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<p>In this study, optical resolution conditions using trichostatic acid as a key intermediate were investigated toward the practical supply of trichostatin A. Since previously reported asymmetric synthetic routes suffered from a decrease in optical purity upon scale-up, attention was focused on racemic trichostatic acid, and optical resolution via recrystallisation of cinchonidine salts was examined. As a result, selective access to both enantiomers was achieved depending on the solvent employed. The obtained optically active trichostatic acids were converted into trichostatin A according to known procedures, and the present method enabled the preparation of both enantiomers on a multi-gram scale.</p>

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Optical resolution of trichostatic acid using cinchonidine salts for the practical synthesis of trichostatin A enantiomers

  • 期刊论文

  • 发表日期：

    2026年3月30日

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  • Takeo Fukuda,
  • Shinya Sasayama,
  • Toshiharu Takeuchi,
  • Kyohei Kawano,
  • Kenta Suzuki

摘要

In this study, optical resolution conditions using trichostatic acid as a key intermediate were investigated toward the practical supply of trichostatin A. Since previously reported asymmetric synthetic routes suffered from a decrease in optical purity upon scale-up, attention was focused on racemic trichostatic acid, and optical resolution via recrystallisation of cinchonidine salts was examined. As a result, selective access to both enantiomers was achieved depending on the solvent employed. The obtained optically active trichostatic acids were converted into trichostatin A according to known procedures, and the present method enabled the preparation of both enantiomers on a multi-gram scale.