SAM类似物及其应用

By constructing a cyclic enzyme cascade reaction of a SAM-dependent methyltransferase mutant and a fluoroalkyl SAM analog, the efficiency and stability issues of the fluoroethylation reaction were solved, achieving high-yield fluoroalkylation modification and providing an environmentally friendly synthetic method.

CN119876074BActive Publication Date: 2026-07-17TIANJIN UNIV

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
TIANJIN UNIV
Filing Date
2024-03-07
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing technologies are difficult to efficiently carry out fluoroalkylation reactions, especially fluoroethylation reactions, and traditional chemical synthesis methods suffer from environmental unfriendliness, poor selectivity, and low yield.

Method used

Using a SAM-dependent methyltransferase mutant and fluoroalkyl SAM analogs, an HMT-MTase cyclic enzyme cascade system was constructed. Fluoroalkylation was carried out via enzymatic synthesis, and SAM analogs FEt-SeAM and FEt-SAM were used as fluoroalkyl group donors to perform fluoroethylation modification of O-, N-, S- and C- nucleophiles.

Benefits of technology

This method improves the product yield of the fluoroethylation reaction, avoids the elimination problem of fluoroethyl groups, enhances the stability and efficiency of the reaction, and provides an environmentally friendly synthetic route.

✦ Generated by Eureka AI based on patent content.

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Abstract

本发明涉及生物催化技术领域,具体公开了SAM类似物及其应用。该SAM类似物具有式Ⅰ结构,可以利用MTases对活性分子进行氟乙基转移反应。其中,FEt‑SeAM可有效避免FEt‑SAM的氟乙基消除问题,更适用于受体底物的氟乙基化。本发明提供的甲基转移酶突变体相比野生型有效地提高了对氟乙基转移的催化活性。本发明还构建了基于SeAH / SAH的HMT‑MTase环酶级联反应体系,成功进行了O‑、N‑、S‑、C‑等亲核试剂的氟乙基化,相比现有化学合成技术具有操作简便,反应条件温和、环保,同时氟乙基供体FEt‑SeAM / FEt‑SAM可循环再生,显著提高了原子经济性和反应效率。
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