chen (Author), Wei-Wei Wang (Author), Jian-Qi Li (Author), Yu Liu (Author)
Format: Book
Published: Georg Thieme Verlag KG, 2022-06-01T00:00:00Z.
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100 1 0 |a Lei Huang  |e author 
700 1 0 |a Yi Zhang  |e author 
700 1 0 |a Hua Chen  |e author 
700 1 0 |a Wei-Wei Wang  |e author 
700 1 0 |a Jian-Qi Li  |e author 
700 1 0 |a Yu Liu  |e author 
245 0 0 |a A Novel and Practical Synthesis of Isavuconazonium Sulfate via Anion Exchange Resin 
260 |b Georg Thieme Verlag KG,   |c 2022-06-01T00:00:00Z. 
500 |a 2628-5088 
500 |a 2628-5096 
500 |a 10.1055/s-0042-1747641 
520 |a 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. 
546 |a EN 
690 |a isavuconazonium sulfate 
690 |a synthesis 
690 |a anion exchange resin 
690 |a Pharmacy and materia medica 
690 |a RS1-441 
655 7 |a article  |2 local 
786 0 |n Pharmaceutical Fronts, Vol 04, Iss 02, Pp e71-e77 (2022) 
787 0 |n http://www.thieme-connect.de/DOI/DOI?10.1055/s-0042-1747641 
787 0 |n https://doaj.org/toc/2628-5088 
787 0 |n https://doaj.org/toc/2628-5096 
856 4 1 |u https://doaj.org/article/f8504e55c8ba42cd8e37adf7d7585bb2  |z Connect to this object online.