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Salt of picrasma quassioides alkaloid derivative

A technology of alkaloids and bitter wood, which can be used in drug combinations, medical preparations containing active ingredients, organic active ingredients, etc., can solve problems such as adverse reactions, drug resistance, and unsatisfactory therapeutic effects, and achieve practical therapeutic activity. Effect

Inactive Publication Date: 2014-07-09
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 for the treatment of cancer, these existing drugs are likely to cause multiple and severe adverse reactions, and some produce drug resistance, and the therapeutic effect of the existing drugs is still not ideal.

Method used

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  • Salt of picrasma quassioides alkaloid derivative
  • Salt of picrasma quassioides alkaloid derivative
  • Salt of picrasma quassioides alkaloid derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Bitterwood alkaloid fumarate

[0048] Dissolve 2.54 g (0.01 mol) of the compound eucalyptus alkaloids and 1.17 g (0.01 mol) of fumaric acid in 77 ml of boiling ethanol. The hot solution is filtered through diatomaceous earth, then slowly cooled under gentle stirring, and left to stand for several hours at a temperature of 0-5°C to precipitate bitterwood alkaloid fumarate crystals, and filter out bitterwood alkaloid fumarate Salt crystals were washed with ethanol and dried under vacuum at 50°C to obtain 3.68 g of product.

Embodiment 2

[0050] Bitterwood alkaloid fumarate

[0051] Stir 2.54 g of fumarate and 1.17 g of fumaric acid into 77 ml of refluxing ethanol until the solids are completely dissolved. Add activated carbon, filter the hot solution through diatomaceous earth, and cool down to room temperature while stirring. Standing for several hours in a temperature environment of 0-5°C, the crystals of bitterwood alkaloid fumarate are precipitated, the crystals of bitterwood alkaloid fumarate are filtered out, washed with ethanol and dried under vacuum at 50°C to obtain 3.66 g of product.

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Abstract

The invention relates to a fumaric acid salt of picrasma quassioides alkaloid and a derivative and a pharmaceutically acceptable solvate, and an application of fumaric acid salt and the solvate in preparation of medicine for treating cancer.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to organic acid salts of eucalyptus alkaloids and their pharmaceutical applications. Background technique [0002] For now, although there are many kinds of drugs for treating cancer, these existing drugs are likely to cause multiple and severe adverse reactions, and some produce drug resistance, and the therapeutic effect of the existing drugs is still not ideal. Some active compounds for treating cancer are described in the Chinese invention patent application publication number CN102526041A. 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 stability and solid form stability. Some of these compoun...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/437A61P35/00
CPCC07D471/04
Inventor 不公告发明人
Owner SHANGHAI YIZHI MEDICAL TECH
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