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Reagent and method for resolution of ofloxacin racemate

A technology of ofloxacin and ‐ofloxacin, applied in the field of chiral pharmaceutical chemical separation, can solve the problems of difficulty in the resolution of ofloxacin racemates, unfavorable industrial applications, etc., and reduce the need for resolution The effects of reagents, improved efficiency, and simple operation process

Active Publication Date: 2016-03-30
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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  • Reagent and method for resolution of ofloxacin racemate
  • Reagent and method for resolution of ofloxacin racemate
  • Reagent and method for resolution of ofloxacin racemate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

Embodiment 2

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

Embodiment 3

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

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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 medicines, in particular to a reagent and method for resolving racemates of ofloxacin. Background technique [0002] Ofloxacin racemate is a broad-spectrum antibacterial fluoroquinolone. Ofloxacin racemate is easy to absorb when taken orally, and its mechanism of action is to inhibit bacterial DNA gyrase, and its clinical application has remarkable curative effect. L-ofloxacin is one of the chiral isomers of the racemate of ofloxacin. L-ofloxacin has more advantages than ofloxacin racemate, its antibacterial activity is 2 times of ofloxacin racemate, water solubility is 8 times of ofloxacin racemate, its Less toxic and side effects. [0003] The separation factor of enantiomers is an important factor to investigate the effect of chiral resolution. It is defined as the ratio of the distribution coefficients of two isomers. Generally speaking, when the separation factor is 1, it means that the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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