Method for preparing biapenem by using micro-reaction technology

A biapenem and micro-reaction technology, which is applied in the field of preparing biapenem by using micro-reaction technology, can solve the problems of many by-products, low yield, long reaction time, etc., to prevent side reactions, increase specific surface area, The effect of reducing the amount of solvent used

Inactive Publication Date: 2014-06-18
周小明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] The purpose of the present invention is to provide a method for preparing biapenem using micro-reaction technology to solve the problems of long reaction time, many by-products and low yield

Method used

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  • Method for preparing biapenem by using micro-reaction technology
  • Method for preparing biapenem by using micro-reaction technology
  • Method for preparing biapenem by using micro-reaction technology

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Synthesis of (4R, 5S, 6S)-3-[(6,7-dihydro-5H-pyrazol[1,2-a][1,2,4]triazolium-6-yl by microreaction technique )]-thio-6-[(R)-1-hydroxyethyl]-4-methylcarbapenicill-2-ene-2-p-nitrophenyl ester (1)

[0044] This reaction was carried out using a microchannel reaction system (FRX 100, Syrris). The first reserve part of the reaction system is loaded with 4.88g (8.0mmol) (4R, 5S, 6S)-3-diphenylphosphate oxy-6-[(R)-1-hydroxyethyl]-4-methyl carbon Penicillium-2-ene-2-p-nitrophenyl ester (2) and 30ml of anhydrous acetonitrile and slightly heated compound (4R, 5S, 6S)-3-diphenylphosphate oxy-6-[(R)- 1-Hydroxyethyl]-4-methylcarbapillin-2-en-2-p-nitrophenyl ester (2) was dissolved. The second storage portion of the reaction system was charged with 1.14 g (8.0 mmol) of 6-mercapto-(6,7-dihydro-5H-pyrazol[1,2-a][1,2,4]triazole ylide ( 3), 1.2ml (8.8mmol) diisopropylethylamine and 30ml anhydrous acetonitrile make it dissolve.Microchannel mixing part is the volume of reaction part is 1...

Embodiment 2

[0046] Synthesis of (4R, 5S, 6S)-3-[(6,7-dihydro-5H-pyrazol[1,2-a][1,2,4]triazolium-6-yl by microreaction technique )]-thio-6-[(R)-1-hydroxyethyl]-4-methylcarbapenicill-2-ene-2-p-nitrophenyl ester (1)

[0047] This reaction was carried out using a microchannel reaction system (FRX 100, Syrris). The first reserve part of the reaction system is loaded with 4.88g (8.0mmol) (4R, 5S, 6S)-3-diphenylphosphate oxy-6-[(R)-1-hydroxyethyl]-4-methyl carbon Penicillium-2-ene-2-p-nitrophenyl ester (2) and 30ml of anhydrous acetonitrile and slightly heated compound (4R, 5S, 6S)-3-diphenylphosphate oxy-6-[(R)- 1-Hydroxyethyl]-4-methylcarbapillin-2-en-2-p-nitrophenyl ester (2) was dissolved. The second storage portion of the reaction system was charged with 1.14 g (8.0 mmol) of 6-mercapto-(6,7-dihydro-5H-pyrazol[1,2-a][1,2,4]triazole ylide ( 3), 1.2ml (8.8mmol) diisopropylethylamine and 30ml anhydrous acetonitrile make it dissolve.Microchannel mixing part is the volume of reaction part is 1...

Embodiment 3

[0049] Synthesis of (4R, 5S, 6S)-3-[(6,7-dihydro-5H-pyrazol[1,2-a][1,2,4]triazolium-6-yl by microreaction technique )]-thio-6-[(R)-1-hydroxyethyl]-4-methylcarbapenicill-2-ene-2-p-nitrophenyl ester (1)

[0050] This reaction was carried out using a microchannel reaction system (FRX 100, Syrris). The first reserve part of the reaction system is loaded with 4.88g (8.0mmol) (4R, 5S, 6S)-3-diphenylphosphate oxy-6-[(R)-1-hydroxyethyl]-4-methyl carbon Penicillium-2-ene-2-p-nitrophenyl ester (2) and 30ml of anhydrous acetonitrile and slightly heated compound (4R, 5S, 6S)-3-diphenylphosphate oxy-6-[(R)- 1-Hydroxyethyl]-4-methylcarbapillin-2-en-2-p-nitrophenyl ester (2) was dissolved. The second storage portion of the reaction system was charged with 1.14 g (8.0 mmol) of 6-mercapto-(6,7-dihydro-5H-pyrazol[1,2-a][1,2,4]triazole ylide ( 3), 1.2ml (8.8mmol) diisopropylethylamine and 30ml anhydrous acetonitrile make it dissolve.Microchannel mixing part is the volume of reaction part is 1...

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Abstract

The present invention provides a method for preparing biapenem by using a micro-reaction technology. The method is characterized in that: the preparation process is performed in a micro-reactor. During the development process of the micro-reaction technology, positive input and accelerating research of the industry provide important effects. The micro-reaction technology is a new technology field, which meets the industry requirements of green chemistry, energy saving and emission reduction, low cost and high efficiency, and the social development requirements. The micro-reaction technology focusedly studies a modern manufacturing technology of the micro-reactor, micro heat transfer characteristics of the micro-reactor, micro extraction characteristics of the micro-reactor, transfer and reaction characteristics of a multiphase system in the micro-reactor, an application of the traditional chemical reaction in the micro-reactor, and the micro-reaction technology conversion of the projects with the hazardous or bad conditions, wherein the micro-reaction technology conversion of the projects can not be achieved by using the traditional chemical engineering technology.

Description

technical field [0001] The invention relates to the field of medicine preparation, and in particular provides a method for preparing biapenem by using micro-reaction technology. Background technique [0002] Biapenem (Biapenem) is a 1β-methylcarbapenem antibiotic for injection developed by Lederle Company of Japan and Cyanoamide Company of the United States. It was approved for marketing in Japan in March 2002 and is currently undergoing Phase II clinical trials in the United States. test. Like meropenem, biapenem has the characteristics of broad antibacterial spectrum and strong antibacterial activity. Biapenem has strong antibacterial activity against Gram-positive bacteria, Gram-negative bacteria (including drug-resistant Pseudomonas aeruginosa), anaerobic bacteria, etc.; it is stable to β-lactamase; it is stable to DHP-1 Stronger than imipenem. Compared with other carbapenems on the market, biapenem has almost zero nephrotoxicity, can be administered alone, has no cen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D519/06
Inventor 周小明邵英禄沈柳兰闫庆礼王艳
Owner 周小明
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