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Efficient Synthesis of Stable 34S Isotope Labeled Compounds

有机合成与工艺文献分享 2025-07-31 08:40

文章摘要

本文探讨了34S同位素标记化合物的高效合成方法。研究背景源于药物开发中对非卤素稳定同位素标记化合物的需求，要求质量数增加3个以上且未标记母体含量低于0.2%。传统方法在核苷类似物MK-1454的合成中存在步骤过多的问题。研究目的是开发一种后期硫化方法，通过引入34S原子来制备含硫磷硫代磷酸酯寡核苷酸的稳定同位素标记物。研究发现初始使用二硫化碳溶剂时因硫同位素交换而失败，改用乙腈溶剂并优化反应条件后，微量水可显著加速反应速率，最终成功建立了有效的合成方法。

Efficient Synthesis of Stable 34S Isotope Labeled Compounds

查看文献： 34S: A New Opportunity for the Efficient Synthesis of Stable Isotope Labeled Compounds
查看期刊： Chemistry - A European Journal

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