Synthesis and Characterization of Related Substances of Torasemide

Jiong Chen, W. Ming, De-Hua Fan, Shuang‐Xi Gu
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Abstract

Torasemide, a pyridine-3-sulfonylurea derivative, is a high-efficiency loop diuretic. During the process development of torasemide, five process-related substances, which have been specified in the pharmacopeia, would be produced. In this study, all these related substances, including compounds A–E, were synthesized via simple procedures and subsequently characterized by 1H nuclear magnetic resonance (NMR), 13C NMR, and mass spectrometry. Particularly, a simple synthetic method for compound A has not been found in previous literature. It is worth noting that other related substances could be prepared from compound B in one or two steps. The availability of these related substances could allow for quality control in the process of torasemide.
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托拉塞胺相关物质的合成与表征
托拉塞胺是一种吡啶-3-磺酰脲衍生物,是一种高效的环型利尿剂。在torasemide的工艺开发过程中,将生产药典中指定的五种工艺相关物质。在本研究中,所有这些相关物质,包括化合物A-E,都是通过简单的方法合成的,随后通过1H核磁共振(NMR)、13C核磁共振(NMR)和质谱分析进行了表征。特别是化合物a的简单合成方法在以往文献中尚未发现。值得注意的是,化合物B可以通过一到两步制得其他相关物质。这些相关物质的可获得性可用于托拉塞米生产过程的质量控制。
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24
审稿时长
15 weeks
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