Extending the chiral resolution toolbox using cocrystallization
(2023)
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- Authors
- Supervisors
- tom, leyssens
- Abstract
- Research on chirality and chiral resolution experienced a long history, while studies on cocrystals are in the ascendant. In the pharmaceutical field, cocrystallization is found to be versatile, not only being used to modify API’s physicochemical properties but also in various applications, such as chiral resolution. In this work, we focused on etiracetam, mandelic acid and L-proline as model compounds to extend the toolbox on chiral resolution. Meanwhile, we investigated potential associations while doing racemate-racemate cocrystallization studies. Combining mandelic acid and etiracetam racemates which forms a cocrystal conglomerate system. We developed a preferential crystallization for this system, successfully and simultaneously resolved two racemic compounds. As there are many outcomes possible when combining racemates, we investigated the propensity of conglomerate formation between racemates. Results show that cocrystal conglomerates are rather rare, with most cases leading to double racemate solid forms. Working with mandelic acid and L-proline, we proposed a stoichiometry-controlled system strategy can be applied under the condition stoichiometric cocrystals involving the different enantiomers exist.
- Affiliations
Citations
Zhou, F. (2023). Extending the chiral resolution toolbox using cocrystallization. https://hdl.handle.net/2078.5/102439