现代药物中酯键的合成研究进展
Research Progress on the Synthesis of Ester Bonds in Modern Drugs
DOI: 10.12677/hjmce.2026.143025, PDF,    科研立项经费支持
作者: 周 苗, 王承薇, 高如琴, 刘 辉*：华北水利水电大学生态环境学院，河南 郑州
关键词: 酯键；药物合成；酯化反应；氧化还原脱水；Ester Bond； Drug Synthesis； Esterification； Redox Dehydration
摘要: 酯键是有机化学中最基础、最重要的官能团之一，也是现代药物分子中关键的功能结构，在前药设计、药代动力学优化及活性提升方面发挥着不可替代的作用。文章总结了近年来国内外上市的代表性药物中酯键的合成方法，包括酸催化的酯化反应、酸酐/酰氯/缩合试剂促进的酯化反应、羧酸与卤代烃的亲核取代反应、酯交换反应及氧化还原脱水反应等多种酯键构建策略。在此基础上，对各种合成方法的优缺点进行了评述，并对药物中酯键合成的发展方向进行了展望。
Abstract: Ester bonds are among the most fundamental and important functional groups in organic chemistry. As a key structural motif in modern drug molecules, the ester bond plays an irreplaceable role in prodrug design, pharmacokinetic optimization, and activity enhancement. This review article summarizes the synthetic methods for ester bonds in representative drugs approved both domestically and internationally in recent years, including acid-catalyzed esterification, esterification promoted by anhydrides, acyl chlorides, and coupling reagents, nucleophilic substitution reactions of carboxylic acids with alkyl halides, transesterification, and redox dehydration strategies. Building upon this foundation, the advantages and limitations of each synthetic approach are discussed, and future directions for the synthesis of ester bonds in pharmaceuticals are proposed.
文章引用：周苗, 王承薇, 高如琴, 刘辉. 现代药物中酯键的合成研究进展[J]. 药物化学, 2026, 14(3): 251-261. https://doi.org/10.12677/hjmce.2026.143025

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