Unprotected aryl c-glycoside synthesis method and application
The direct synthesis of unprotected aryl C-glycosides via photoredox nickel-catalyzed cross-coupling reaction solves the problems of multi-step protecting group operation and high cost, and achieves simplified synthesis with high yield and bioactivity screening.
CN122404431APending Publication Date: 2026-07-17JIANGXI NORMAL UNIV
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Patent Information
- Application Number
- CN202610855659.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-06-15
- Publication Date
- 2026-07-17
AI Technical Summary
Technical Problem
The synthesis of unprotected aryl C-glycosides in the prior art has problems such as multiple protecting group operations, harsh reaction conditions, and high synthesis costs.
Method used
A photoredox nickel-catalyzed cross-coupling reaction was employed, utilizing unprotected glycosyl donors and acceptors under inert gas protection, and employing a photocatalyst, a transition metal catalyst, ligands, a base, and a solvent to generate aryl C-glycosides.
Benefits of technology
It simplifies the synthetic route, improves the yield, reduces the reaction cost, avoids ultra-low temperature conditions and multiple cumbersome column chromatography purification steps, and provides a more direct functionalization and bioactivity screening pathway.
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Abstract
本发明公开了一种无保护的芳基C‑糖苷的合成方法及应用，涉及化学和医药技术领域。合成方法包括：在惰性气体保护下，将无保护糖基供体、受体、光催化剂、过渡金属催化剂、配体、碱、自由基前体和溶剂进行反应，得到芳基C‑糖苷。本发明所要解决的问题是现有无保护芳基C‑糖苷合成需要多步保护基操作、反应条件苛刻且成本高，本发明直接利用全羟基糖类供体进行糖苷化反应，能简化合成路线，为后期官能团化及生物活性筛选提供更直接的途径，且本发明方法还能用于合成SGLT2抑制剂类药物，相较于传统合成路线需要超低温条件（‑78 ℃）和多步保护基引入和脱除策略，本发明能在室温下进行，避免昂贵试剂的使用和多步繁琐的纯化步骤。
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