A Novel and Practical Synthesis of Isavuconazonium Sulfate via Anion Exchange Resin-Reference-Cited by-同舟云学术

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

Published:2022-06 Issue:02 Volume:04 Page:e71-e77
ISSN:2628-5088
Container-title:Pharmaceutical Fronts
language:en
Short-container-title:Pharmaceutical Fronts

Author:

Huang Lei¹²,Zhang Yi¹²,Chen Hua¹²,Wang Wei-Wei¹²,Li Jian-Qi¹²,Liu Yu¹²

Affiliation:

1. Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, People's Republic of China

2. Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, People's Republic of China

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.

Publisher

Georg Thieme Verlag KG

Subject

General Earth and Planetary Sciences,General Environmental Science

Link

http://www.thieme-connect.de/products/ejournals/pdf/10.1055/s-0042-1747641.pdf

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