Abstract Deuterated drugs are valuable in the fields of drug discovery and medicinal chemistry. 2′,3′,5′,5″-tetradeuterated uridine derivatives were synthesised from 2,3,5,5′-selectively tetradeuterated ribose using Sajiki’s H–D exchanged Ru/C–H2–D2O–NaOH system and silyl–Hilbert–Johnson methods. The total deuterium content of the tetradeuterated uridines was over 92% using either basic or acidic reaction conditions. These derivatives would be expected as building blocks for the synthesis of deuterium-substituted nucleic acid probes for tracking the pharmacokinetics of nucleic acid drugs. Graphical Abstract

中文翻译：

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2',3',5',5"-四氘化尿苷衍生物的实用可靠合成

摘要 氘代药物在药物发现和药物化学领域具有重要价值。使用 Sajiki 的 H-D 交换 Ru/C-H2-D2O-NaOH 系统和甲硅烷基-Hilbert，从 2,3,5,5'-选择性四氘化核糖合成 2',3',5',5"-四氘化尿苷衍生物——约翰逊方法。使用碱性或酸性反应条件，四氘化尿苷的总氘含量超过 92%。这些衍生物有望作为合成氘取代核酸探针的构件，用于追踪核酸药物的药代动力学。图形概要