Technology for producing cefdinir by changing organic base feeding mode

Abstract

A technology for producing cefdinir by changing an organic base feeding mode comprises the following steps: 1), 7-AVCA (7-amino-3-vinyl-3-cephem-4-carboxylic acid), dimethylacetamide and an organic solvent are added into a reaction kettle, and the temperate is decreased to subzero 5 DEG C; 2), triethylamine is added in one time, and stirring is performed for 10 min; 3), active ester is added, and a reaction is performed for 20-25 h at the temperature of 0-5 DEG C; 4), an end point of the reaction is detected, p-toluene sulfonic acid is added, and the mixture is stirred for 30 min; 5), an intermediate is dissolved in the organic solvent, and acid is added, and the mixture is stirred for 30 min; 6), cefdinir salt is obtained through filtering; and 7), the cefdinir salt is dissolved in the organic solvent, base is added to regulate the pH value, activated carbon is added for decoloration, and cefdinir is obtained. The technology has the benefits as follows: the triethylamine feeding mode is changed from original dripping to direct one-time feeding in a condensation step for cefdinir synthesis, meanwhile, the temperature before and after feeding is controlled, so that the operation steps are reduced for a worker, the production time is shortened, labor intensity of the worker is reduced, and 7-AVCA stability and reaction yield can be guaranteed simultaneously.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a process for producing cefdinir by changing the way of adding organic base. Background technique [0002] Cefdinir is a third-generation broad-spectrum antibiotic developed by Japan Fujisawa Pharmaceutical Co., Ltd. It has well-balanced antibacterial activity against Gram-positive and negative aerobic and anaerobic bacteria, especially Gram-positive bacteria such as methicillin-sensitive Staphylococcus aureus (MIC is 0.39mg / L), Streptococcus pyogenes and Streptococcus pneumoniae (MICs are 0.025mg / L and 0.1mg / L, respectively), with very strong antibacterial activity. In addition, it is superior to cefaclor in its activity against major Gram-negative bacteria such as Escherichia coli and Klebsiella pneumoniae, and against important respiratory pathogens such as Moraxella catarrhalis and Haemophilus influenzae. It is more stable to β-lactamase than cephalexin and cefaclor. [0003] The s...

AI Technical Summary

Problems solved by technology

The feeding method of the organic base is usually slowly dropped to control the pH value. Although a better product yield is obtained in this way, the workload of the staff is increased, and the process needs to be improved.

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