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A technology of platinum complexes and compounds, applied in the field of new antitumor drug platinum complexes
Inactive Publication Date: 2006-11-08
张金超 +1
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From the perspective of chemical structure, there are three potential leaving groups in the platinum complexes involved in the present invention. It is speculated that its anticancer mechanism is different from that of non-classical platinum anticancer complexes, which has not been reported at home and abroad. Belongs to the category of non-classical platinum complexes
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[0069] ①cis-[Pt(C 2 h 5 NH 2 ) 2 I 2 ] Preparation of (i): Dissolve potassium chloroplatinite in water, add potassium iodide solution at an injection rate of 15 ml / min under agitation, react at 25° C. for 40 minutes, filter, and under agitation, Add ethylamine to the filtrate at an injection rate of 20 ml / min, react at 25°C for 30 minutes, filter the precipitate obtained by washing with water, ethanol and ether in sequence, then dry under vacuum conditions, potassium chloroplatinite: Potassium iodide: ethylamine=1mmol: 10mmol: 2.5mmol; ②[Pt(C 2 h 5 NH 2 ) I 2 ] 2 Preparation of (ii): Add perchloric acid and ethanol solution to the precipitate obtained in step ① respectively, stir for 40 hours at 50°C, filter, and wash the precipitate obtained by filtering with an ethanol-water mixed solvent to obtain the Platinum complex, vacuum drying then, the precipitate of step 1. gained: perchloric acid: ethanol=1mmo...
[0072] The steps for preparing the precursor complex are as described in Example 1 ①, ② and ③, ④ add silver carbonate, p-methoxybenzoic acid and an appropriate amount of methanol solution to the precipitate obtained in step ③, and at 25 ° C, avoid Lightly stirred for 46 hours, filtered, and the precipitate obtained by filtering was washed with water and ether respectively, and then vacuum-dried, the precipitate obtained in step ③: silver carbonate: p-methoxybenzoic acid=1mmol: 0.98mmol: 2.2mmol;
[0075] The steps for preparing the precursor complex are as described in Example 1 ①, ② and ⑧. ④ Add silver carbonate, benzoic acid and an appropriate amount of methanol solution to the precipitate obtained in step ③, and stir for 40 hours at 35°C in the dark , filtered, the precipitate obtained by filtering was washed with water and ether respectively, then vacuum-dried, the precipitate obtained in step 3.: silver carbonate: benzoic acid=1mmol: 0.96mmol: 2.1mmol;
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Abstract
The present invention relates to platinum complexes of antineoplastic drugs. The general structural formula of the platinum complexes of the present invention is as follows, ∴ or ∴ where the substituent X is acetate, monochloroacetate, dichloroacetate, benzoate, p-methoxy Monocarboxylates such as base benzoate, propionate and phenylacetate; Y is dicarboxylates such as oxalate, malonate, succinate, 1,1-cyclobutanedioate and maleate; the present invention Also disclosed are the preparation method of the complexes, the application of the complexes in the preparation of medicines for treating cancer and the pharmaceutical compositions containing them.
Description
Technical field: [0001] The present invention relates to new antitumor drug platinum complexes, their preparation method and their application in the preparation of antitumor drugs. Background technique: [0002] Cancer has become one of the main threats to human health, and it is showing a clear upward trend. Cancer has become the most important cause of death in the United States, and the cancer mortality rate ranks first among all causes of death in cities in my country. Therefore, my country has listed the research of anticancer drugs as one of the most important strategic issues in the development of new drugs, and researching new anticancer drugs with high efficiency, low toxicity and high selectivity has become a long-term goal and task for drug researchers. The platinum group metal complex cis-dichlorodiammine platinum (II), namely cisplatin, was discovered in 1967 to have anti-tumor activity, entered phase I clinical trials in 1971, and was approved for the treatmen...
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