期刊
CRYSTALS
卷 8, 期 2, 页码 -出版社
MDPI
DOI: 10.3390/cryst8020085
关键词
febuxostat; minoxidil; salt solvates; crystal structure
资金
- Guangdong Science and Technology Department [2015B090901029, 2014A020210002]
- Guangzhou Science Technology and Innovation Commission [201704020036]
Three febuxostat-minoxidil salt solvates with acetone (ACE), tetrahydrofuran (THF) and isopropanol (IPA) are synthesized by solvent-assisted grinding and characterized by infrared (IR), nuclear magnetic resonance (H-1-NMR), single crystal and powder X-ray diffraction (PXRD), thermogravimetry (TG) and differential scanning calorimetry (DSC). These febuxostat-minoxidil salt solvates feature isostructural with the same stoichiometries (1:1:1 molecule ratio). The proton transfers from the carboxylic group of febuxostat (FEB) to imino N atom of minoxidil (MIN), which forms the motif with combined R-2(2)(9) R-4(2)(8) R-2(2)(9) graph set in the three solvates. The solvents occupy the different positions related to the motif, which results in the apparent differences in PXRD patterns before/after desolvation although they are isostructures. The FEB-MIN.THF was more thermostable than FEB-MIN.ACE and FEB-MIN.IPA relative to solvent removal from DSC patterns, which is different from the results from the solvent-exchange experiments in chemical kinetics. All three salt solvates exhibit increased equilibrium solubility compared to FEB in aqueous medium.
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