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Thiophosphorylation Process for 2′F-Thio-Adenosine Monophosphate

有机合成与工艺文献分享 2025-08-26 08:47

文章摘要

背景：本研究针对2′F-硫代腺苷单磷酸的硫代磷酸化工艺进行优化。研究目的：解决未保护核苷反应产率低、聚合物副产物形成、溶剂分解及产物分离稳定性差等问题。结论：通过改用新戊酰保护基提高溶解度，采用四甘醇二甲醚和三乙基磷酸酯作为绿色溶剂，结合过程分析技术开发出稳健的结晶方案，最终在2.5 kg规模实现77%总收率，成功抑制产物分解。

Thiophosphorylation Process for 2′F-Thio-Adenosine Monophosphate

查看文献： Development of a Thiophosphorylation Process for the Synthesis of 2′F-Thio-Adenosine Monophosphate
查看期刊： Organic Process Research & Development

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