A large-scale synthesis process of N-Boc-4-fluoro-l-proline (1) from N-Boc-4-hydroxy-l-proline methyl ester (2) using nosyl fluoride (13) as a deoxyfluorinating agent has been developed. An eco-friendly and large-scale feasible process using a single solvent was developed to afford moderate yields of products with excellent purity >99% by high-performance liquid chromatography . The key feature of the optimization involving chromatography-free purification and isolation on a kilogram-scale at a pilot plant scale is described.

中文翻译：

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Boc保护的4-氟-1-脯氨酸的大规模实用合成

已经有使用壬基氟（13）作为脱氧氟化剂由N -Boc-4-羟基-1-脯氨酸甲酯（2）大规模合成N -Boc-4-氟-1-脯氨酸（1）的方法。发达。通过高效液相色谱法，开发了一种使用单一溶剂的生态友好型大规模可行方法，可提供中等收率的产品，其纯度> 99％的卓越纯度。描述了优化的关键特征，其中涉及在中试规模的千克级无色谱纯化和分离。