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Process for purifying satraplatin

A purification method, the technology of Scitraplatin, which is applied in the field of purification of the anti-tumor drug Scitraplatin, can solve the problems of easy introduction of impurities, long synthesis route, and impact on product quality, etc.

Inactive Publication Date: 2006-08-16
KUNMING INST OF PRECIOUS METALS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] It can be seen from the preparation route of Saite Platinum that due to the long synthesis route, many intermediate links and intermediate raw materials used, impurities are easily introduced into the product, which affects the quality of the product.

Method used

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  • Process for purifying satraplatin
  • Process for purifying satraplatin
  • Process for purifying satraplatin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Dissolve 10 grams of the crude product containing 70% of Saite Platinum in 95ml of DMF / hydrochloric acid solution at 50°C, the volume ratio of N-N dimethylformamide:hydrochloric acid solution=5:1, and the concentration of the used hydrochloric acid solution is 0.5mol / L , glass sand funnel to filter twice, add 800ml of acid aqueous solution at 7°C to the mother liquor for reverse analysis, the concentration of hydrochloric acid aqueous solution used for reverse analysis is 0.3mol / L, let it stand for 2.5 hours, filter the separated precipitate, wash with water and ethanol three times respectively , and dried to obtain 4.5 g, the yield was 64%. After high-performance liquid chromatography analysis, the content of Saite platinum is 98.7%.

Embodiment 2

[0026] 10 grams of the crude product containing 83% of Saite Platinum was dissolved in 90ml DMF / hydrochloric acid aqueous solution at 70°C, N-N dimethylformamide:hydrochloric acid aqueous solution volume ratio=1:1, the concentration of the used hydrochloric acid aqueous solution was 1mol / L, glass Filter through sand funnel twice, add 850ml of hydrochloric acid aqueous solution at 10°C to the mother liquor for reverse analysis, the concentration of hydrochloric acid aqueous solution used for reverse analysis is 1mol / L, let it stand for 3 hours, filter the separated precipitate, wash with water and ethanol three times respectively, and dry Obtain 5.5 grams, productive rate is 66%, through high performance liquid chromatography analysis, content is 99.0%

Embodiment 3

[0028] Dissolve 10 grams of the crude product containing 91% of Saite Platinum in 85ml of DMF / hydrochloric acid solution at 100°C, the volume ratio of N-N dimethylformamide:hydrochloric acid solution=1:1, and the concentration of the used hydrochloric acid solution is 0.01mol / L . Filter twice with a glass sand funnel, add 900ml of hydrochloric acid aqueous solution at 5°C to the mother liquor for reverse analysis, the concentration of the aqueous hydrochloric acid solution used for reverse analysis is 0.01mol / L, let it stand for 2 hours, filter the separated precipitate, wash with water and ethanol three times respectively, and dry 6.1 g, 68% yield. After high performance liquid chromatography analysis, the content is 99.5%.

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Abstract

The technological process of purifying antitumor medicine Satraplatin includes dissolving coarse Satraplatin material in mixed water solution of N, N-dimethyl methane amide and hydrochloric acid, filtering, adding proper amount of water solution of hydrochloric acid into the filtrate for reverse separation to obtain pure Satraplatin product. The said purification process can purifying coarse Satraplatin material of 700-95 % content to refined Satraplatin product with 98 % over content.

Description

technical field [0001] The invention relates to a method for purifying antineoplastic drug Satraplatin. Background technique [0002] Satraplatin (English name Satraplatin, referred to as JM216) is a new type of platinum group metal anti-tumor drug, and its chemical structure is as follows: [0003] [0004] It is the first platinum-group metal anticancer drug to enter clinical trials with oral administration, and there is no cross-resistance or low cross-resistance with cisplatin and carboplatin. At present, in Europe, America and Japan, Scitraplatin has entered the phase III clinical trial stage, mainly used for the treatment of hormone-resistant prostate cancer, and also effective for ovarian cancer, small cell lung cancer, etc., and is expected to be approved for use in the near future in the clinic. [0005] The synthesis of Saiteplatin is extremely difficult, and its preparation process uses cisplatin as the starting material, including multi-step chemical reactio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00
Inventor 普绍平余尧高文桂刘祝东金毅
Owner KUNMING INST OF PRECIOUS METALS
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