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一种实用且环保的α-氘代羧酸合成方法。

A practical and environmentally friendly protocol for synthesis of α-deuterated carboxylic acids.

机构信息

Red Glead Discovery, Lund, Sweden.

Department of Chemistry, Lund University, Lund, Sweden.

出版信息

J Labelled Comp Radiopharm. 2023 Apr-May;66(4-6):138-144. doi: 10.1002/jlcr.4021. Epub 2023 Mar 2.

DOI:10.1002/jlcr.4021
PMID:36823686
Abstract

α-deuterated carboxylic acids have been synthesized from the corresponding malonic acids via hydrogen/deuterium exchange and decarboxylation in presence of D O. The method is general, mild and efficient and does not require organic solvents or other additives. Yields range between 83% and 94% and purification was not necessary. Starting materials were easy accessible and the α-deuterated carboxylic acids may easily be transformed to other labeled compounds such as alcohols, aldehydes, esters, and amides. Characterization with NMR confirmed purity and isotopic purity.

摘要

α-氘代羧酸已通过相应的丙二酸在 D2O 存在下的氢/氘交换和脱羧反应合成。该方法通用、温和且高效,不需要有机溶剂或其他添加剂。产率在 83%至 94%之间,无需进一步纯化。起始原料易得,α-氘代羧酸可轻松转化为其他标记化合物,如醇、醛、酯和酰胺。NMR 表征证实了产物的纯度和同位素纯度。

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