Preparation method of cefdinir and novel intermediate compound thereof

Abstract

The invention discloses a preparation method of cefdinir and a novel intermediate compound thereof. The cefdinir is prepared by adopting a method which is simpler, short in line and more environmentally friendly, and the prepared cefdinir is high in yield and higher in purity. The following reaction formula is adopted by the preparation method. The reaction formula is as shown in the specification.

Description

technical field [0001] The invention relates to the technical field of preparation methods of compounds, in particular to a preparation method of cefdinir and a new intermediate compound thereof. Background technique [0002] Cefdinir (Cefdinir) is the third-generation oral cephalosporin developed by Fujisawa Pharmaceutical Co., Ltd. in Japan. It is to improve the effect of third-generation cephalosporins such as cefixime on G + Insufficiency of poor bacterial action, obtained by modifying the structure of cefixime, C 7 The position is the side chain of demethylaminothioxime, C 3 The position is vinyl, which maintains high stability to β-lactamase and improves the resistance to G + It is a broad-spectrum antibacterial active agent and can be used to treat Staphylococcus, Streptococcus, Pneumococcus, Peptostreptococcus, Propionibacterium, Neisseria gonorrhoeae, and Mora catarrh that are sensitive to cefdinir. bacteria, Escherichia coli, Klebsiella, Proteus mirabilis, Provi...

AI Technical Summary

Problems solved by technology

[0007] In these methods, the side chain is first introduced, then ring-closed, and then the method for removing the 4-carboxyl protecting group of the mother core has a long synthetic route, low yield, and product quality cannot be guaranteed, so it is only suitable for a small amount of preparation in the laboratory; the acid chloride method is adopted. The introduction of side chains needs to be reacted in a solvent without active hydrogen. Although the yield of the condensation process is high, the 4-position carboxyl protecting group needs to be removed. The side chain acid chloride is not easy to obtain and store, which also leads to low yield and low cost. High, not suitable for large-scale production; the method of constructing amide bonds by the active thioester method and modifying the 7-amino side chain has mild reaction conditions, is easy to operate, and has a high yield, but the reaction reagent used is more toxic, which is not conducive to environmental protection

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