Practical and scalable one-pot synthesis of arbekacin

Abstract

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.