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SpeedMixing: Rapid Tribochemical Synthesis and Discovery of Pharmaceutical Cocrystals without Milling or Grinding Media.

Yong TeohGhada AyoubIgor HuskićHatem M TitiChristopher W NickelsBrad HerrmannTomislav Friščić
Published in: Angewandte Chemie (International ed. in English) (2022)
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.
Keyphrases
  • small molecule
  • high throughput
  • loop mediated isothermal amplification
  • ionic liquid
  • genome wide
  • gene expression
  • dna methylation