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Latamoxef aluminium chloride (stannum)-anisole complex, as well as preparation method and application thereof

A technology of Latamoxef aluminum chloride and Latamoxef, which is applied in tin organic compounds, chemical instruments and methods, compounds containing Group 3/13 elements of the periodic table, etc., can solve severe equipment corrosion, high equipment requirements, Recycling difficulties and other problems, to achieve the effect of low cost, simple preparation method, and overcome the lack of purity

Active Publication Date: 2012-07-25
ZHEJIANG WHITESON PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] In this method, there is following shortcoming, and the consumption of trifluoroacetic acid is 8-10 times of required amount, and excessive trifluoroacetic acid is difficult to completely remove completely, and can remain in latamoxycetidine, for trifluoroacetic acid In addition, it needs to be salted with sodium bicarbonate, and purified with resin after acidification to obtain Latamoxefacic acid; at the same time, trifluoroacetic acid is a highly corrosive chemical raw material, which severely corrodes equipment, requires high equipment, and is difficult to recycle.

Method used

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  • Latamoxef aluminium chloride (stannum)-anisole complex, as well as preparation method and application thereof
  • Latamoxef aluminium chloride (stannum)-anisole complex, as well as preparation method and application thereof
  • Latamoxef aluminium chloride (stannum)-anisole complex, as well as preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Compound IV (R1 = p-methoxybenzyl, R2 = p-methoxybenzyl) (100 g) was dissolved in dichloromethane (500 mL), cooled to -25 ° C, added anisole (250 mL), batch Add aluminum trichloride (80g), keep warm at -25°C for 4.0h, filter, beat and wash the solid with dichloromethane (300mL), filter and dry to obtain 138.4g of Latamoxefal aluminum chloride anisole complex.

[0035] Content detection: Latamoxef: 38.4%, aluminum 10.0%, chlorine: 31.6%, anisole: 20.0%, calculation n=2, m=2.5

Embodiment 2

[0037] The mixture of dichloromethane (500mL) and anisole (100mL) was cooled to -20°C, aluminum chloride (50g) was added, and compound IV (R1=p-methoxybenzyl, R2=p-methoxybenzyl) was added in batches benzyl (100g), keep warm at -15~-20°C for 3.0h, filter, beat and wash the solid with dichloromethane (200mL), filter and dry to obtain 95.4g of Latamoxefal Aluminum Chloride Anisole Complex.

[0038] Content detection: Latamoxef: 56.3%, aluminum: 8.8%, chlorine: 23.2%, anisole: 11.7%, calculation n=0, m=1.0

Embodiment 3

[0040] Anisole (350mL) was cooled to -15°C, aluminum chloride (65g) was added, and dichloride of compound IV (R1=p-methoxybenzyl, R2=p-methoxybenzyl) (100g) was added dropwise. Methane (500 mL) solution was incubated at -15 to -20°C for 2.0 h, filtered, the solid was washed with dichloromethane (350 mL), filtered and dried to obtain 131.2 g of Latamoxefal aluminum anisole complex.

[0041] Content detection: Latamoxef: 40.8%, aluminum: 8.5%, chlorine: 25.2%, anisole: 25.5%, calculation n=1, m=3.0

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Abstract

The invention relates to an intermediate for synthesizing latamoxef and a preparation method of the intermediate. The intermediate provided by the invention is a latamoxef aluminium chloride (stannum)-anisole complex which is simple and convenient in preparation method, easy to separate, high in content and yield and stability and low in cost and can be conveniently converted to latamoxef acid (sodium) for current use, so that the difficulty that purity of latamoxef acid (sodium) synthesized by the prior art is inadequate can be overcome. The latamoxef sodium prepared by using the complex as raw material and hydrolyzing has a purity of greater than 99%, and the purity is considerably higher than the standard of the Chinese pharmacopoeia (single impurity is not higher than 2% and total impurities are not higher than 5%) and that of the Japanese pharmacopoeia.

Description

technical field [0001] The invention belongs to the technical field of latamoxef intermediate and its preparation method. Background technique [0002] Latamoxef is an oxycephem antibiotic developed by Shionogi Pharmaceutical Co., Ltd. in Japan. Its disodium salt was first listed in Germany under the trade name "Festmoxin" in 1981. After 1982, it was mainly sold in Japan and South Korea for clinical use. Named "shiomarin". Latamoxef has a broad antibacterial spectrum, and its antibacterial activity is similar to that of the third-generation cephalosporins. Its effect on Gram-negative bacilli is 4 to 16 times stronger than that of general cephalosporins, and its effect on anaerobic bacteria, especially Bacteroides fragilis, is obviously superior. It is suitable for the first, second and third generation cephalosporins; it is highly stable to β-lactamase and has a strong antibacterial effect on enzyme-producing drug-resistant negative bacilli and Staphylococcus aureus; the T1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/06C07F7/22C07D505/20
CPCY02P20/55
Inventor 钱静杰方秀炜
Owner ZHEJIANG WHITESON PHARMA
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