期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 61, 期 41, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202206293
关键词
Cocrystals; Crystal Engineering; Green Chemistry; Mechanochemistry; Solid-State Chemistry
This study presents a rapid blending technology called SpeedMixing for fast mechanosynthesis and discovery of model pharmaceutical cocrystals. The method utilizes rapid spinning in the absence of bulk solvents and milling/grinding media. Syntheses of pharmaceutical cocrystals based on different active pharmaceutical ingredients demonstrate that SpeedMixing is a rapid, scalable, controllable, and selective method for the synthesis of cocrystals, cocrystal polymorphs, and stoichiomorphs.
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.
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