1. Cocrystallization‐Induced Spontaneous Deracemization: A General Thermodynamic Approach to Deracemization.
- Author
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Guillot, Michael, Meester, Joséphine, Huynen, Sarah, Collard, Laurent, Robeyns, Koen, Riant, Olivier, and Leyssens, Tom
- Subjects
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DERACEMIZATION , *ENANTIOMERIC purity , *RACEMIC mixtures , *RESOLUTION (Chemistry) , *ORGANIC compounds - 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. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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