Abstract
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.
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Acknowledgements
The authors thank the QC group at TCI Fukaya Plant for measuring optical rotations, IR spectra, and chiral HPLC analyses of (+)-1 and (-)-1.
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Fukuda, T., Sasayama, S., Takeuchi, T. et al. Optical resolution of trichostatic acid using cinchonidine salts for the practical synthesis of trichostatin A enantiomers. J Antibiot (2026). https://doi.org/10.1038/s41429-026-00917-z
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DOI: https://doi.org/10.1038/s41429-026-00917-z
