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Salt of oxodehydrocaaverine derivative

A carvinoline and dehydrogenation technology, applied in organic chemistry, antibacterial drugs, etc., can solve problems such as adverse reactions and unsatisfactory drug treatment effects, and achieve the effect of practical therapeutic activity

Inactive Publication Date: 2014-06-18
SHANGHAI YIZHI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] For now, although there are many kinds of drugs against methicillin-resistant Staphylococcus aureus, the existing drugs are likely to cause multiple and severe adverse reactions, and the therapeutic effect of the existing drugs is still not ideal.

Method used

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  • Salt of oxodehydrocaaverine derivative
  • Salt of oxodehydrocaaverine derivative
  • Salt of oxodehydrocaaverine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Oxydehydrocarbenyl fumarate

[0048] Dissolve 2.77 g (0.01 mol) of the compound oxodehydrocarbenol and 1.17 g (0.01 mol) of fumaric acid in 80 ml of boiling ethanol. The hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and stood for several hours at a temperature of 0-5°C to precipitate oxodehydrocarbenline fumarate crystals, and the oxodehydrocarbenline fumarate was filtered out. Hydrocarvinine fumarate crystals were washed with ethanol and dried under vacuum at 50°C to obtain 3.92 g of product.

Embodiment 2

[0050] Oxydehydrocarbenyl fumarate

[0051] Stir 2.77 g of the compound oxodehydrocarvinine fumarate and 1.17 g of fumaric acid in 80 ml of refluxing ethanol until all the solids are dissolved. Add activated carbon, filter the hot solution through diatomaceous earth, and cool down to room temperature while stirring. Stand for several hours in a temperature environment of 0-5°C, precipitate oxo-dehydrocarbonline fumarate crystals, filter out oxo-dehydrocarbonline fumarate crystals, wash with ethanol and dry at 50°C Drying under vacuum gave 3.91 g of product.

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Abstract

The invention relates to fumarate or pharmaceutically acceptable solvate of oxodehydrocaaverine (7-oxodehydrocavverine) and a derivative thereof, and application of oxodehydrocaaverine in preparation of a methicillin-resistant staphylococcus aureus medicine.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular to an organic acid salt of oxodehydrocaaverine (7-oxodehydrocaaverine) and its pharmaceutical application. Background technique [0002] For now, although there are many kinds of drugs against methicillin-resistant Staphylococcus aureus, these existing drugs are likely to cause multiple and severe adverse reactions, and the therapeutic effect of the existing drugs is still not ideal. The patent specification of Chinese invention patent application publication number CN 1 01822675A describes some active compounds with resistance to methicillin-resistant Staphylococcus aureus. Contents of the invention [0003] The present invention discloses some new compounds, preparation methods of these compounds, pharmaceutical compositions containing these compounds and pharmaceutical applications of these compounds and compositions. [0004] These compounds exhibit good water solubility...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/18A61K31/473A61P31/04
CPCC07D221/18
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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