A kind of method of high-speed countercurrent chromatographic separation of cis-trans isomers of sertraline hydrochloride

A technology of high-speed countercurrent chromatography and sertraline hydrochloride, which is applied in the field of high-speed countercurrent chromatography separation, can solve the problem of high cost, and achieve the effects of mild conditions, high economic benefits, and large separation and preparation volume.

Active Publication Date: 2021-12-07
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the above separation techniques are mainly used for the analysis of sertraline isomers, and there are certain limitations in the preparative separation process, and the cost is very high

Method used

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  • A kind of method of high-speed countercurrent chromatographic separation of cis-trans isomers of sertraline hydrochloride
  • A kind of method of high-speed countercurrent chromatographic separation of cis-trans isomers of sertraline hydrochloride
  • A kind of method of high-speed countercurrent chromatographic separation of cis-trans isomers of sertraline hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) Mix 93.65ml 0.10mol / L citric acid aqueous solution with 6.35ml 0.20mol / L disodium hydrogen phosphate aqueous solution to obtain a citric acid-disodium hydrogen phosphate buffer solution with pH=7.6, then add 15.07g hydroxypropyl-β - Cyclodextrin is mixed to obtain a citric acid-disodium hydrogen phosphate buffer solution containing hydroxypropyl-β-cyclodextrin, wherein the concentration of hydroxypropyl-β-cyclodextrin is 0.10mol / L;

[0036] Then mix n-hexane with citric acid-disodium hydrogen phosphate buffer solution containing hydroxypropyl-β-cyclodextrin according to the volume ratio of 1:1 and place them in a separatory funnel, shake well, let stand to separate layers, and wait for equilibrium After separation, the obtained organic phase was used as the stationary phase, and the aqueous phase was used as the mobile phase.

[0037] (2) Weigh 2 mg of racemic sertraline hydrochloride (mainly cis-sertraline hydrochloride, synthetic method references: Peng Dongming, ...

Embodiment 2

[0043](1) Mix 95.75ml 0.10mol / L citric acid aqueous solution with 4.25ml 0.20mol / L disodium hydrogen phosphate aqueous solution to obtain pH=7.8 citric acid-disodium hydrogen phosphate buffer solution, then add 15.07g hydroxypropyl-β- The cyclodextrins are mixed to obtain a citric acid-disodium hydrogen phosphate buffer solution containing hydroxypropyl-β-cyclodextrin, wherein the concentration of hydroxypropyl-β-cyclodextrin is 0.10mol / L;

[0044] Then mix n-hexane with citric acid-disodium hydrogen phosphate buffer solution containing hydroxypropyl-β-cyclodextrin according to the volume ratio of 1:1 and place them in a separatory funnel, shake well, let stand to separate layers, and wait for equilibrium After separation, the obtained organic phase was used as the stationary phase, and the aqueous phase was used as the mobile phase.

[0045] (2) Weigh 2 mg of racemic sertraline hydrochloride and dissolve it in 1 ml of water phase, fully dissolve to make a sample solution for ...

Embodiment 3

[0051] (1) Mix 93.65ml 0.10mol / L citric acid aqueous solution with 6.35ml 0.20mol / L disodium hydrogen phosphate aqueous solution to obtain a citric acid-disodium hydrogen phosphate buffer solution with pH=7.6, then add 15.07g hydroxypropyl-β- The cyclodextrins are mixed to obtain a citric acid-disodium hydrogen phosphate buffer solution containing hydroxypropyl-β-cyclodextrin, wherein the concentration of hydroxypropyl-β-cyclodextrin is 0.10mol / L;

[0052] Then mix n-hexane with citric acid-disodium hydrogen phosphate buffer solution containing hydroxypropyl-β-cyclodextrin according to the volume ratio of 1:1 and place them in a separatory funnel, shake well, let stand to separate layers, and wait for equilibrium After separation, the obtained organic phase was used as the stationary phase, and the aqueous phase was used as the mobile phase.

[0053] (2) Weigh 4 mg of racemic sertraline hydrochloride and dissolve it in 1 ml of water phase, fully dissolve to make a sample solut...

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Abstract

The invention discloses a method for separating cis-trans isomers of sertraline hydrochloride by using high-efficiency countercurrent chromatography. The specific method is: firstly, an organic solvent is mixed with citric acid-disodium hydrogen phosphate containing hydroxypropyl-β-cyclodextrin The buffer solution is mixed at a volume ratio of 1:0.5 to 10 to form a solvent system, and the organic phase is used as a stationary phase, and the aqueous phase is used as a mobile phase, and then separated by countercurrent chromatography to obtain cis-sertraline hydrochloride and trans-hydrochloride Sertraline. The conditions of the separation and purification process are mild, the separation process is efficient and convenient, the separation and preparation amount is large, and the separation degree is high, and the purity of the cis-sertraline and trans-sertraline obtained after purification are both greater than 98%.

Description

technical field [0001] The invention relates to a high-speed countercurrent chromatographic separation method, in particular to a high-speed countercurrent chromatographic separation method for cis-trans isomers of sertraline hydrochloride. Background technique [0002] Sertraline hydrochloride is a selective serotonin reuptake inhibitor, which has been widely used in the treatment of depression and obsessive-compulsive disorder. It can help improve the body's ability and effectively relieve the patient's depressive symptoms. Sertraline hydrochloride will form cis- and trans-isomers during the synthesis process. There are two chiral centers in its molecular structure, and there are two pairs of enantiomers (cis-1S, 4S and cis-1R, 4R and trans-1S, 4R and trans-1R, 4S), the specific structural formula is as follows: [0003] [0004] Among them, sertraline hydrochloride (1S, 4S) with medicinal value exists in the cis isomer, therefore, in order to ensure the effectiveness ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C209/88C07C211/42
CPCC07B2200/07C07C209/88C07C211/42
Inventor 童胜强孙文宇颜继忠
Owner ZHEJIANG UNIV OF TECH
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