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Carbapenems antibiotics

A compound and carboxyl technology, applied in the field of medicine, can solve the problems of not meeting clinical needs, increasing bacterial resistance, and low clinical availability.

Inactive Publication Date: 2013-09-04
黄振华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Moreover, due to the increase in clinical application of penem antibiotics, bacterial resistance continues to increase, and due to the limitation of digestive tract absorption, the currently marketed penem antibiotics can only be administered as injections in clinical practice, and the clinical utilization is not high. , can not meet the clinical needs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0174] Example 1 Preparation of 3-mercapto-N-(ethylbenzoate-3-yl)methyl-azetidine

[0175] In the dry reaction flask, add 3-acetylthio-azetidine 13.1g (100mmol), dichloromethane 100ml, triethylamine 20ml, then drop into 3-bromomethyl-ethyl benzoate 24.3g ( 100mmol) in 100ml of dichloromethane solution, stirred at room temperature for 6 hours, after the reaction was completed, 100ml of water was added, the organic layer was separated, dried, concentrated under reduced pressure and evaporated to remove the solvent, the residue was added to 100ml of dichloromethane, stirred to dissolve, and then added 4mol / 50ml of hydrochloric acid solution in L, heated up to 40°C, stirred for 2 hours, and the reaction was completed, the organic layer was separated, dried, and the solvent was evaporated under reduced pressure, and the residue was recrystallized from ethyl acetate-cyclohexane to obtain a light yellow solid product 21.8 g, yield: 86.8%.

Embodiment 2

[0176] Example 2 Preparation of 3-mercapto-N-(ethyl benzoate-3-yl)methyl-pyrrolidine

[0177] Preparation method Referring to Example 1, 14.5 g (100 mmol) of 3-acetylthio-pyrrolidine and 24.3 g (100 mmol) of ethyl 3-bromomethyl-benzoate were added to obtain 23.5 g of the product, yield: 88.4%.

Embodiment 3

[0178] Example 3 Preparation of 3-mercapto-N-(ethyl benzoate-3-yl)methyl-piperidine

[0179] Preparation method Referring to Example 1, 15.9 g (100 mmol) of 3-acetylthio-piperidine and 24.3 g (100 mmol) of ethyl 3-bromomethyl-benzoate were added to obtain 22.8 g of the product, yield: 81.6%.

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Abstract

The invention belongs to the field of medicine technology, more specifically relates to carbapenems antibiotics, and pharmaceutically acceptable salt, hydrolyzed ester, isomer, hydrate, hydrate of ester or salt thereof shown in the general formula (I), wherein, R1, R2, R3 and ring A are defined in the specification; the invention also relates to the preparation method of compounds, and pharmaceutical composition containing the compounds, and purposes of the compounds in preparation of medicaments for infectious disease treatment and / or prevention.

Description

1. Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to penem antibiotics, pharmaceutically acceptable salts thereof, easily hydrolyzed esters, isomers thereof, hydrates thereof, and hydrates of esters or salts thereof, and the preparation of these compounds Methods, pharmaceutical compositions containing these compounds, and uses of these compounds in the preparation of medicaments for treating and / or preventing infectious diseases. 2. Background technology [0002] Penem antibiotics are a class of β-lactam antibiotics developed in the 1970s. It has attracted much attention because of its broad antibacterial spectrum, strong antibacterial activity, and stability to β-lactamase. Its structural feature is that the sulfur at the 1-position of the penicillane core is replaced by carbon, and the 2-position has a double bond, which combines the five-membered ring of penicillin and the conjugated double bond of cephalosporin...

Claims

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Application Information

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IPC IPC(8): C07D477/20A61K31/407A61P31/04
CPCY02P20/55
Inventor 黄振华
Owner 黄振华
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