Department of Chemistry, University of Namur, rue de Bruxelles, 61, B-5000 Namur, Belgium.
Eur J Med Chem. 2010 Aug;45(8):3511-7. doi: 10.1016/j.ejmech.2010.04.028. Epub 2010 May 4.
Cocrystallization (formation of a "cocrystal") is an emerging method to optimize physico-chemical properties of pharmaceutically active compounds. One elegant technique used to obtain such cocrystals is grinding the components together, either alone or in the presence of a small amount of solvent (so called solvent-drop grinding). Dry grinding has been used here to obtain cocrystals (actually a hydrated salt) of L-Proline and MnCl(2). In that context, a new crystalline structure of a multicomponent molecular complex composed of L-Proline and MnCl(2) is here reported. The complex was characterized by powder and single-crystal X-ray diffraction and differential scanning calorimetry. This study underlines the interest of grinding as a method to synthesize original solid-state complexes. It also emphasizes the advantage of combining calorimetric and X-ray diffraction to characterize the newly formed solids. Finally, our work provides structural basis for the role that L-Proline can play within multicomponent solid-state molecular complexes, in particular as a potential cocrystal former acting by both ionic and H-bond interactions when combined to molecules of pharmaceutical interest.
共晶（“共晶”的形成）是一种新兴的方法，可以优化药物活性化合物的物理化学性质。一种用于获得此类共晶的优雅技术是将成分一起研磨，无论是单独研磨还是在少量溶剂（所谓的溶剂滴研磨）存在的情况下。在这里，干磨用于获得 L-脯氨酸和 MnCl（2）的共晶（实际上是水合盐）。在这种情况下，报道了一种由 L-脯氨酸和 MnCl（2）组成的多组分分子配合物的新晶体结构。该配合物通过粉末和单晶 X 射线衍射和差示扫描量热法进行了表征。这项研究强调了研磨作为合成原始固态配合物的方法的重要性。它还强调了将量热法和 X 射线衍射相结合以表征新形成的固体的优势。最后，我们的工作为 L-脯氨酸在多组分固态分子配合物中可能发挥的作用提供了结构基础，特别是作为与药物相关分子结合时通过离子和氢键相互作用发挥潜在共晶形成作用的可能性。
