Department of Chemistry, McGill University, 801 Sherbrooke St. W., Montreal, H3A 0B8, Canada.
Flacktek Inc., 1708 SC-11, Landrum, SC 29356, USA.
Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202206293. doi: 10.1002/anie.202206293. Epub 2022 Aug 17.
We present SpeedMixing, a rapid blending technology, as an approach for fast mechanosynthesis and discovery of model pharmaceutical cocrystals through rapid spinning in the absence of bulk solvents and milling/grinding media. Syntheses of pharmaceutical cocrystals based on the active pharmaceutical ingredients (APIs) carbamazepine, dihydrocarbamazepine, and nicotinamide demonstrate SpeedMixing as a method for rapid, scalable, as well as controllable and selective synthesis of cocrystals, cocrystal polymorphs and stoichiomorphs, including the discovery of an unexpected methanol solvate of the archetypal cocrystal of carbamazepine and saccharin, which has eluded extensive screens over 20 years.
我们提出了一种快速混合技术——SpeedMixing，它通过在没有大量溶剂和研磨/磨介的情况下快速旋转，为快速机械合成和发现模型药物共晶提供了一种方法。基于活性药物成分 (API) 卡马西平、二氢卡马西平和烟酰胺的药物共晶的合成表明，SpeedMixing 是一种快速、可扩展以及可控和选择性合成共晶、共晶多晶型物和同晶型物的方法，包括发现卡马西平和糖精的典型共晶的意外甲醇溶剂化物，这在过去 20 多年的广泛筛选中一直难以捉摸。
