Preparation process of biapenem

A preparation process and biapenem technology are applied in the field of preparation technology of biapenem, which can solve the problems of increasing the cost of recovered solvent, low purity of the preparation process, large amount of solvent used, etc., and achieves reduction of industrial production cost and simple process. , the effect of high yield

Inactive Publication Date: 2014-02-12
ANHUI YOUCARE KAIYUE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Compared with the preparation process of apenem, the existing technology has lower purity and a large amount of solvent used, which increases the cost of solvent recovery

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A preparation process of biapenem: comprising the following steps:

[0021] 1, the preparation of two (6,7 dihydro-5H-pyrazol [1,2-α] [1,2,4] triazolium-6-yl) disulfide dichloride (product 1): to Add 14 g of bis(4-pyrazolidinyl) disulfide dihydrochloride, 20 g of potassium bicarbonate, and 300 ml of water into a 1 L three-necked flask. After cooling in an ice bath until the internal temperature reached 0°C, 55 g of ethoxymethimine hydrochloride was added. After stirring for 1 h, the pH was adjusted to 3-4 with hydrochloric acid, and evaporated to dryness under reduced pressure to obtain a white solid. Add ethanol to dissolve, and filter with suction to remove insoluble matter. The filtrate was evaporated to dryness to obtain a pale yellow oil. Add ethanol to dissolve the activated carbon for decolorization, and slowly cool and crystallize to obtain 12.3 g of a light yellow solid with a yield of 69%.

[0022] 2. Preparation of dihydro-6-mercapto-5H-pyrazol[1,2-α][1,2...

Embodiment 2

[0027] A preparation process of biapenem: comprising the following steps:

[0028] 1, the preparation of two (6,7 dihydro-5H-pyrazol [1,2-α] [1,2,4] triazolium-6-yl) disulfide dichloride (product 1): to Add 12 g of bis(4-pyrazolidinyl) disulfide dihydrochloride, 20 g of potassium bicarbonate, and 310 ml of water into a 1 L three-necked flask. After cooling in an ice bath until the internal temperature reached 0°C, 60 g of ethoxymethimine hydrochloride was added. After stirring for 1 h, the pH was adjusted to 3-4 with hydrochloric acid, and evaporated to dryness under reduced pressure to obtain a white solid. Add ethanol to dissolve, and filter with suction to remove insoluble matter. The filtrate was evaporated to dryness to obtain a pale yellow oil. Add ethanol to dissolve activated carbon for decolorization, slowly cool and crystallize to obtain 11.6 g of light yellow solid.

[0029] 2. Preparation of dihydro-6-mercapto-5H-pyrazol[1,2-α][1,2,4]triazole ylide chloride (me...

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PUM

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Abstract

The invention discloses a preparation process of biapenem. The preparation process of the biapenem comprises the following steps: preparing bis(6,7-dihydro-5H-pyrazolyl-[1,2-alpha][1,2,4]-triazolyl ylide-6-yl) disulfide dichloride; preparing dihydro-6-mercapto-5H-pyrazolyl[1,2-alpha][1,2,4]-triazolium chloride; preparing (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-alpha][1,2,4]triazolyl-6-yl)sulfenyl-6-[(R)-1-hydroxyethyl]-1-methyl-carbapenem-2-ene-3-p-nitrobenzyl carboxylate chloride; preparing the biapenem; refining the biapenem. The preparation process is simple; no special equipment is required; a solvent is recyclable, so that the industrial production cost is reduced; the product yield is high.

Description

technical field [0001] The invention relates to a preparation process of biapenem. Background technique [0002] Carbapenem antibiotics are a class of broad-spectrum antibiotics developed in the 1970s. They have strong antibacterial activity and have good antibacterial effects on aerobic and anaerobic bacteria. They are stable to β-lactamase and are especially suitable for many A variety of bacteria, especially the mixed infection of aerobic bacteria and anaerobic bacteria, and it also has a killing effect on static bacteria. In addition, because this kind of drug has fewer adverse reactions, the application time is shorter, and the drug resistance has not been significantly strengthened, it is sometimes used as the last line of defense against bacteria and plays an important role in the treatment of severe hospital infections. Biapenem, the English name is "Biapenem", the chemical name is "6-[[(4R,5S,6S)-2-carboxy-6-((1R)-1-hydroxyethyl)-4-methyl -7-Oxo-1-azabicyclo[3.2.0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/06
CPCC07D519/06
Inventor 周如国
Owner ANHUI YOUCARE KAIYUE PHARMA
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