Angewandte Chemie International Edition · 2022 · 26 citations · 60 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryPharmaceutical ManufacturingPharmaceutical TechnologyCrystal EngineeringHigh-throughput SynthesisMechanochemistryBlendingCocrystal FormationMechanochemical SynthesisPharmaceutical CocrystallizationSelective SynthesisSolvate EffectsSpinningSpinning Technology
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.
60
Gregory R. Fulmer, Alexander J. M. Miller, Nathaniel H. Sherden et al. · Organometallics · 2010 · 3.9K citations
CHEM21 selection guide of classical- and less classical-solvents
Denis Prat, A.S. Wells, John Hayler et al. · Green Chemistry · 2015 · 2.1K citations · Full text
Pharmaceutical Cocrystals and Their Physicochemical Properties
N. Schultheiss, Ann Newman · Crystal Growth & Design · 2009 · 1.5K citations · Full text