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An Electrophilic Approach to Fluorinated Nucleosides (2)

有机合成与工艺文献分享 2025-08-19 11:13
文章摘要
本文研究了氟化核苷合成中的关键步骤——氟酮i-Bu-2的立体选择性还原。研究发现，使用三乙酰氧基硼氢化钠(STAB)在乙腈中可实现81:19的选择性，而添加乙酸可进一步提高至92:8。研究通过控制温度、稀释度、STAB预处理和加料顺序等参数优化了非对映选择性。此外，通过拉曼光谱监测结晶过程，确定了最佳结晶条件，最终以仅6%的母液损失获得了目标产物。
An Electrophilic Approach to Fluorinated Nucleosides (2)
查看文献： Development of a Kilogram-Scale Synthesis of a Key Ulevostinag Subunit Part II: An Electrophilic Approach to Fluorinated Nucleosides
查看期刊：Organic Process Research & Development
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