Method for efficiently preparing lobaplatin anhydrous substance

Abstract

The invention discloses a method for efficiently preparing a lobaplatin anhydrous substance. The method comprises the following steps: by taking trans-1, 2-diaminomethyl-cyclobutane hydrochloride andpotassium chloroplatinite as raw materials and water as a solvent, firstly neutralizing the trans-1, 2-diaminomethyl-cyclobutane hydrochloride under an alkaline condition to dissociate trans-1, 2-diaminomethyl-cyclobutane, and then reacting with potassium chloroplatinite to generate dichloride; performing replacement reaction on dichloride and silver nitrate; filtering out generated silver chloride precipitates, reacting a filtrate with sodium lactate at a certain pH value, transferring a reaction liquid into a dialysis bag with the molecular weight cutoff of 200, dialyzing, concentrating anddrying to obtain the lobaplatin anhydrous substance. The method has the advantages of few operation steps, short synthesis time, simplicity in operation, high purity of the obtained lobaplatin anhydrous substance and high yield.

Description

technical field [0001] The invention relates to the field of chemical synthesis, in particular to a method for efficiently preparing lobaplatin anhydrate. Background technique [0002] Lobaplatin (lobaplatin) is also known as lobaplatin and lobaplatin. Its chemical name is 1,2-diaminomethyl-cyclobutane-lactate platinum (II). Its chemical structure is as follows: [0003] It is a third-generation platinum-based antitumor drug developed by ASTAMedica, Germany. Studies have shown that the drug has definite cytotoxic effects on a variety of animal and human tumor cell lines, which is equivalent to or better than the tumor inhibitory effects of cisplatin and carboplatin, and has no cross-resistance with cisplatin, and has anticancer activity Strong, less toxic and side effects, good solubility of the drug, stable in water, mainly used for the treatment of chronic myelogenous leukemia, inoperable metastatic breast cancer and small cell lung cancer. [0004] After the original ...

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Problems solved by technology

Among the above methods, the ion exchange method has the longest steps, takes the longest time, and introduces many impurities. Especially when the reactants are ion-exchanged with anion-exchange resins, it is likely to produce monohydroxy nitrate impurities due to incomplete ion exchange. Thereby improving product purification difficulty, increased production cost; One-step reaction method step is least, and total preparation time is short, but the Cl introduced in the reaction process - , I - 、K + And trans-1,2-diaminomethyl-cyclobutane and L-lactic acid can not be effectively removed in the product, and the product quality is relatively poor; the pH method of adjusting the reaction solution has few reaction steps, short production cycle, and low production cost. The operation is simple, but a large amount of acetone needs to be used in the purification process to obtain a product with higher purity, which limits the production scale of lobaplatin

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