Switching polymorph stabilities with impurities provides a thermodynamic route to benzamide form III.
| Autor: | Kras W; Department of Chemical Engineering and Analytical Science, The University of Manchester, Manchester, UK.; Chemical Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield, UK., Carletta A; Namur Institute of Structured Matter (NISM), University of Namur, Namur, Belgium., Montis R; Department of Chemical Engineering and Analytical Science, The University of Manchester, Manchester, UK., Sullivan RA; Chemical Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield, UK., Cruz-Cabeza AJ; Department of Chemical Engineering and Analytical Science, The University of Manchester, Manchester, UK. aurora.cruzcabeza@manchester.ac.uk.; Chemical Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield, UK. aurora.cruzcabeza@manchester.ac.uk. |
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| Jazyk: | angličtina |
| Zdroj: | Communications chemistry [Commun Chem] 2021 Mar 17; Vol. 4 (1), pp. 38. Date of Electronic Publication: 2021 Mar 17. |
| DOI: | 10.1038/s42004-021-00473-7 |
| Abstrakt: | Almost 200 years ago, benzamide was reported as polymorphic with two of its forms (II and III) found to be difficult to crystallise. In a recent study, it was shown that benzamide form I can easily convert into benzamide form III using mechanochemistry in the presence of nicotinamide. Here we show, experimentally and computationally, that this transformation is the result of a thermodynamic switch between these two polymorphic forms driven by the formation of solid solutions with small amounts of nicotinamide. The presence of nicotinamide in the crystallisation environment promotes the robust and exclusive crystallisation of the elusive form III. These results represent a promising route to the synthesis and utilisation of elusive polymorphs of pharmaceutical interest. (© 2021. The Author(s).) |
| Databáze: | MEDLINE |
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