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Cefathiamidine hydrate, preparation method thereof and application thereof

A technology of cefathiamidine and hydrate, which is applied in the field of medicine to achieve the effects of low toxicity, good dissolution performance, and convenient storage and transportation

Inactive Publication Date: 2010-07-07
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, the published literature only reports Cefathiamidine (Cefathiamidine), chemical name (6R, 7R)-3[(acetoxy)methyl]-7-[α-(N,N-diisopropylamidinesulfur Base)-acetylamino]-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylate betaine (C 19 h 28 N 4 o 6 S 2 , Molecular weight: 472.59), up to now, there is no open bibliographical report cefathiamidine crystalline hydrate and its preparation method and application both at home and abroad

Method used

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  • Cefathiamidine hydrate, preparation method thereof and application thereof
  • Cefathiamidine hydrate, preparation method thereof and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Example 1 Preparation of Cefathiamidine 0.25 Hydrate Suspend 8 g of 7-bromoacetyl ACA in 160 ml of dichloromethane, add 3 ml of triethylamine, stir to dissolve completely, add 0.2 g of activated carbon and stir for 30 minutes, filter, filter Wash the cake with 10ml of dichloromethane, combine the filtrate and washing liquid, add 3.8g of N,N'-diisopropylthiourea, stir, react at 35-40°C for 1.5 hours, cool to below 15°C, and slowly add Acetone 200ml, chloroform 20ml, stand for 3 hours, filter with suction, soak the crystals with a small amount of chloroform and acetone for 3 times, filter with suction, dissolve the obtained solid in 20ml of water, slowly add 120ml of acetone, 20ml of acetonitrile, place below 10°C, After the precipitate is fully separated, it is dried by suction filtration, and the solid is dried at about 40°C for about 5 hours to obtain 3.3 g of off-white crystals, melting point: 155°C decomposition (ELECTROTHERMALMELTING POINT APPARATUS, uncorrected), HP...

Embodiment 2

[0038] Example 2 Example 1 Preparation of Cefathiamidine 0.5 Hydrate Suspend 8 g of 7-bromoacetyl ACA in 180 ml of dichloromethane, add 3.2 ml of diisopropylamine, stir to dissolve completely, add 0.2 g of activated carbon and stir for 25 minutes , filtered, the filter cake was washed with 10ml of chloroform, the combined filtrate and washing liquid were added with 3.8g of N,N'-diisopropylthiourea, stirred, reacted at 35-40°C for 1.5 hours, cooled to below 10°C, Slowly add 200ml of acetone and 20ml of ethyl acetate, let stand for 3 hours, filter with suction, soak the crystals with a small amount of acetone and acetonitrile for 3 times, filter with suction, dissolve the obtained solid in 20ml of water, slowly add 120ml of acetone, 20ml of ethanol, iso Propyl ether 10ml, place below 10°C, wait until the precipitate is fully separated, filter to dryness, and dry the solid at about 35°C for about 5 hours to obtain 3.0g off-white crystals, melting point: 155°C decomposition (ELECTR...

Embodiment 3

[0040] Example 3 Put 5 g of cefathiamidine in a container and add 10 ml of water to dissolve it, put the solution in a freeze-drying box, lower the temperature of the liquid to -40°C, and pre-freeze for 4 hours; lower the temperature of the condenser to -45°C, Vacuumize, control the degree of vacuum and control the temperature of the plate layer to rise below -15°C, freeze and sublimate, and sublimate and dry for about 17 hours; continue heating to gradually increase the temperature to about 30°C at a rate of 10°C per hour, and keep warm for about 3 hours. Close the hydrazine butterfly valve of the box for 3 minutes, and when the pressure of the box rises to within 5Pa, the entire freeze-drying process is ended, and the gas is released from the box to obtain cefathiamidine 0.5 hydrate; [α] D 20 : +140; Karl Fischer's method of measuring moisture is 1.96%, thermal analysis: platform weight loss of about 1.80%, which is within the error range with the result of the sample contai...

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Abstract

The invention relates to a cefathiamidine hydrate, a preparation method thereof and application thereof. The crystalline hydrate has high storage stability, and is applicable in preparing medicaments for treating or preventing gram positive or negative bacteria sensitive bacteria, infections of human or animal respiratory system, liver and biliary system, five sense organs and urogenital system, bone and joint infection and soft skin tissue infection caused by the gram positive or negative bacteria sensitive bacteria, and diseases such as endocarditis, ichorrhemia, meningitis and the like.

Description

technical field [0001] The invention relates to the technical field of medicines, and specifically provides an antibacterial drug-ceftiamidine hydrate, a preparation method and application thereof. Background technique [0002] At present, the published literature only reports cefathiamidine (Cefathiamidine), chemical name (6R, 7R)-3[(acetoxy)methyl]-7-[α-(N,N-diisopropylamidinesulfur Base)-acetylamino]-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylate betaine (C 19 h 28 N 4 o 6 S 2 , Molecular weight: 472.59), so far, there is no published literature at home and abroad to report cefathiamidine crystalline hydrate and its preparation method and use. Contents of the invention [0003] The present invention relates to cefathiamidine crystalline hydrate and its preparation method and application, furthermore, it relates to an antibacterial infection drug, that is, the pharmaceutically acceptable salt crystalline hydrate of alkyl acetaldehyde sulfite and its prepara...

Claims

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Application Information

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IPC IPC(8): C07D501/28C07D501/04A61K31/545A61P31/04
Inventor 刘力
Owner 刘力
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