Practical and scalable one-pot synthesis of arbekacin,Reaction Chemistry & Engineering

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Practical and scalable one-pot synthesis of arbekacin
Reaction Chemistry & Engineering ( IF 3.4 ) Pub Date : 2024-01-23 , DOI: 10.1039/d3re00598d
Hongsen Zhang ₁ , Chunxiao Wang ₁ , Kai Liu ₁ , Chao Li ₁ , Renzhong Qiao ₁

Affiliation

An efficient and scalable one-pot production process was developed to prepare arbekacin from dibekacin. The impurities derived from side chains at different NH₂ sites were separated, and analyzed by ESI-HRMS² and 2D NMR. The reactivities of NH₂ were evaluated through DFT theoretical calculations to optimize the process conditions. Solvent polarity was found to be an important factor affecting the ratio of product to impurities, and the possible mechanism was investigated. This work gave a practical synthetic process of arbekacin, especially for large scale production.

中文翻译：

阿贝卡星的实用且可规模化的一锅法合成

开发了一种高效且可扩展的一锅法生产工艺，以从地贝卡星制备阿贝卡星。分离源自不同NH ₂位点侧链的杂质，并通过ESI-HRMS ²和2D NMR进行分析。通过DFT理论计算评价NH ₂的反应活性，优化工艺条件。发现溶剂极性是影响产物与杂质比例的重要因素，并对其可能的机制进行了研究。本工作给出了阿贝卡星的实用合成工艺，特别适合大规模生产。

更新日期：2024-01-23

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