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首页> 外文期刊>Crystal growth & design >Synthesis and Structural Characterization of Cocrystals and Pharmaceutical Cocrystals: Mechanochemistry vs Slow Evaporation A from Solution
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Synthesis and Structural Characterization of Cocrystals and Pharmaceutical Cocrystals: Mechanochemistry vs Slow Evaporation A from Solution

机译：共晶体和药物共晶体的合成和结构表征：溶液的机械化学与缓慢蒸发A

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摘要

The reliability of solvent drop grinding (SDG), also referred to as liquid assisted grinding, wet cogrinding, or mechanochemistry, to facilitate cocrystal formation is addressed with a series of model cocrystals and pharmaceutical cocrystals. The synthesis and single crystal structures of 17 new cocrystals that are sustained by COOH center dot center dot center dot N-arom and OH center dot center dot center dot N-arom supramolecular heterosynthons are presented. These cocrystals were prepared by both slow evaporation from solution and SDG. We also investigated whether or not SDG could be used to prepare previously reported carbarnazepine (CBZ) pharmaceutical cocrystals. The following eight cocrystal formers were investigated in this context: 4,4'-bipyridine, 4-aminobenzoic acid/H2O, 2,6-pyridinedicarboxylic acid, benzoquinone, terephthalaldehyde, saccharin, nicotinamide, and aspirin. Our results reveal that all of the cocrystals that were grown from solution and characterized by single crystal X-ray crystallography can also be prepared by SDG. SDG therefore appears to be a cost-effective, green, and reliable method for discovery of new cocrystals as well as for preparation of existing cocrystals.
机译：溶剂滴磨（SDG）的可靠性，也称为液体辅助研磨，湿式共研磨或机械化学，以促进共晶形成，其可靠性通过一系列模型共晶和药物共晶解决。介绍了由COOH中心点中心点中心点N-arom和OH中心点中心点中心点N-arom超分子杂合子维持的17种新共晶体的合成和单晶结构。通过从溶液和SDG中缓慢蒸发制备这些共晶体。我们还研究了SDG是否可用于制备先前报道的卡巴西平（CBZ）药物共晶体。在此背景下研究了以下八种共晶形成剂：4,4'-联吡啶，4-氨基苯甲酸/ H2O，2,6-吡啶二羧酸，苯醌，对苯二甲醛，糖精，烟酰胺和阿司匹林。我们的结果表明，也可以通过SDG制备从溶液中生长出来并通过单晶X射线晶体学表征的所有共晶体。因此，SDG似乎是一种经济高效，绿色且可靠的方法，可用于发现新的共晶以及制备现有的共晶。

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