Co-crystallization Induced Spontaneous Deracemization - Development and Optimization

de Meester, Joséphine
(2020)

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Supervisors
Leyssens, Tom
Faculty
Faculté des sciences
Degree label
Master [120] en sciences chimiques
Abstract
Nowadays, one of the current pharmaceutical hot topics is deracemization of racemic mixtures. Indeed, while most of the currently marketed drugs are racemates, pharmaceutical industries are pushed towards the development of enantiopure drugs since the beginning of the XXI century. One of the scopes of Professor Leyssens’s group lies in the development of novel deracemization methods, allowing the transformation of a racemic mixture into an enantiopure compound. This work focuses on the development of a thermodynamic deracemization method based on co-crystallization of the target enantiomer. The first part of the project is to develop and optimize the deracemization process for (R,S)-1-(4-fluorophenyl)-4,4-dimethyl-2-(1H-1,2,4- triazol-1-yl)pentan-3-one (BnFTP). In the second part, we will valorize the compound BnFTP by a reduction reaction and we will study its diastereoselectivity.