AI Article Synopsis
- Enantiomerically pure compounds are crucial for the pharmaceutical industry, and crystallization-induced diastereomeric transformation can theoretically achieve 100% conversion from racemic mixtures.
- A new method called cocrystallization is introduced to overcome the limitation of needing to form salts for effective deracemization.
- The study successfully demonstrates this innovative approach using a model chiral fungicide, showing its potential for future development in creating pure enantiomers.
Article Abstract
Processes leading to enantiomerically pure compounds are of utmost importance, in particular for the pharmaceutical industry. Starting from a racemic mixture, crystallization-induced diastereomeric transformation allows in theory for 100 % transformation of the desired enantiomer. However, this method has the inherent limiting requirement for the organic compound to form a salt. Herein, this limitation is lifted by introducing cocrystallization in the context of thermodynamic deracemization, with the process applied to a model chiral fungicide. We report a new general single thermodynamic deracemization process based on cocrystallization for the deracemization of (R,S)-4,4-dimethyl-1-(4-fluorophenyl)-2-(1H-1,2,4-triazol-1-yl)pentan-3-one. This study demonstrates the feasibility of this novel approach and paves the way to further development of such processes.
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| http://dx.doi.org/10.1002/anie.202002464 | DOI Listing |
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