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Split reagent and method for ofloxacin racemic mixture

A technology of ofloxacin and resolution reagents, which is applied in the field of chiral pharmaceutical chemical separation, can solve the problems of difficulty in resolution of racemates of ofloxacin and unfavorable industrial applications, etc., and achieve the reduction of reagents required for resolution, The effect of improving efficiency and simple operation process

Active Publication Date: 2014-03-26
CHINA CONSTR IND & ENERGY ENG GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The separation factors of various resolution methods currently used are all within 1.4, and the resolution of ofloxacin racemate is difficult, which is not conducive to industrial application

Method used

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  • Split reagent and method for ofloxacin racemic mixture
  • Split reagent and method for ofloxacin racemic mixture
  • Split reagent and method for ofloxacin racemic mixture

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Ofloxacin racemate and 1-ethyl-3-methylimidazole L-tartrate are dissolved in deionized water to form 1-ethyl-3-methylimidazole L-tartrate with a concentration of 0.05mol / L , The aqueous phase of ofloxacin racemate concentration is 1000ppm, and D-dibenzoyltartaric acid is dissolved in n-decyl alcohol to form an organic phase containing D-dibenzoyltartaric acid with a concentration of 0.2mol / L. Mix the organic phase and the water phase with a volume ratio of 1:1 and put them in a shaker, shake for 2 hours, and let stand. Take the clear liquid of the water phase to detect the concentration of L-ofloxacin and D-ofloxacin, and the separation factor Reach 3.17.

Embodiment 2

[0023] Dissolve ofloxacin racemate and 1-ethyl-3-methylimidazole L-tartrate in deionized water to form 1-ethyl-3-methylimidazole L-tartrate with a concentration of 0.5mol / L , The aqueous phase of ofloxacin racemate concentration is 1000ppm, and D-dibenzoyltartaric acid is dissolved in n-decyl alcohol to form an organic phase containing D-dibenzoyltartaric acid with a concentration of 0.2mol / L. Mix the organic phase and the water phase with a volume ratio of 1:1 and put them in a shaker, shake for 2 hours, and let stand. Take the clear liquid of the water phase to detect the concentration of L-ofloxacin and D-ofloxacin, and the separation factor Reached 1.9.

Embodiment 3

[0025] Ofloxacin racemate and 1-ethyl-3-methylimidazole L-tartrate are dissolved in deionized water to form 1-ethyl-3-methylimidazole L-tartrate with a concentration of 0.05mol / L , The aqueous phase of ofloxacin racemate concentration is 1000ppm, and D-dibenzoyltartaric acid is dissolved in n-decyl alcohol to form an organic phase containing D-dibenzoyltartaric acid with a concentration of 0.5mol / L. Mix the organic phase and the water phase with a volume ratio of 1:10 and put them in a shaker, shake for 4 hours, and let stand. Take the clear water phase to detect the concentration of L-ofloxacin and D-ofloxacin, and separate factors Reached 2.01.

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PUM

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Abstract

The invention discloses a split reagent and a split method for an ofloxacin racemic mixture. The method is as below: dissolving an ofloxacin racemic mixture and an alkyl imidazole L-tartaric acid salt ionic liquid in deionized water to form an aqueous phase, and at the same time dissolving D-dibenzoyl tartaric acid in n-decyl alcohol to form an organic phase; mixing the organic phase and the aqueous phase; oscillating the mixture in an oscillator and standing; detecting concentration of L-ofloxacin and D-ofloxacin in a clear aqueous phase; acquiring the concentration of L-ofloxacin and D-ofloxacin in organic phase respectively by the law of conservation of mass; respectively calculating the distribution coefficient of the L-ofloxacin and D-ofloxacin; and further calculating a separation factor. The reagent and the method have good separation effect, and is successfully in splitting. The invention uses alkyl imidazole L-tartaric acid salt ionic liquid and D-dibenzoyl tartaric acid for splitting of the ofloxacin racemic mixture, improves the splitting efficiency and reduces the reagents required by splitting; and the method has simple operation and high selectivity, and is suitable for industrial production.

Description

Technical field [0001] The invention relates to the chemical separation of chiral drugs, in particular to a reagent and method for the separation of ofloxacin racemate. Background technique [0002] Ofloxacin racemate is a broad-spectrum antibacterial fluoroquinolone drug. Ofloxacin racemate is easily absorbed by oral administration, and its mechanism of action is to inhibit bacterial DNA gyrase, which has significant clinical effects. L-ofloxacin is one of the chiral isomers of ofloxacin racemate. L-ofloxacin has more advantages than ofloxacin racemate. Its antibacterial activity is twice that of ofloxacin racemate, and its water solubility is 8 times that of ofloxacin racemate. Less toxic side effects. [0003] The separation factor of enantiomers is an important factor for investigating the effect of chiral resolution. It is defined as the ratio of the partition coefficients of the two isomers. Generally speaking, when the separation factor is 1, it means that the two isomers...

Claims

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Application Information

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IPC IPC(8): C07D498/06
CPCC07D498/06
Inventor 陈冬璇罗能镇张本贺相咸高何潮洪徐义明周俊超岳昌海
Owner CHINA CONSTR IND & ENERGY ENG GRP CO LTD
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