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Guaiac orchid hydrocarbon azulene ramification and preparing method and application thereof

A technology for guaiazulene and derivatives, applied in the field of guaiazulene derivatives and their preparation and application, capable of solving problems such as compound performance change and loss

Inactive Publication Date: 2014-08-27
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, since the performance of the compound is affected by many factors, such as the steric effect and electronic effect of the substituent group, hydrophilicity or hydrophobicity, etc., any modification of the compound structure may lead to the change or loss of the compound performance, and it is not arbitrary. Chuanglan azulene derivatives can exert excellent pharmacodynamic activity

Method used

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  • Guaiac orchid hydrocarbon azulene ramification and preparing method and application thereof
  • Guaiac orchid hydrocarbon azulene ramification and preparing method and application thereof
  • Guaiac orchid hydrocarbon azulene ramification and preparing method and application thereof

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Embodiment 1

[0047] Among them, the preparation method of starting compound A can be found in Chinese patent application: 201310127788.8. The synthesis of embodiment 1 compound B1~B8

[0048] Add 10mL of isopropanol to a 25mL flask, then dropwise add 10 drops of dilute hydrochloric acid, then add 0.4g of paraformaldehyde, then add 0.2g of compound A, add 4mL of acetone, and fully Stir, keep the temperature at 45°C, and reflux with a condenser tube. The reaction time is 48h. Cool down after stopping heating, add water corresponding to its volume into the reaction flask, extract with ethyl acetate and spin dry, the crude product is purified by column chromatography, and dried under reduced pressure to obtain compound B1.

[0049] Refer to the preparation method of compound B1, change the reaction raw material compound B to obtain compounds B2-B8, and the detection data of each compound are as follows:

[0050] B1:

[0051] Purple crystal, yield 39.0%, m.p.57-58°C; IR (KBr): 3449, 2960, 292...

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Abstract

The invention provides guaiac orchid hydrocarbon azulene ramification shown in the formula I in the specification or a salt or pro-drug accepted in the pharmaceutical science. R represents C1-C4 alkyl group, phenyl group or substituent phenyl group. The substituent group of the substituent phenyl group is selected from C1-C4 alkyl group, halogen or C1-C4 alkoxy. As shown in the research, the compound has a certain anti-peptic ulcer activity, the activity of the compound B2 and B8 is superior, the anti-gastric ulcer function of the compound B2 and B8 is equal to or close to that of the typical medicine of omeprazole, and a new choice is provided for clinical medication.

Description

technical field [0001] The invention relates to a guaiazulene derivative, a preparation method and an application thereof. Background technique [0002] Guaiazulene, namely 1,4-dimethyl-7-isopropyl azulene, is an active ingredient of the plant chamomile, and its structural formula is as follows: [0003] [0004] The compound has strong effects of anti-pepsin, anti-inflammation, anti-allergic, and promoting mucosal metabolism, and many derivatives thereof have shown good biological activities. Compound guaiazulene ointment (Shanxi Tongsheng Pharmaceutical Co., Ltd.) can be used for burns, scalds, burns, frostbite, chapped, decubitus, radiation heat protection, dermatitis, etc. Sodium azulene sulfonate is a water-soluble derivative of guaiazulene, which has good anti-inflammatory and wound-healing properties, and is also the main component of glutamine granules, a drug currently on the market for treating gastric ulcers. In this drug, sodium azulene sulfonate acts direct...

Claims

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Application Information

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IPC IPC(8): C07D295/16A61K31/495A61P1/04
CPCC07D295/16
Inventor 尹述凡袁明兴蒋丽娟袁丽黎勇张晓伟张晓双李阳董林李颖
Owner SICHUAN UNIV
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