一种二甲弗林类似物的制备方法
By using acid and salt as additives for demethylation reaction in the preparation of dimethylflun analogues, and combining it with conventional post-processing steps, the problems of controlling the quality of dimethylflun and finding alternative drugs were solved, and a high-yield preparation method was achieved.
CN117304154BActive Publication Date: 2026-07-17SPH NO 1 BIOCHEM & PHARMA CO LTD
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- SPH NO 1 BIOCHEM & PHARMA CO LTD
- Filing Date
- 2023-09-26
- Publication Date
- 2026-07-17
AI Technical Summary
Technical Problem
Existing technologies make it difficult to effectively control the quality of dimethylformin and to discover new alternative drugs.
Method used
The demethylation reaction was carried out in the presence of additives. The specific method included treating the compound shown in Formula 1 with an acid and/or its salt as an additive at 100-200°C. The additives were salts of hydrochloric acid, hydrobromic acid, hydroiodic acid and acetic acid. The demethylation reaction time was 20-42 hours. Subsequent steps included concentration, quenching, filtration, pH adjustment, extraction, drying and purification.
Benefits of technology
A high-yield preparation of dimethylfurine analogues was achieved, the operation is simple, and it is suitable for industrial production.
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Figure CN117304154B_ABST
Abstract
本发明公开了一种二甲弗林类似物的制备方法。本发明提供了一种如式2所示的化合物的制备方法，其包括以下步骤：在添加剂的存在下，在100～200℃下，如式1所示的化合物进行脱甲基反应即可；所述的添加剂为酸和 / 或其盐；所述的酸为盐酸、氢溴酸、氢碘酸和醋酸中的一种或多种；所述的盐为吡啶与所述酸形成的盐。本发明的制备方法操作简单，收率高。
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