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Inhibitor of tricycro beta lactamase and preparation method

A technology for lactamase and inhibitors, applied in the field of tricyclic β-lactamase inhibitors and its preparation, can solve the problems of curative effect reduction and failure

Inactive Publication Date: 2006-02-01
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] β-lactam antibiotics are the most widely used clinically effective, low-toxicity, broad-spectrum anti-infective drugs, but the resistance of β-lactamase-producing bacteria to β-lactam antibiotics has become the A serious pharmacological problem in which the efficacy of similar drugs is reduced or even ineffective

Method used

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  • Inhibitor of tricycro beta lactamase and preparation method
  • Inhibitor of tricycro beta lactamase and preparation method
  • Inhibitor of tricycro beta lactamase and preparation method

Examples

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Embodiment 1

[0020] 1) Preparation of 4-sulfonyloxyadamantan-2-one (2)

[0021] Mix 2-adamantanone (1) and ethanesulfonic acid at a molar ratio of 1:1.0 evenly, add sodium azide equivalent to 1.4 molar times of (1) at room temperature, and continue to react at 35°C until the conversion of raw materials is complete , then the reaction mixture was poured into crushed ice, neutralized with saturated aqueous sodium bicarbonate, and extracted 3 times with chloroform, the combined extracts were washed with saturated sodium chloride, dried over anhydrous sodium sulfate, and evaporated under reduced pressure to remove the solvent The resulting crude product was recrystallized from ethyl acetate / hexane to give 4-sulfonyloxyadamantan-2-one (2);

[0022] 2) Preparation of bicyclo[3.3.1]non-6-ene-3-carboxylic acid (±)-(3)

[0023] 4-sulfonyloxyadamantan-2-one (2) is dissolved in dichloromethane to make a 0.8 mol / liter solution, and 20% potassium hydroxide aqueous solution corresponding to (2) 4.5 mol...

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Abstract

A tricyclo-beta-lactamase depressant is prepared through preparing 4-sulfonyloxy adamantane-2-one, preparing bicyclo [3,3,1]-nonyl-6-enyl-3-formic acid [(+ / -)-(3)], preparing bicyclo [3,3,1] nonyl-6-enyl-3-formate or amide (+ / -)-(4), preparing 4-oxy-3-azatricyclo [5,3,1,02.5] undecane-9-formate or amide (+ / -)-(5), and preparing 4-oxy-3-azatricyclo [5,3,1,02.5] undecane-9-formate or amide-N-sulfonate (+ / -)-(6) solid.

Description

technical field [0001] The invention relates to an enzyme inhibitor, in particular to a class of tricyclic β-lactamase inhibitors and a preparation method thereof. Background technique [0002] β-lactam antibiotics are the most widely used clinically effective, low-toxicity, broad-spectrum anti-infective drugs, but the resistance of β-lactamase-producing bacteria to β-lactam antibiotics has become the It is a serious pharmacological problem that the curative effect of similar drugs is reduced or even becomes invalid. Discovered in recent years (You Hedong, Medicinal Chemistry, Beijing: Chemical Industry Press, 2004, 455-476; Zhang Chunhui, etc., research progress of β-lactamase inhibitor sulbactam [J], Chinese Journal of Veterinary Medicine, 2004 , 1:19-20; Bai Guoyi et al., Research progress of β-lactamase inhibitors[J], Chemical Industry and Engineering, 2001, 18:395-400) some β-lactam compounds such as clavulanic acid, Sulbactam and tazobactam, etc., can inhibit the dru...

Claims

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Application Information

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IPC IPC(8): C07D205/12
Inventor 陈安齐梁国娟
Owner XIAMEN UNIV
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