New forms of apremilast with halogen derivatives of benzoic acid

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22310%2F25%3A43932779" target="_blank" >RIV/60461373:22310/25:43932779 - isvavai.cz</a>
Result on the web
<a href="https://pubs.rsc.org/en/content/articlelanding/2025/ce/d5ce00770d" target="_blank" >https://pubs.rsc.org/en/content/articlelanding/2025/ce/d5ce00770d</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/d5ce00770d" target="_blank" >10.1039/d5ce00770d</a>

Result language
angličtina
Original language name
New forms of apremilast with halogen derivatives of benzoic acid
Original language description
Apremilast is a poorly soluble active pharmaceutical ingredient. It is prone to form multicomponent crystals and crystallizes in very similar molecular arrangements. We have crystallized apremilast with derivatives of halogen benzoic acid. Such compounds are known to moderate crystallization processes to different polymorphs of paracetamol. Surprisingly, apremilast structure packing was able to accommodate the o- and m-halogen benzoic acid derivatives in the same structure type as for known structures. On the other hand, crystallization with p-halogen benzoic acid derivatives leads to a cocrystal form with a rare molecular arrangement, which is likely less stable, and hence not preferred in the structures with smaller co-formers. The new forms were characterized by Single Crystal and Powder X-Ray Diffraction, and their stability was studied and compared by Differential Scanning Calorimetry and Thermogravimetric Analysis.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10406 - Analytical chemistry

Project
<a href="/en/project/GX21-05926X" target="_blank" >GX21-05926X: Nanocrystallography of molecular crystals</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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