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Preparation method of beta-patchoulene, medicinal composition and application thereof

A technology of patchoulene and composition, which is applied in the field of preparation of β-patchoulene, can solve the problems such as difficult preparation of β-patchoulene, and achieve the effects of increasing application, promoting industry, and high purity

Inactive Publication Date: 2017-08-08
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The object of the present invention is to provide a kind of β-patchoulene and its preparation method, pharmaceutical composition and application, which aims to improve the problem that the existing β-patchoulene is not easy to prepare

Method used

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  • Preparation method of beta-patchoulene, medicinal composition and application thereof
  • Preparation method of beta-patchoulene, medicinal composition and application thereof
  • Preparation method of beta-patchoulene, medicinal composition and application thereof

Examples

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preparation example Construction

[0036] A preparation method of β-patchoulene, which comprises the steps of reacting patchouli alcohol and acid in an organic solvent, extracting the reaction product with a non-polar solvent, and then separating the extract with a chromatographic column.

[0037] The present invention adopts synthetic method to synthesize β-patchoulene from patchouli alcohol, and the reaction structural formula and mechanism are as follows:

[0038]

[0039] Using acid as a catalyst, the patchouli alcohol undergoes a dehydration reaction to obtain a high yield of β-patchoulene, which is as high as 80% through the inventor's detection of the experimental results. After the reaction is complete, the reaction product is extracted with a non-polar solvent. In a preferred embodiment of the present invention, the reaction product is subjected to multiple extractions, and the extracts from multiple extractions are combined and then concentrated. After concentration, the product β-patchoulene was ...

Embodiment 1

[0065] The present embodiment provides a kind of β-patchoulene, which is mainly prepared by the following steps:

[0066] Place the container containing dilute hydrochloric acid on a shaker, vibrate at 37°C and 120rpm, add patchouli alcohol-ethanol solution to the container, the ratio of patchouli alcohol to ethanol is 1mg / mL; the volume of dilute hydrochloric acid The fraction is 10%; the volume ratio of dilute hydrochloric acid to patchouli alcohol-ethanol solution is: 3:2. After the reaction was complete, the reaction product was extracted twice with an equal volume of n-hexane, the extracts were combined, and concentrated by rotary evaporation to obtain a mixture.

[0067] The mixture was separated by 200-mesh silica gel column chromatography and 200-mesh neutral alumina column chromatography, eluted with n-hexane, and the eluents were combined and concentrated by rotary evaporation.

Embodiment 2

[0069] The present embodiment provides a kind of β-patchoulene, which is mainly prepared by the following steps:

[0070] Place the container containing dilute hydrochloric acid on a shaker, vibrate at 35°C and 220rpm, add patchouli alcohol and methanol solution to the container, the ratio of patchouli alcohol to methanol is 6mg / mL; the volume of dilute hydrochloric acid The fraction is 8%; the volume ratio of dilute hydrochloric acid to patchouli alcohol-methanol solution is: 1:1. After the reaction was complete, the reaction product was extracted three times with an equal volume of petroleum ether, and the extracts were combined and concentrated by rotary evaporation to obtain a mixture.

[0071] The mixture was separated by 300-mesh silica gel column chromatography and 300-mesh neutral alumina column chromatography, eluted with n-hexane, and the eluents were combined and concentrated by rotary evaporation.

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Abstract

The invention relates to the field of biological medicines, particularly relates to a preparation method of beta-patchoulene, a medicinal composition and application thereof. The preparation method of the beta-patchoulene comprises the following steps: performing a reaction on patchouli alcohol and acid in an organic solvent, extracting a reaction product by using a non-polar solvent, and then separating an extract by using a chromatographic column. Through a dehydration reaction on the patchouli alcohol and hydrochloric acid, the beta-patchoulene is prepared, and by the preparation method, the yield is as high as 80%, the product is easily separated, and the prepared beta-patchoulene is high in purity; when the patchouli alcohol is used as a raw material for preparing the patchoulene, the raw material is easy to obtain, processes during preparation are reduced, and the application of the patchoulene is widened; in addition, the beta-patchoulene is applied to medicines for preventing and / or treating acute gastric ulcer, so that novel application of the beta-patchoulene is achieved, and industrialization and commercialization of the beta-patchoulene are promoted.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a preparation method, pharmaceutical composition and application of β-patchoulene. Background technique [0002] β-patchoulene, one of the natural sesquiterpene components present in patchouli, has the molecular formula C 15 h 24 , the molecular weight is 204.36. Appearance is light yellow oily liquid, insoluble in water, easily soluble in common organic solvents such as ethanol and petroleum ether. Currently, researchers have done very little research on patchoulene. The inventors found that β-patchoulene can be extracted and separated from patchouli oil by rectification-column chromatography, but the content of β-patchoulene in the raw material of patchouli oil varies depending on the place of origin , and the content is low, only β-patchoulene is obtained from patchouli oil, and the application of β-patchoulene is not used. Contents of the invention [0003] The object of the...

Claims

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Application Information

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IPC IPC(8): C07C1/24C07C7/00C07C7/10C07C13/605A61K31/015A61P1/04
CPCA61K31/015A61P1/04
Inventor 苏子仁黎玉翠刘煜洪陈建南赖小平
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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