Cephalosporins Intermediates (Z) Synthesis And Drug-2-Methoxy Imino-2-Furan Acetic Acid Ammonium Salt Eutectic Preparation

Cephalosporin drugs are clinically very extensive application anti-infectives medicine inparticular, cefuroxime sodium and cefuroxime axetil antibacterial effect are good, low toxicand side effect, it is a commonly used at home and abroad of antibacterial drugs. The (Z)-2-methoxy imino furan ammonium acetate (-2-SMIA) is an important intermediate species ofthe synthesis of cephalosporins cefuroxime sodium and cefuroxime axetil chain.In this paper, through the synthetic technics conditions in the experiment on the basis ofthe original materials hace been improved,namely,using acetyl furan as raw material, preparedthe2-oxo-2-furan acetic acid, then oximation reaction and methoxyamine hydrochloride,was (Z)-2-methoxy imino furan acetic acid ammonium salt-2-was prepared. Experimentsresults show that, in the preparation of2-oxo-2-furan acetic acid, sodium nitrite additiontime, reaction temperature and pH changes,etc, have significant effects on the experimentalresults. In this paper we eventually made comprehensive yield of product reach55%bycontrolling sodium nitrite reaction time, reaction temperature and pH values through a seriesof experiments which is of great significance for industrial production and life.In recent years, the cocrystal is a new subject for more and more attention, in the medical,pharmaceutical, chemical and biological aspects, it is more and more important for thecontribution of life. With the rapid development of the crystal engineering of supramolecularchemistry, development of drug crystal situation also received more and more attention. Inthis paper, through the analysis of the active pharmaceutical ingredient, we have successfulsynthesis of three fluorine-4,4，-bipyridine pharmaceutical cocrystals.Synthesis includes solvent evaporation method,the cocrystal grinding method,supercritical fluid method et al. Physicochemical properties of drugs affected by the noveleutectic compounds, such as stability, melting point, solubility, hygroscopicity, metabolicstability, rate of dispersion, solubility, drug delivery have been improved. Synthesis ofpharmaceutical cocrystals is ineffable for effect of medical and health industry, trustingproducts also point the day and await for it.