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Celastrine grape aminomethane salt and preparation method thereof

A kind of technology of anthophyllin and meglumine, applied in the direction of steroids, chemical recovery, organic chemistry, etc., can solve problems such as affecting the stability of preparations

Inactive Publication Date: 2007-09-26
SHANGHAI HUATUO MEDICAL SCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, there are some methods that add the above-mentioned organic amine as a solubilizer in the preparation process of the preparation to make an injection or powder injection with water as the solvent. Will affect the stability of the formulation

Method used

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  • Celastrine grape aminomethane salt and preparation method thereof
  • Celastrine grape aminomethane salt and preparation method thereof
  • Celastrine grape aminomethane salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The preparation of embodiment 1 compound (I)

[0024] After dissolving 99.2mg of ceglumine in 4ml of absolute ethanol, add 41.0mg of meglumine to it, stir at room temperature 21°C for 2.5 hours, the meglumine is completely dissolved, continue to stir for 2 hours, and concentrate under reduced pressure at 40°C to Dry, crush the solid, grind it finely, add 3ml of acetone, stir for several minutes, filter with suction, wash the solid twice with acetone to obtain a reddish-brown powder, dry under reduced pressure at 40°C to obtain 98.2 mg of the product compound (I). Yield: 70.1%.

[0025] Analysis results: 1 HNMR (DMSO-d6, 300M), δ7.080 (2H, d, J=7.1Hz, H-6), 6.392 (1H, s, H-1), 6.356 (1H, d, J=7.1Hz, H -7), 3.3~3.7 (6H, multiplet, CH and CH connected to oxygen on meglumine 2 ), 2.620 (2H, d, J=4.4, -CH 2 -N), 2.293 (3H, s, CH 3 -N), 2.087 (3H, s, CH 3 -23), 1.382 (3H, s, CH 3 -25), 1.222 (3H, s, CH 3 -26), 1.080 (3H, s, CH 3 -30), 1.063 (3H, s, CH 3 -28), 0.644 ...

Embodiment 2

[0028] The preparation of embodiment 2 compound (I)

[0029] After dissolving 101.2 mg of ceglumine in 3 ml of isopropanol, add 41.8 mg of meglumine to it with stirring, raise the temperature to 30° C., and stir for 2 hours after the meglumine is completely dissolved. Concentrate under reduced pressure to dryness at 35°C, crush the solid, grind it finely, add 3ml of ethyl acetate, stir for several minutes, filter with suction, wash the solid with ethyl acetate twice to obtain a reddish-brown powder, dry under reduced pressure at 35°C, The product compound (I) 96 mg was obtained. Yield: 67.1%.

Embodiment 3

[0030] The preparation of embodiment 3 compound (I)

[0031]After dissolving 10.15 g of ceglumine in 200 ml of absolute ethanol, add 4.188 g of meglumine to it, stir at room temperature at 18° C., and stir for 3 hours after all the meglumine is dissolved. Concentrate to dryness under reduced pressure at 30°C, crush the residue, grind finely, add 300ml of ethyl acetate to dissolve, stir for 10 minutes, filter with suction, wash the solid with ethyl acetate twice to obtain a reddish-brown powder, reduce to 35°C Press and dry to obtain 10.61 g of product compound (I). Yield: 74.0%.

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Abstract

The invention discloses a celastrine glucomethylamine salt compound and preparing method with the molar rate of acid group and alkaline group at 1: 1 through ionic bond, which possesses certainly structure to be recycled by low-poison or non-poison solvent, wherein the agent pattern contains injecting agent, pill, capsule, particle and solution.

Description

technical field [0001] The present invention relates to seraphine meglumine salt and a preparation method thereof. Background technique [0002] Celastrol, also known as tripterygium, is an anticancer active ingredient present in Euonymus plants Tripterygium wilfordii and Celastrol. Document 1: Pristimerin.Spectroscopic properties of the dienone-phenol-type rearrangement products and other derivatives [KojiNakanishi, Yoshikazu Takahashi, et al.J.Org.Chem., 1965(30), 1729] Mentioned, earlier than 1960, That is to say, it has been found that this type of compound has antitumor activity, the latest literature 2: Celastrol, a Triterpene Extracted from the Chinese Thunder of God Vine Is a Potent Proteasome Inhibitor and Suppresses Human Prostate Cancer Growth in Nude Mice [Huanjie Yang, Di Chen, et al. Cancer Research, 2006 (66), 4758] confirmed that cereli is an effective proteasome inhibitor by inhibiting proteasome activity and then inducing cancer cell apoptosis. . Therefo...

Claims

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Application Information

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IPC IPC(8): C07J63/00
CPCY02P20/582
Inventor 曾佳烽潘俊芳李宝莹朱勤
Owner SHANGHAI HUATUO MEDICAL SCI CO LTD