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Derivant of Deacetoxy cephalosporanicacid, preparation and application
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A technology for acetoxycephalosporanic acid and derivatives, which is applied in the field of new cephalosporins, and can solve the problems that the synthesis method of desacetoxycephalosporanic acid derivatives has not been disclosed.
Active Publication Date: 2007-05-16
GUANGZHOU BAIYUNSHAN PHARM CO LTD
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Problems solved by technology
The new derivatives of deacetoxycephalosporanic acid and their salts and their synthetic methods have not been disclosed
Method used
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Embodiment 1
[0059] Preparation of 3-deacetoxy-7-bromoacetamicephalosporanic acid:
[0060] Add 30ml of acetonitrile and 10g of 3-desacetoxy-7-aminocephalosporanic acid (7-ADCA) into a 250ml three-necked flask, add 6ml of tetramethylguanidine at 10°C-30°C, and add Bromoacetyl bromide 1.3ml, react at 0-5°C for 3 hours, add hydrochloric acid to adjust PH=1-2, solid precipitates, stir and grow crystals for 3 hours, filter, vacuum dry at room temperature until the water content is 3%, and obtain 8.6 grams of 3-methyl -7-Bromoacetamidocephalosporanic acid. Content 96% (HPLC).
Embodiment 2
[0062] Preparation of 3-deacetoxy-7-bromoacetamide cephalosporanic acid:
[0063] Add 80ml of dichloromethane, 10g of 3-deacetoxy-7-aminocephalosporanic acid (also known as 7-ADCA) into a 250ml three-necked flask, add 6ml of triethylamine dropwise at 0-10°C, and add 20ml of 2.5% NaHCO 3 Aqueous solution, 2.3ml of bromoacetyl bromide reacted for 3 hours, after the reaction was completed, let stand to separate the phases, discarded the organic phase, added hydrochloric acid to the aqueous phase to adjust the pH=1-2, precipitated a solid, grew crystals for 2 hours, filtered, and vacuum dried to 2 %, get 12.8 grams of product, content 95% (HPLC)
Embodiment 3
[0065] Preparation of 3-deacetoxy-7-bromoacetamicephalosporanic acid:
[0066] Add 160ml of ethyl acetate, 60ml of methanol, 60ml of water, 20g of 7-ADCA into a 500ml three-necked flask, add 12ml of triethylamine, dissolve the solid, add 9ml of bromoacetyl bromide at 0-15°C, react for 4 hours, separate phases, and water Use pH=1-2, grow crystals for 3 hours, filter, and vacuum-dry for 2 hours to obtain 24.6 g of the product. Content 93% (HPLC)
[0067] Preparation of the final product
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Abstract
A deacetoxy cephalophytanic acid derivative or its pharmacologically acceptable salt is disclosed, which has high antibacterial activity to G+ bacterium and a certain antibacterial activity to enteroococcus and G- bacterium. It is prepared by the reaction between deaetoxy cephalophytanic acid (7-ADCA) and bromoacetyl bromine or N,N bisubstituted thiourea.
Description
technical field [0001] The present invention relates to new cephalosporins, more specifically, the present invention relates to deacetoxy cephalosporanic acid derivatives with antimicrobial activity and pharmaceutically acceptable salts thereof, as well as their preparation methods and applications. technical background [0002] Deacetoxycephalosporanic acid 7-ADCA is an important cephalosporin nucleus, and a series of important cephalosporins were synthesized from 7-ADCA as the starting material. By modifying its C-7 position and introducing p-hydroxyphenylglycine and p-hydroxydihydrophenylglycine, the first-generation cephalosporins such as cephalexin, cephradine, and cefadroxil, which are quite effective against Gram-positive bacteria, were successfully prepared ; The side chain of aminothioxime acetic acid was introduced into the side chain at the 7th position to obtain the third-generation cephalosporin ceftazidime pivoxil and the like. All of these varieties have exce...
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