Abstract
In the pharmaceutical industry, co-crystals are becoming increasingly valuable as crystalline solids that can offer altered/improved physical properties of an active pharmaceutical ingredient (API) without changing its chemical identity or biological activity. In order to identify new solid forms of diclofenac—an analgesic with extremely poor aqueous solubility for which few co-crystal structures have been determined—a range of pyrazoles, pyridines, and pyrimidines were screened for co-crystal formation using solvent assisted grinding and infrared spectroscopy with an overall success rate of 50%. The crystal structures of three new diclofenac co-crystals are reported herein: (diclofenac)·(2-aminopyrimidine), (diclofenac)·(2-amino-4,6-dimethylpyrimidine), and (diclofenac)·(2-amino-4-chloro-6-methylpyrimidine).
Highlights
Co-crystallization offers the supramolecular chemist a unique opportunity—it provides the ability to tune a compound’s physical properties without altering its chemical identity
Using solvent assisted grinding (SAG) and IR, eighteen compounds from three different families—pyrazoles, pyridines, and pyrimidines—were screened for their ability to co-crystallize with diclofenac
From the list of co-crystallizing agents presented in Table 1, three structures of diclofenac and
Summary
Co-crystallization offers the supramolecular chemist a unique opportunity—it provides the ability to tune a compound’s physical properties without altering its chemical identity. Infrared spectroscopy was used to probe the reaction of diclofenac with compounds from an extensive list of pyrazoles, pyridines, and pyrimidines spanning a wide range of charges on the aromatic nitrogen. The results from this screen as well as the crystal structures of three new co-crystals of diclofenac are presented in this study
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