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Preparation method of latamoxef mother nucleus

A technology of Latamoxef mother nucleus and Oxefefene mother nucleus, which is applied in the field of preparation of Latamoxef mother nucleus, can solve the problems of less research on Latamoxef, achieve the advantages of purity, simple synthesis operation, and easy industrialization

Inactive Publication Date: 2019-07-12
山西千岫制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Latamoxef works by inhibiting bacterial cell wall biology Synthesized to play a bactericidal effect. Compared with the first and second generation cephalosporins, its antibacterial spectrum is further expanded, and it is highly stable to β-lactamase, so it is resistant to penicillinase. strain Or some Gram-negative bacteria resistant to the first and second-generation cephalosporins have antibacterial effects. At present, there are certain studies on the literature on the removal of carboxyl protecting groups in China, but there are few studies on Latamoxef in the early stage. This right provides A key preparation technology from Oxefem nucleus to Latamoxef nucleus

Method used

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  • Preparation method of latamoxef mother nucleus
  • Preparation method of latamoxef mother nucleus
  • Preparation method of latamoxef mother nucleus

Examples

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preparation example Construction

[0040] A preparation method for Latamoxef mother nucleus, comprising the following preparation steps:

[0041] (1), add oxycephem parent nucleus and dimethylformamide in reaction vessel, stir until oxycephem parent nucleus dissolves completely;

[0042] (2), after the oxycephem mother nucleus dissolves completely in the step (1), add 1-methyl-5-mercaptotetrazolium in the reaction feed liquid, the reaction temperature is controlled at 0~20 ℃, stirs the reaction feed liquid, The reaction time is 1.5~5h;

[0043] (3) After the reaction in step (2) is completed, add crystallization solvent 1 to the reaction feed liquid, stir the reaction feed liquid, the crystallization time is 0.5-3h, filter after crystallization, wash the crystals with a leaching solvent and dry to obtain the product (6R,7R)-7-[(4-methylbenzoyl)amino]-3-[(1-methyl-1H-tetrazol-5-ylthio)methyl]-8-oxo- 5-Oxa-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester (001);

[0044] (4) Mix and stir (001) wi...

Embodiment

[0060] Example: Add 20 g (0.0387 mol) of the oxycephem nucleus and 100 mL of dimethylformamide into a reaction vessel, stir until the oxycephem nucleus is completely dissolved, and control the temperature at 15° C., 1-methyl-5-mercapto Tetrazolium 4.94g (0.0425mol), stirred for 2h, after the reaction was over, 100ml of purified water was added to the reaction feed liquid, stirred for 0.5h, filtered after crystallization, washed with 30ml of methanol, and dried at 40°C to obtain (001 ), take (001) 22.16g (0.0371mol) and dichloromethane 220mL, stir until (001) is completely dissolved, add pyridine 5.87g (0.0742mol) to the reaction feed liquid, add phosphorus pentachloride 9.26g (0.0445 mol), the control reaction temperature is 15°C, and the reaction time is 2h. After the reaction, 150ml of methanol is added to the reaction feed liquid, and the reaction time is 2h. After the reaction, 6.05g (0.0853mol) of chlorine gas is passed into the reaction feed liquid , control the reaction...

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Abstract

The invention discloses a preparation method of latamoxef mother nucleus, comprising the following preparation steps: oxacephem mother nucleus, which is used as a raw material, reacts with 1-methyl-5-mercaptotetrazole to prepare (001); 7 protective groups are removed from (001) to prepare (002); and (002) reacts with chlorine and lithium methoxide to prepare the final product latamoxef mother nucleus. The latamoxef mother nucleus preparation method disclosed in the invention has advantages of low cost, simple synthetic operation and easy industrialization. In addition, the product purity (HPLC) can reach 99%. The preparation method has great advantages in the aspect of purity.

Description

technical field [0001] The invention relates to the technical field of medicine and chemical industry, in particular to a preparation method of Latamoxef mother nucleus. Background technique [0002] Latamoxef works by inhibiting bacterial cell wall biology Synthesized to play a bactericidal effect. Compared with the first and second generation cephalosporins, its antibacterial spectrum is further expanded, and it is highly stable to β-lactamase, so it is resistant to penicillinase. strain Or some Gram-negative bacteria resistant to the first and second-generation cephalosporins have antibacterial effects. At present, there are certain studies on the literature on the removal of carboxyl protecting groups in China, but there are few studies on Latamoxef in the early stage. This right provides A key preparation technology from Oxecefem nucleus to Latamoxefm nucleus has been developed. Contents of the invention [0003] The object of the present invention is exactly in or...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D505/18C07D505/16C07D505/06
CPCC07D505/06C07D505/16C07D505/18Y02P20/55
Inventor 王作弟
Owner 山西千岫制药有限公司
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