Preparing method of lipid soluble platinum coordination compound with antitumor activities

Abstract

The invention provides a preparing method of a lipid soluble platinum coordination compound with antitumor activities. The prepared platinum coordination compound is called cis-[bis-myristic acid-trans-dimethylamino-cyclobutane chloride (II)], and the molecular formula is C34H68N2O4Pt. The preparing method comprises the specific steps of firstly, preparing trans-diiodine-cyclobutane chloride, thendissolving silver nitrate and prepared trans-dimethylamino-cyclobutane chloride into a reaction solvent to be subjected to a hydrolysis reaction to obtain hydrolysate and filtering the hydrolysate; adding the filtered hydrolysate into myristic acid or myristic acid salt, so that the white substance generated in the reaction is the coarse product of the platinum coordination compound, and after the coarse product is recrystallized, the fine product can be obtained. The lipid soluble platinum coordination compound prepared according to the method is high in lipid solubility and stable and has agood inhibiting effect on liver cancer cells, can be prepared into freeze-dried powder and lipiodol turbid liquid and is conveniently used for clinically preparing liver cell cancer.

Description

technical field [0001] The application belongs to the technical field of medicinal chemistry, and in particular relates to a preparation method of a fat-soluble platinum complex with antitumor activity. Background technique [0002] Platinum antineoplastic drugs are widely used chemotherapy drugs in clinical practice, with a history of nearly 50 years of research and use. At present, there are a total of 8 platinum-based antineoplastic drugs on the market in the world or some countries and regions. They are cisplatin (global), carboplatin (global), oxaliplatin (global), nedaplatin (Japan), heptad Platinum (Korea), Lobaplatin (China), Miplatinum (Japan) and Bicycloplatin (China). [0003] Lobaplatin, also known as Lobaplatin, Lobaplatin, code name D-19466, full name cis-[trans-1,2-dimethylaminocyclobutane-lactic acid] platinum (II). It was approved by the State Food and Drug Administration (CFDA) in 2005 and listed as a new drug, mainly for the treatment of chronic myelogen...

AI Technical Summary

Problems solved by technology

[0008] U.S. Patent No. 5,023,335 discloses a large number of Pt (II) complexes with trans-1,2-dimethylaminocyclobutane as a carrier group, and its leaving group includes chloride ion, oxalic acid, malonic acid, etc., but Compounds that do not have long-chain fatty acids as leaving groups

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