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Method for preparing hydroxy carboxylic acid platinum complexes

A platinum complex and hydroxycarboxylic acid technology, applied in the field of hydroxycarboxylic acid platinum complexes, can solve the problems of low yield and complicated production process, and achieve the effects of high yield, short process and good purity

Inactive Publication Date: 2010-07-28
HANGZHOU MINSHENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the above-mentioned method, there are problems such as complex production process and low yield as in the preparation method of nedaplatin.

Method used

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  • Method for preparing hydroxy carboxylic acid platinum complexes
  • Method for preparing hydroxy carboxylic acid platinum complexes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1--the preparation of nedaplatin

[0024] Feeding:

[0025] Platinum diiododiammine 4.83g 0.01mol

[0026] Silver oxide 2.30g 0.01mol

[0027] Glycolic acid 0.80g 0.01mol

[0028] 150ml deionized water

[0029] Add the above items into a 250ml one-necked bottle, and react with electromagnetic stirring at room temperature for 16 hours. After filtration, the filtrate was evaporated to dryness under reduced pressure at 60°C. Cool, wash with water, filter, wash with ethanol, and dry under vacuum at 40°C for 2 to 3 hours to obtain 1.85 g of the product nedaplatin, with a yield of 61.1% and a content of 99.7%.

[0030] The obtained product is consistent with the target product through elemental analysis:

[0031] Elemental analysis:

[0032] PtC 2 h 5 N 2 o 3 M=303.18

[0033] Theoretical value: C: 7.92% H: 2.64% N: 9.24% Pt: 64.36%

[0034] Found: C: 7.90% H: 2.63% N: 9.25% Pt: 64.33%

Embodiment 2

[0035] Embodiment 2--the preparation of nedaplatin

[0036] Feeding:

[0037] Platinum diiododiammine 4.83g 0.01mol

[0038] Silver oxide 2.30g 0.01mol

[0039] Glycolic acid 0.80g 0.01mol

[0040] 150ml deionized water

[0041] The above items were added into a 250ml single-necked bottle, and reacted with electromagnetic stirring at 60°C for 6 hours. After filtration, the filtrate was evaporated to dryness under reduced pressure at 60°C. Cool, wash with water, filter, wash with ethanol, and dry under vacuum at 45° C. for 2 to 3 hours to obtain 2.05 g of the product nedaplatin, with a yield of 67.7% and a content of 99.6%.

[0042] The obtained product is consistent with the target product through elemental analysis:

[0043] Elemental analysis:

[0044] PtC 2 h 5 N 2 o 3 M=303.18

[0045] Theoretical value: C: 7.92% H: 2.64% N: 9.24% Pt: 64.36%

[0046] Found: C: 7.89% H: 2.62% N: 9.23% Pt: 64.31%

Embodiment 3

[0047] Embodiment 3--the preparation of lobaplatin

[0048] Feeding:

[0049] cis-[trans-1,2-cyclobutylbis(methylamine)-N,N]-diiodoplatinum 5.63g 0.01mol

[0050] Silver oxide 2.30g 0.01mol

[0051] L-lactic acid 0.90g 0.01mol

[0052] 150ml deionized water

[0053] Add the above items into a 250ml one-necked bottle, and react with electromagnetic stirring at 40°C for 10 hours. After filtration, the filtrate was evaporated to dryness under reduced pressure at 60°C. Cool, wash with water, filter, wash with ethanol, and vacuum-dry at 40°C for 2 to 3 hours to obtain 2.65 g of lobaplatin, with a yield of 58.8% and a content of 99.6%.

[0054] The obtained product is consistent with the target product through elemental analysis:

[0055] Elemental analysis:

[0056] PtC 9 h 24 N 2 o 6 M=451.38

[0057] Theoretical value: C: 23.95% H: 5.36% N: 6.21% Pt: 43.22%

[0058] Found: C: 23.93% H: 5.33% N: 6.18% Pt: 43.19%

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Abstract

The invention relates to a method for preparing hydroxy carboxylic acid platinum complexes, in particular to a method for preparing platinum anticancer drugs of nedaplatin and lobaplatin. The preparation method includes that: compounds (I) and (II) and silver oxide in molar ratio of 1:1: 1, and certain quantity of water are added to a reactor and stirred to conduct light-shielding reaction for 1-20 hours at the temperature of 0-80 DEG C. The filtrate after filtration is concentrated to be dry, is cooled and rinsed by water, filtrated and rinsed by ethanol and is finally pumped out to obtain the product (III) after vacuum drying for 2-3 hours at the temperature of 40-45 DEG C. The invention obtains the product water solution through one-step reaction, concentrates the water solution to obtain the final product, has no need to adjust the pH value in the synthesis process, avoids the Na<+>, NO<3->, SO4<2->, Ba<2+> interference reaction, and accordingly realizes high productivity and good purity.

Description

technical field [0001] The invention relates to hydroxycarboxylic acid platinum complexes, in particular to a preparation method of platinum antitumor drugs nedaplatin and lobaplatin. Background technique [0002] Hydroxycarboxylic acid platinum complex drugs currently include nedaplatin, lobaplatin, etc. [0003] Nedaplatin (254-S) is the second-generation platinum-based antineoplastic drug after cisplatin and carboplatin. Chemical Structure Nedaplatin was developed by Shionogi Co., Ltd. in Japan, and was approved for marketing in Japan in June 1995. Nedaplatin is characterized by good water solubility; small toxic and side effects, and the dose-limiting toxicity is bone marrow suppression, without nephrotoxicity and neurotoxicity; It has a wide cancer spectrum and is active against head and neck cancer, ovarian cancer, esophageal cancer, bladder cancer and small cell lung cancer. In "Synthesis of (Glycolato-O, O')Diammineplatimun (II) and its Related Complexes" in "The...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00
Inventor 庄胜利郭殿武沈慈敏
Owner HANGZHOU MINSHENG PHARM CO LTD
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