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Method for producing arbekacin by one-pot continuous flow

A technology of arbekacin and dibekacin, which is applied in the field of preparation of arbekacin, can solve the problems of large waste liquid discharge, need for more labor, and long process, so as to simplify operation, reduce cost, and reduce production cost effect

Active Publication Date: 2019-05-07
山东安信制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, arbekacin can be further prepared by a continuous flow process in one device, which can well solve the problems of cumbersome operation in traditional multi-step chemical synthesis, long process, need for more labor, and large amount of waste liquid discharge.

Method used

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  • Method for producing arbekacin by one-pot continuous flow
  • Method for producing arbekacin by one-pot continuous flow
  • Method for producing arbekacin by one-pot continuous flow

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Add 3.2L acetone in the 5L single-necked bottle that 1mol dibekacin silylate is housed, stir until the material liquid dissolves clear, add 370g active thioester and 2.2L acetone in another single-necked bottle, stir until dissolved clear, Bekacin silyl compound flows in the microreactor A unit with the flow velocity of 100ml / min, and active thioester flows in the microreactor A unit with the flow velocity of 77ml / min simultaneously, and the residence time of this reaction is 22.4 seconds, and the reaction temperature control at 15°C.

[0037] After the reaction solution flows out of the microreactor A unit, simultaneously the dilute hydrochloric acid with a concentration of 18% flows into the microreactor B unit at a flow rate of 20ml / min. The residence time of the reaction is 19.0 seconds, and the reaction temperature is controlled at 15°C .

[0038] After the feed liquid flows out from the microreactor, it is added to the resin column for adsorption. After the adsor...

Embodiment 2

[0040] Add 3.2L acetone in the 5L single-necked bottle that 1mol dibekacin silylate is housed, stir until the feed solution dissolves clear, add 370g active thioester and 2.5L acetone in another single-necked bottle, stir until dissolved, Bekacin silyl compound flows in the microreactor A unit with the flow velocity of 100ml / min, and active thioester flows in the microreactor A unit with the flow velocity of 87ml / min simultaneously, and the residence time of this reaction is 22.0 seconds, and the reaction temperature control at 15°C.

[0041] After the reaction solution flows out of the microreactor A unit, dilute hydrochloric acid flows into the microreactor B unit together at a flow rate of 20ml / min. The residence time of the reaction is 19.0 seconds, and the reaction temperature is controlled at 15°C.

[0042]After the feed liquid flows out from the microreactor, it is added to the resin column for adsorption. After the adsorption is completed, it is eluted sequentially wit...

Embodiment 3

[0044] Add 3.2L acetone in the 5L single-necked bottle that 1mol dibekacin silylate is housed, stir until the material liquid dissolves clear, add 370g active thioester and 2.2L acetone in another single-necked bottle, stir until dissolved clear, Bekacin silyl compound flows in the microreactor A unit with the flow velocity of 100ml / min, and active thioester flows in the microreactor A unit with the flow velocity of 77ml / min simultaneously, and the residence time of this reaction is 22.4 seconds, and the reaction temperature control at 15°C.

[0045] After the reaction solution flows out of the microreactor A unit, dilute hydrochloric acid flows into the microreactor B unit together at a flow rate of 25ml / min. The residence time of the reaction is 18.0 seconds, and the reaction temperature is controlled at 15°C.

[0046] After the feed liquid flows out from the microreactor, it is added to the resin column for adsorption. After the adsorption is completed, it is eluted sequent...

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Abstract

The invention provides a method for producing arbekacin through one-pot process continuous flow. The method is characterized in that a silanization product of dibekacin and active thioester undergo a reaction in a microreactor as initial raw materials. The combination of the active thioester and the advantage of the high selectivity of a microchannel reactor reduces a hydrazine hydrolysis process, improves the selectivity of the reaction, improves the product conversion rate to 70% or above, greatly reduces the difficulty of subsequent purification and separation and reduces the discharge of waste liquids and waste residues. The method for producing arbekacin through continuous flow technology one-pot process well solves the problems of tedious operation, long technologic process, much labor and large waste liquid discharge volume in traditional multi-step chemical synthesis.

Description

technical field [0001] The invention relates to a method for preparing arbekacin by using a microreactor one-pot continuous flow method, which belongs to the technical field of medicine. Background technique [0002] Since Waksman et al. discovered streptomycin produced by Streptomyces in 1944, there have been more than 3,000 natural and semi-synthetic aminoglycoside antibiotics reported, including nearly 200 natural aminoglycoside antibiotics produced by microorganisms. Aminoglycoside antibiotics have the structure of aminosugar and aminocyclic alcohol, which are composed of aminosugar molecules and aglycones in non-sugar parts. They are clinically important broad-spectrum anti-infective drugs with strong antibacterial ability and antibacterial spectrum Broad, stable chemical properties, easy absorption and metabolism; these antibiotics also have common characteristics in terms of antibacterial spectrum, antibacterial mechanism, serum protein binding rate, gastrointestinal ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H15/234C07H1/00
CPCC07H1/00C07H15/234
Inventor 常宝磊李德才陈中南周先国杨庆坤吴柯
Owner 山东安信制药有限公司