Synthesis method of astringent active component DMAG and intermediate thereof

The preparation of DMAG via a three-step reaction using ellagic acid as the starting material solves the problem of low natural DMAG content in Sanguisorba officinalis and realizes an efficient and simple synthesis method suitable for industrial production.

CN122404450APending Publication Date: 2026-07-17SOUTHWEST MEDICAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-04-30
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

In existing technologies, the natural content of DMAG in Sanguisorba officinalis is low, and the separation and purification process is complex, resulting in limited product quantity and high price, which makes it difficult to meet the needs of research and application.

Method used

Using ellagic acid as the starting material, DMAG was prepared through a three-step reaction: methylation, glycosylation, and deprotection. The specific steps included methylation using potassium carbonate and iodomethane, glycosylation using β-bromoglucotetraacetic acid, and deprotection in ammonia-methanol solution. The reaction conditions were mild and the operation was simple.

Benefits of technology

The method achieves efficient preparation of DMAG with a total yield of 22.5%. The reaction steps are simple and suitable for industrial production, solving the problem of low efficiency in natural extraction.

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Abstract

本发明涉及药物化学合成领域,具体涉及一种地榆活性成分DMAG(3,3'‑二甲基鞣花酸‑4'‑O‑葡萄糖苷)及其中间体的合成方法。本发明提供了一种如式Ⅱ所示化合物的合成方法,它是以鞣花酸为起始物料,经甲基化、糖基化得到的:。本发明还提供了一种如式Ⅱ所示的化合物在合成地榆活性成分DMAG中的应用。本发明还提供了一种地榆活性成分DMAG的合成方法,它是由如式Ⅱ所示化合物脱保护得到的:,该方法具有制备步骤简洁、反应条件温和、整体收率较高的优势。
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