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高度区域选择性的肌苷核苷酸甲基化:7-甲基肌苷核苷酸的有效合成。

Highly regioselective methylation of inosine nucleotide: an efficient synthesis of 7-methylinosine nucleotide.

机构信息

Life Sciences Solutions Group, Thermo Fisher Scientific, Austin, Texas, USA.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2020;39(7):1011-1019. doi: 10.1080/15257770.2020.1738457. Epub 2020 Mar 19.

Abstract

A facile, straightforward, reliable, and an efficient chemical synthesis of inosine nucleotides such as 7-methylinosine 5'--monophosphate, 7-methylinosine 5'--diphosphate, and 7-methylinosine 5'--triphosphate, starting from the corresponding inosine nucleotide is delineated. The present methylation reaction of inosine nucleotide utilizes dimethyl sulfate as a methylating agent and water as a solvent at room temperature. It is noteworthy that the present methylation reaction proceeds smoothly under aqueous conditions that is highly regioselective to afford exclusive 7-methylinosine nucleotide in good yields with high purity (>99.5%).

摘要

本文描述了一种从相应的肌苷核苷酸出发,简便、直接、可靠且高效地合成肌苷核苷酸,如 7-甲基肌苷 5'-单磷酸、7-甲基肌苷 5'-二磷酸和 7-甲基肌苷 5'-三磷酸的化学合成方法。本研究中的肌苷核苷酸甲基化反应以硫酸二甲酯为甲基化试剂,水为溶剂,在室温下进行。值得注意的是,该甲基化反应在水相条件下能顺利进行,且具有高度的区域选择性,以高纯度 (>99.5%)获得了高收率的 7-甲基肌苷核苷酸。

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