Crystal Growth & Design · 2011 · 63 citations · 31 references
Combinatorial ChemistryPharmaceutical ScienceSupramolecular AssemblyEngineeringElusive PolymorphOrganic ChemistryChemistryPharmaceutical ChemistryMedicinal ChemistryPharmaceutical TechnologySimple RouteParacetamol Form IiSynthetic MacromoleculePharmacologyCrystallographyBiomolecular EngineeringBulk ProductionNatural SciencesSynthetic ChemistryDrug Discovery
A simple route to crystallization of the pharmaceutically important paracetamol form II is reported. The method is based around multicomponent crystallization techniques, involving various second components containing carboxylic acid groups and a range of solvents. These crystallization experiments do not produce multicomponent molecular complexes, but instead they provide the conditions in which the metastable paracetamol form II is reliably produced in 100% yields and with stability of greater than one year. To date, batches of paracetamol form II have been produced easily on the 100 mg scale with clear potential for bulk production.
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S.L. Childs, Leonard J. Chyall, J.T. Dunlap et al. · Journal of the American Chemical Society · 2004 · 625 citations
Combinatorial Chemistry, Hydrogen Bond Acceptors, Engineering +19