Novel method for synthesizing antineoplastic medicament carboplatin

An anti-tumor drug, carboplatin technology, applied in the direction of anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of difficult purification, long reaction process, poor product purity, etc., to achieve good product purity, easy operation, and process short effect

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

[0015] The reaction process of this method is short, can directly obtain carboplatin solid, and productive rate is better, about 75%, and shortcoming is that product purity is poor, and Ag + Generally more than 100 ppm, the purification is more difficult
[0016] The above method has shortcomings such as long reaction process or poor product purity, so it is necessary to develop a method for preparing carboplatin with short production cycle, high yield and good purity.

Method used

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  • Novel method for synthesizing antineoplastic medicament carboplatin
  • Novel method for synthesizing antineoplastic medicament carboplatin
  • Novel method for synthesizing antineoplastic medicament carboplatin

Examples

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Embodiment 1

[0033] Example 1: 3 grams of 1,1-cyclobutanedicarboxylic acid and 1.6 grams of NaOH were added with an appropriate amount of water and stirred evenly, then mixed, and the pH value was adjusted to neutral, 11.6 grams of Hg 2 (NO 3 ) 2 2H 2 O is made into a solution, and the two solutions are mixed under stirring to obtain a white product precipitate, which is filtered, washed with water and absolute ethanol, and dried to obtain Hg 2 (1,1-CBDCA)(1,1-cyclobutanedicarboxymercurous acid) 6.71 g, yield 59.3%.

[0034] 5 g Pt(NH 3 ) 2 I 2 Add an appropriate amount of water and stir evenly with 180ml of purified water, add 5.6 g of mercurous 1,1-cyclobutanedicarboxylate, react in the dark at 55°C for 8 hours, filter to remove HgI precipitate, and concentrate the resulting solution under reduced pressure to obtain a white solid. Wash with water and absolute ethanol respectively, and dry to obtain 3.31 g of carboplatin solid product with a yield of 86.15%. The structure is consis...

Embodiment 2

[0040] Example 2: 3 grams of 1,1-cyclobutanedicarboxylic acid and 1.6 grams of NaOH were added with an appropriate amount of water and stirred evenly, then mixed, and the pH value was adjusted to neutral, 11.6 grams of Hg 2 (NO 3 ) 2 2H 2 O is made into a solution, and the two solutions are mixed under stirring to obtain a white product precipitate, which is filtered, washed with water and absolute ethanol, and dried to obtain Hg 2 (1,1-CBDCA) 7.19 g, yield 61.5%.

[0041] 5 g Pt(NH 3 ) 2 I 2Add 200ml of purified water and stir evenly, add 5.6g of mercurous 1,1-cyclobutanedicarboxylate, react in the dark at 60°C for 10 hours, filter to remove HgI precipitate, concentrate the obtained solution under reduced pressure to obtain a white solid, filter The precipitated white solid was washed with water and absolute ethanol respectively, and dried to obtain 3.34 g of carboplatin as a solid product with a yield of 86.79%. The structure is consistent with the target compound by ...

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Abstract

The invention relates to a method for preparing an antitumor drug of carboplatin H12C6O4N2Pt, which comprises that: a reagent of cis-diiododiammineplatinum(II) is added with water, stirred uniformly, heated in water bath to 50 to 60 DEG C, kept away from sunshine, added with mercury(I) 1,1-cyclobutyldicarboxylate(Hg2CBDCA) slowly for reaction for 8 to 10 hours; and the products of the reaction are filtered, and c a illiterate is concentrated under reduced pressure and thus solid carboplatin is obtained. The molar ratio of Pt (NH3)2I2 to Hg2CBDCA is 1:1. The method for preparing the carboplain is short in preparation process, avoids introducing an impurities containing Ag+, allows for easy removal of HgI due to small solubility product and achieves high target product yield up to more than 80 percent. (CBDCA is used to replace 1,1-cyclobutyldicarboxylate radical).

Description

technical field [0001] The invention relates to platinum antitumor drugs, in particular to the synthesis and preparation of antitumor drug carboplatin. Background technique [0002] Carboplatin is the second-generation platinum-based antitumor drug after cisplatin. It was jointly developed by Johnson Matthey Company of the United Kingdom, the Institute of Cancer Research of the United Kingdom and Squibb-Bristol Myer Company of the United States. It was launched in the United States in 1986 and is currently widely used all over the world. application. The English name of carboplatin is Carboplatin, referred to as CBP, and the chemical name is cis-1, 1-cyclobutane dicarboxylic acid-diammine platinum (II) [Cis-1, 1-cyclobutandicarboxylacid-diammine platinum (II)] . The molecular weight is 371.28, and the chemical structural formula is: [0003] [0004] Carboplatin is characterized by good water solubility (17.6mg / ml), and its antitumor activity is equivalent to that of c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00
Inventor 王庆琨普绍平丛艳伟侯树谦李永年何键朱泽兵李学杰
Owner KUNMING GUIYAN PHARMA
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