阅读说明：本技术 一种水溶性氟苯尼考钠盐的制备方法 (Preparation method of water-soluble florfenicol sodium salt ) 是由 王存亮 许灵艳 严学文 黄焕军 王小桥 于 2018-06-27 设计创作，主要内容包括：本发明公开了一种水溶性氟苯尼考钠盐的制备方法,首先在有机溶剂中加入氟苯尼考,琥珀酸或柠檬酸,加入缚酸剂,反应制备氟苯尼考单酯,加入氢氧化钠或碳酸氢钠反应得到水溶性氟苯尼考钠盐；本发明工艺简单,成本低,转化率高,产品水溶性和稳定性好,适合企业化生产。(The invention discloses a preparation method of water-soluble florfenicol sodium salt, which comprises the steps of firstly adding florfenicol, succinic acid or citric acid into an organic solvent, adding an acid-binding agent, reacting to prepare florfenicol monoester, and adding sodium hydroxide or sodium bicarbonate to react to obtain the water-soluble florfenicol sodium salt; the method has the advantages of simple process, low cost, high conversion rate, good water solubility and stability of the product, and suitability for industrialized production.)

1. A preparation method of water-soluble florfenicol sodium salt is characterized by comprising the following steps: adding florfenicol, succinic acid or citric acid into an organic solvent, adding an acid-binding agent, reacting to prepare florfenicol monoester, and adding sodium hydroxide or sodium bicarbonate to react to obtain the water-soluble florfenicol sodium salt.

2. The method for preparing the water-soluble florfenicol sodium salt according to claim 1, wherein the method comprises the following steps: the organic solvent is any one or more of dichloromethane, chloroform and ethyl acetate.

3. The method for preparing the water-soluble florfenicol sodium salt according to claim 1, wherein the method comprises the following steps: the acid-binding agent is any one or more of diethylamine, triethylamine and N, N-dimethylformamide.

4. The preparation method of the water-soluble florfenicol sodium salt according to claim 1, characterized in that the weight ratio of the organic solvent to the florfenicol is 5 ~ 10:1, and the molar ratio of the florfenicol, succinic acid and the acid-binding agent is =1:1 ~ 3:2 ~ 7.

Technical Field

The invention relates to a preparation method of a compound, in particular to a preparation method of water-soluble florfenicol sodium salt.

Background

Florfenicol is a new generation of broad-spectrum antibiotic special for chloramphenicol animals, has the characteristics of broad-spectrum antibacterial property, good absorption, wide in-vivo distribution, safety, high efficiency and the like, particularly has no potential effects of causing aplastic anemia, teratogenicity, carcinogenesis and mutagenesis, has obvious treatment effect on animal bacterial diseases caused by sensitive bacteria, has extremely wide antibacterial spectrum, and brings great inconvenience to clinical application due to low water solubility of florfenicol, so researchers do a lot of work on the aspect. Starting from the solvent perspective, many florfenicol injections and oral exclusive solvents have been introduced. Although the water solubility is improved to a certain extent, problems still exist in the using process, such as low temperature, slow dissolving speed or florfenicol precipitation in the prepared solution; in the dissolving process, if water exists, florfenicol is separated out, the solution becomes turbid, and the production cost is increased if a special solvent is used.

Disclosure of Invention

The invention aims to provide a preparation method of florfenicol sodium salt with good water solubility and good stability.

The invention is realized by the following technical scheme: adding florfenicol, succinic acid or citric acid into an organic solvent, adding an acid-binding agent, reacting to prepare florfenicol monoester, and adding sodium hydroxide or sodium bicarbonate to react to obtain the water-soluble florfenicol sodium salt.

The organic solvent is any one or more of dichloromethane, chloroform and ethyl acetate.

The acid-binding agent is any one or more of diethylamine, triethylamine and N, N-dimethylformamide.

The weight ratio of the organic solvent to the florfenicol is 5 ~ 10:1, and the molar ratio of the florfenicol, the succinic acid and the acid-binding agent is =1:1 ~ 3:2 ~ 7.

The method has the advantages of simple process, low cost, high conversion rate, good water solubility and stability of the product, and suitability for enterprise production.

Detailed Description