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Bergenin isopentene group derivative and preparation method and application thereof

A technique for primo-prenyl and derivatives, which is applied in the field of petrolatum prenyl derivatives and their preparation, can solve the problems of poor oral absorption, weak antiviral effect, etc., achieves enhanced lipophilicity, is beneficial to Intestinal absorption and the effect of improving curative effect

Inactive Publication Date: 2010-10-27
HENAN AGRICULTURAL UNIVERSITY
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Problems solved by technology

The present invention aims at the shortcomings of petracenin's weak antiviral effect and poor oral absorption, and provides a petracenin isopentenyl derivative, which uses petracenin as a lead compound and uses etherification reaction to seal part of the parent body. Hydroxyl makes it more lipophilic, and because it changes the oil-water partition coefficient, it is beneficial to intestinal absorption, thus improving the curative effect

Method used

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  • Bergenin isopentene group derivative and preparation method and application thereof
  • Bergenin isopentene group derivative and preparation method and application thereof
  • Bergenin isopentene group derivative and preparation method and application thereof

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Abstract

The invention relates to a bergenin isopentene group derivative and a preparation method and an application thereof. The compound has the following structural formula I or II: the synthesis method is characterized in that: lead compound bergenin has etherification with prenyl bromide in acetone to be chromatography separated by a silica gel layer to obtain the product copound. The bergenin isopentene group derivatives I and II have the function for resisting hepatitis B virus.

Description

technical field The invention belongs to the field of drug synthesis, and in particular relates to a petracenin isopentenyl derivative and a preparation method and application thereof. Background technique Bergenin (bergenin) is also known as pygmycin, phyllophyllin, saxifrage, and bergamot. It is widely distributed in many plants of Saxifragaceae and Purple Gold Bovine, and its content is relatively high. The 1990 edition of the Pharmacopoeia of the People's Republic of China recorded that petrinin is an antitussive drug for the treatment of chronic bronchitis. . In recent years, it has been reported that petracenin has anti-inflammatory, liver-protecting, anti-HIV virus and immune-enhancing effects, but modern pharmacological experiments have also shown that petracenin also has weak medicinal effects and poor oral absorption (the original form can be seen in the urine 1 hour after oral administration) Drugs), weak anti-infection ability and other shortcomings (Wang Gang ...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61K31/366A61P31/20A61P1/16
Inventor 申进文麻兵继阮元余海尤
Owner HENAN AGRICULTURAL UNIVERSITY
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