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Preparation method of flomoxef parent nucleus

A technology of Oxycephem nucleus and Fluoxefem, which is applied in the field of medicine and chemical industry, can solve the problems of hindering bacterial cell wall biosynthesis and less research, and achieve the effects of low production cost, easy industrialization, and simple synthesis operation

Inactive Publication Date: 2019-07-19
山西千岫制药有限公司
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AI Technical Summary

Problems solved by technology

[0002] Fluoxefef is an Oxecefem (Oxacephalosporin) antibiotic similar to Latamoxef. Instead, similar to other β-lactam antibiotics, flumoxef may also inhibit bacterial cell wall biosynthesis by binding to one or more penicillin-binding proteins (PBPs), thereby inhibiting bacterial activity. Currently, There is a certain amount of research on the literature on the removal of carboxyl protecting groups in China, but there is less research on fluoxyceph in the early stage. The present invention discloses a key preparation technology from the mother nucleus of fluoxycephm to the mother nucleus of fluoxycephin

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  • Preparation method of flomoxef parent nucleus
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  • Preparation method of flomoxef parent nucleus

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preparation example Construction

[0032] A preparation method of fluoxycephalosporin nucleus, comprising the following preparation steps:

[0033] (1) Add oxycephem nuclei and chloroform to the reaction vessel, stir until the oxycephem nuclei are completely dissolved, add organic base and phosphorus pentachloride to the reaction feed liquid, and control the reaction temperature at -10 to 10°C , as the reaction proceeds, naturally heat up to 0-5°C, keep warm, and the reaction time is 1.5-5h;

[0034] (2), after the reaction of step (1) is completed, add methanol to the reaction feed liquid and control the temperature at 0-5°C, stir the reaction feed liquid, and the reaction time is 1.5-5h;

[0035] (3) After the reaction in step (2), add purified water to the reaction feed liquid, stir the reaction feed liquid for 5 to 15 minutes, let it stand for stratification, take the chloroform phase, add sodium sulfate to the chloroform phase to dry , obtain the reaction feed liquid containing intermediate 1 after filtra...

Embodiment

[0046] Example: Add 10.00 g (0.0193 mol) of oxycephem parent nucleus and 50 mL of chloroform into the reaction vessel, stir until the oxycephem parent nucleus is completely dissolved, control the temperature of the reaction feed liquid to -10 ° C, and add Add quinoline 2.74g (0.0213mol), then add phosphorus pentachloride 4.23g (0.0203), as the reaction proceeds, the reaction feed liquid naturally warms up to 0 ~ 5 ℃, heat preservation, the reaction time is 2h, after the reaction, Add 50ml of methanol to the reaction feed liquid, control the reaction temperature at 0-5°C, keep warm, stir for 3 hours, take a sample for detection, after the reaction is complete, add 100 ml of purified water to the reaction feed liquid, stir for 5 minutes, let stand for stratification, and take chloroform Add 1g of sodium sulfate to dry, filter to obtain the reaction feed liquid containing intermediate 1, add tert-butyl hypochlorite 4.20g (0.0387mol) to the reaction feed liquid, then add dropwise t...

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Abstract

The invention discloses a preparation method of a flomoxef parent nucleus. The preparation method comprises the following preparation steps: in a chloroform solvent, reacting an oxycephem parent nucleus with an organic alkali and phosphorus pentachloride, removing a 7th-site protecting group under the action of methanol, washing the reaction material liquid with water, then conducting drying and filtering, sequentially adding a methanol solution of tert-butyl hypochlorite and lithium methoxide for reaction, washing the reaction material liquid with water again after the reaction is ended, thenconducting drying and filtering, and adding pyridine and difluoromethylthio acetyl chloride for reaction, so as to obtain a final product, namely the flomoxef parent nucleus after the reaction is finished. The preparation method of the flomoxef parent nucleus disclosed by the invention has the advantages that the raw materials are cheap and easy to obtain, the production cost is low, the synthesis operation is simple, the purity of the finished product can reach 99%, and the preparation process is continuous production and is easy to industrialize.

Description

technical field [0001] The invention relates to the technical field of medicine and chemical industry, in particular to a method for preparing fluoxycephalosporin mother nuclei. Background technique [0002] Fluoxefef is an Oxecefem (Oxacephalosporin) antibiotic similar to Latamoxef. Instead, similar to other β-lactam antibiotics, flumoxef may also inhibit bacterial cell wall biosynthesis by binding to one or more penicillin-binding proteins (PBPs), thereby inhibiting bacterial activity. Currently, There is a certain amount of domestic research on the removal of the carboxyl protecting group, but there is little research on fluoxyceph in the early stage. The present invention discloses a key preparation technology from the mother nucleus of fluoxycephene to the mother nucleus of fluoxycephin. Contents of the invention [0003] The object of the present invention is exactly in order to solve the above-mentioned problem, and a kind of preparation method of flumoxyceph mothe...

Claims

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Application Information

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IPC IPC(8): C07D505/18C07D505/06C07D505/08
CPCC07D505/06C07D505/08C07D505/18Y02P20/55
Inventor 王作弟
Owner 山西千岫制药有限公司
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