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Novel method for synthesizing antineoplastic medicament nedaplatin

An anti-tumor drug, nedaplatin technology, applied in the direction of anti-tumor drugs, drug combinations, chemical instruments and methods, etc., can solve the problems of complex operation, long reaction process, low production cost, etc.

Inactive Publication Date: 2009-07-08
KUNMING GUIYAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] The above synthetic methods of nedaplatin all have long reaction process and disadvantages such as complicated operation, so it is necessary to develop a method for preparing nedaplatin with short reaction cycle, low production cost and high yield.

Method used

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  • Novel method for synthesizing antineoplastic medicament nedaplatin
  • Novel method for synthesizing antineoplastic medicament nedaplatin
  • Novel method for synthesizing antineoplastic medicament nedaplatin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 4.2 grams of glycolic acid, 2.2 grams of sodium hydroxide, mixed and stirred after water-soluble, adjust the pH value to 7 with glycolic acid or sodium hydroxide, add 9.4 grams of silver nitrate solution, stir to form a white precipitate, filter, wash (water 2 times, 1 time of absolute ethanol), dried at 60° C., and weighed to obtain 8.4 grams of silver glycolate, with a yield of 83.67%, and a silver content of 58.64% (theoretical value 59.01%).

[0034] Add 10 grams of iodoplatinum, add appropriate amount of deionized water (about 300ml), stir evenly and heat up to 60°C, slowly add 7.5g of silver glycolate, stir and react in the dark for 3 hours, filter to remove AgI, heat the filtrate to 50°C, stir and Slowly add sodium hydroxide dropwise to adjust and keep the pH value at about 7, avoid light and react for 5 hours, transfer the reaction solution to a rotary evaporator and concentrate under reduced pressure to 1 / 8 of the original volume, solids are precipitated, taken ...

Embodiment 2

[0041] 4.2 grams of glycolic acid, 2.2 grams of sodium hydroxide, mixed and stirred after water dissolving, adjusted the pH value to 7 with glycolic acid or sodium hydroxide, added 9.4 grams of silver nitrate solution, stirred to form a white precipitate, filtered, washed (water 2 times, 1 time of absolute ethanol), dried at 50° C., and weighed to obtain 8.2 grams of silver glycolate, with a yield of 81.09%, and a silver content of 58.75% (theoretical value 59.01%).

[0042] Add 10 grams of platinum iodide, add an appropriate amount of deionized water (about 300ml), stir evenly and heat up to 60°C, slowly add 7.5 grams of silver glycolate, stir and react in the dark for 3 hours, filter out AgI, wash AgI twice, combine the filtrate and Wash with water, about 430ml in total, heat to 55°C, stir and slowly add sodium hydroxide dropwise to adjust and keep the pH value at about 7, keep the reaction in the dark for 5.5 hours, transfer the reaction solution to a rotary evaporator and c...

Embodiment 3

[0049] 4.2 grams of glycolic acid, 2.2 grams of sodium hydroxide, mix and stir after water-soluble, adjust the pH value to 8 with glycolic acid or sodium hydroxide, add a solution of 9.5 grams of silver nitrate, stir to form a white precipitate, filter, wash (water 2 times, 1 time of absolute ethanol), dried at 60° C., and weighed to obtain 4.2 grams of silver glycolate, with a yield of 83.06%, and a silver content of 58.82% (theoretical value 59.01%).

[0050] Add 10 grams of platinum iodide, add an appropriate amount of deionized water (about 300ml), stir evenly and heat up to 60°C, slowly add 7.5 grams of silver glycolate, stir and react in the dark for 3 hours, filter out AgI, wash AgI twice, combine the filtrate and Wash with water, about 420ml in total, heat to 60°C, stir and slowly add sodium hydroxide dropwise to adjust and keep the pH value at about 7, keep the reaction in the dark for 7 hours, transfer the reaction solution to a rotary evaporator and concentrate under...

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Abstract

The invention relates to a method for preparing an antitumor drug of nedaplatin C2H8N2O3Pt. The method comprises that: a reactant of cis-diiododiammineplatinum(II) is added with a proper amount of water, uniformly stirred, added with silver glycollate C2H3O3Ag slowly according to a molar ratio of Pt(NH3)2I2 to C2H3O3Ag of 1:2 for reaction at 50-60 DEG C for 2 to 3 hours; and after solid is removed, the pH value of the solution is adjusted by using NaOH to maintain about 7, the solution is heated to 50 to 60 DEG C for reaction for 6 hours totally, reaction liquid is concentrated under reduced pressure and thus solid nedaplatin is obtained. The method for preparing the nedaplatin has the advantages of short technical process, high yield up to more than 60 percent and good product purity.

Description

technical field [0001] The invention relates to platinum antitumor drugs, in particular to the preparation of platinum antitumor drug nedaplatin. Background technique [0002] Nedaplatin (254-S) is the third-generation platinum-based antineoplastic drug after cisplatin and carboplatin. Its English name is Nedaplatin, and its chemical name is cis-glycolic acid-diammineplatinum (II) II)], molecular weight is 303.20, chemical structural formula: [0003] [0004] Nedaplatin was developed by Shionogi Company in Japan and was approved for marketing in Japan in June 1995. At present, this variety has been localized by Nanjing Dongjie Pharmaceutical Co., Ltd., and the product name is Jiebaishu. Nedaplatin is characterized by good water solubility (14.3g / l); small toxic and side effects, dose-limiting toxicity is bone marrow suppression, no nephrotoxicity and neurotoxicity; wide anti-cancer spectrum, effective for head and neck cancer, ovarian cancer, esophageal cancer, Bladder...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/282A61P35/00
Inventor 王庆琨普绍平丛艳伟李永年侯树谦何键刘祝东栾春芳
Owner KUNMING GUIYAN PHARMA
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