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MG_Co-crystallization_induced_spontaneous_deracemization_A_General_innovative_thermodynamic_approach_to_deracemization..pdf (4.78 MB)

Co-Crystallization Induced Spontaneous Deracemization: A General Innovative Thermodynamic Approach to Deracemization.

preprint
submitted on 17.02.2020 and posted on 19.02.2020 by michael guillot, josephine demeester, sarah huynen, laurent collard, koen robeyns, olivier riant, Tom Leyssens
Processes leading to enantiopure compounds are of utmost importance, in particular for the pharmaceutical industry. Starting from a racemic mixture, Crystallization Induced Diastereomeric Transformation allows for a theoretical 100% transformation of the desired enantiomer. However, this method has the inherent limiting requirement for the organic compound to form a salt. In this contribution, this limitation is lifted by introducing cocrystallization in the context of thermodynamic deracemization, with the process applied to a model chiral fungicide. We here report a new general single thermodynamic deracemization process based on co-crystallization for the deracemization of (R,S)-4,4-dimethyl1-(4-fluorophenyl)-2-(1H-1,2,4-triazol-1-yl)-Pentan-3-one. This work presents the feasibility of this novel approach and paves the way to further development of such processes.

History

Email Address of Submitting Author

tom.leyssens@uclouvain.be

Institution

Université Catholique de Louvain

Country

Belgium

ORCID For Submitting Author

0000-0001-7916-1373

Declaration of Conflict of Interest

no conflit of interest

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