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Process for preparing mezlocillin sodium by utilizing a solvent and crystallization

The technology of mezlocillin sodium and solvent is applied in the field of preparing mezlocillin sodium by solvent crystallization, which can solve the problems of poor solubility, low product purity, high energy consumption of mezlocillin sodium and the like, and achieves high solubility, high product yield, Great effect of dissolving

Inactive Publication Date: 2020-07-31
JIANGSU HAIHONG PHARMA
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  • Abstract
  • Description
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Problems solved by technology

[0003] In view of the above problems, the present invention starts with human basic raw materials, optimizes the production process of mezlocillin sodium, and overcomes the problems of high energy consumption, low product purity and poor solubility of mezlocillin sodium by freeze-drying method

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  • Process for preparing mezlocillin sodium by utilizing a solvent and crystallization

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Embodiment 1

[0027] This embodiment utilizes solvent crystallization to prepare mezlocillin sodium. The specific process is as follows figure 1 Shown:

[0028] 1) Synthesis of 1-methylsulfonyl-2-imidazolidinone

[0029] At room temperature, take 40g of 2-imidazolidinone and 60g of methanesulfonyl chloride, put them into a 500mL three-neck flask equipped with mechanical stirring and reflux condenser, turn on the stirring device to mix evenly; then slowly raise the temperature to 65°C for reaction 1h, then raise the temperature to 105-110°C, and react for 4h. During this process, the material gradually became viscous and formed a white solid. After the reaction, 400mL of water was added to dissolve, and the temperature was lowered to 15°C to crystallize, then filtered, and vacuum-dried at 40°C to make Its water content is less than 0.5%, so as to obtain 47g of 1-methylsulfonyl-2-imidazolidinone, the yield is 61.6%, and its melting point is 189-192°C.

[0030] 2) Synthesis of 1-chloroform...

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Abstract

The invention discloses a process for preparing mezlocillin sodium by utilizing a solvent and crystallization. The process comprises firstly synthesizing 1-chloroformyl-2-imidazolidinone; then synthesizing 1-chloroformyl-3-methylsulfonyl-2-imidazolidinone and mezlocillin acid, and finally synthesizing the mezlocillin sodium. Starting from human basic raw materials, the production process of mezlocillin sodium is optimized, the obtained product is high in content, good in solubility and easy to redissolve, a series of problems in a freeze-drying process are solved, and further popularization ofthe product is facilitated.

Description

technical field [0001] The invention relates to a process for preparing mezlocillin sodium by solvent crystallization. Background technique [0002] Mezlocillin sodium is one of the national essential medicines. It is a downstream product of penicillin industrial salt and belongs to the third generation of semi-synthetic broad-spectrum antibiotics. Mezlocillin sodium has good acid resistance, alkali resistance and enzyme resistance, has strong antibacterial effect on Gram-positive cocci and bacillus, and has definite curative effect on bacterial infections such as Pseudomonas aeruginosa, Lebsiella pneumoniae and streptococcus. In recent years, driven by the promotion of rational drug use, the output of mezlocillin sodium has grown rapidly. At present, the domestic production of mezlocillin sodium is mainly based on the freeze-drying process. The products obtained by this process have a series of problems such as low content, poor solubility, and difficulty in reconstitution...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/68C07D499/18C07D499/16
CPCC07D499/68C07D499/18C07D499/16C07B2200/13
Inventor 许前辉李文凯
Owner JIANGSU HAIHONG PHARMA
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