Cefotetan disodium hydrate and preparation method and application thereof

A technology of cefotetan disodium and hydrate, which is applied in the field of medicine and achieves the effects of good sliding property, improved operability, and convenient storage and transportation

Inactive Publication Date: 2010-09-22
胡梨芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the published literature only reports Cefotetan disodium (Cefotetan disodium) (C 17 h 15 N 7 Na 2 o 8 S 4 , Molecular Weight: 619.58, CAS No.:...

Method used

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  • Cefotetan disodium hydrate and preparation method and application thereof
  • Cefotetan disodium hydrate and preparation method and application thereof
  • Cefotetan disodium hydrate and preparation method and application thereof

Examples

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Embodiment 1

[0037]Example 1 Preparation of Cefotetan Disodium Monohydrate Add 10 g of cefotetan diacid and 50 ml of water into a reaction flask, stir to form a suspension, add triethylamine dropwise at 5° C., and stir to make the pH to 7.5 Add 0.1 g of activated carbon, stir for 30 minutes, filter with suction, wash with water, filter with suction, add dropwise an ethanol solution of 28% sodium isooctanoate (5.81 g) in the filtrate at 5° C., stir for 40 minutes, slowly add 250 ml of acetone and 250ml of ethanol, place below -5°C to fully separate out the solid, filter with suction, wash with a small amount of ethanol and chloroform for 3 times, filter with suction, dissolve the obtained solid with a small amount of water, add 200ml of acetone and 100ml of ethanol as a crystallization solvent for recrystallization , placed below -5°C to fully separate the crystals, filter with suction, and vacuum-dry at about 45°C for about 5 hours to obtain 5.2g of off-white crystals, melting point: 140°C ...

Embodiment 2

[0038] Example 2 Preparation of Cefotetan Disodium Monohydrate Add 10 g of cefotetan diacid and 60 ml of water into a reaction flask, stir to form a suspension, add saturated sodium carbonate aqueous solution dropwise at 5°C to bring the pH to 7.0, and stir For 30 minutes, add 0.2 g of activated carbon, stir for 30 minutes, filter with suction, wash with water, and filter with suction, slowly add 300 ml of acetone and 200 ml of acetonitrile dropwise to the filtrate, and place it below -10°C to fully separate out the solid, filter with suction, wash with chloroform three times, and Filter and dissolve the obtained solid with a small amount of water, add 300ml of acetone, 200ml of acetonitrile, and 80ml of diethyl ether as the crystallization solvent for recrystallization, and place it below -10°C overnight to allow the crystals to fully separate out, filter with suction, and dry in vacuum at 45°C for about 5 hours. Obtained 5.6g of off-white crystals, melting point: 141°C discol...

Embodiment 3

[0039] Example 3 Preparation of Cefotetan Disodium 0.5 Hydrate Add 20 g of cefotetan diacid and 130 ml of water into the reaction flask, stir, add saturated sodium bicarbonate solution dropwise to the filtrate at 5°C to bring the pH to 6.9, and stir for 30 Minutes, add 0.2g of activated carbon, stir for 30 minutes, filter with suction, wash with water, filter with suction, slowly add 500ml of acetone and 150ml of diethyl ether dropwise to the filtrate, place it below -5°C to fully separate out the solid, filter with suction, wash with acetone and chloroform for 3 times , suction filtration, the resulting solid was just dissolved with a small amount of water, recrystallized with 300ml of acetone, 300ml of isopropanol, and 20ml of diethyl ether as the crystallization solvent, and placed overnight at -5°C to allow the crystals to fully separate out, suction filtered, and vacuum at 40°C After drying for about 24 hours, 11.2 g of off-white crystals were obtained. Melting point: 142°...

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Abstract

The invention relates to a cefotetan disodium hydrate and a preparation method and application thereof. The cefotetan disodium hydrate has high storage stability, and is applicable to the preparation of medicines for treating or preventing diseases of the human being or animals caused by gram-positive or gram-negative sensitive bacteria, such as respiratory system diseases, hepatobiliary system diseases, five-sense organ diseases, urinary tract infection, celiac infection, pelvic infection, ichorrhemia, skin tissue infection, bone and joint infections, cephalomeningitis and endocarditis.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to provide antibacterial drug-cefetetan disodium hydrate and its preparation method and application. Background technique [0002] Cefotetan disodium (Cefotetan disodium) was first developed by Fujisawa Co., Ltd. of Japan, and it was first listed in Japan in the late 1980s. Astra Company obtained the right to market the product outside Japan. The injection of Cefotetan was released in 2003. Approved to be listed in the United States in 2010, the trade name is CEFOZAN. This antibiotic is a second-generation cephalosporin, and its antibacterial mechanism is the same as that of other cephalosporins, and it mainly exerts bactericidal effect by inhibiting cell wall synthesis. It has a strong antibacterial effect on a variety of Gram-negative aerobic and anaerobic bacteria, such as Escherichia coli, Citrobacter, Klebsiella, Sandella, Proteus, and Haemophilus influenzae The effect is be...

Claims

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Application Information

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IPC IPC(8): C07D501/57C07D501/02A61K31/546A61K31/424A61K31/43A61K31/431A61P31/04A61P11/00A61P13/02A61P7/00A61P17/00A61P19/02A61P19/08A61P25/00A61P15/00A61K9/19A61K9/14A61K9/20A61K9/48A61K9/08
Inventor 刘力
Owner 胡梨芳
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