Method for preparing lobaplatin trihydrate by usingoxalate

A technology of lobaplatin trihydrate and oxalate, applied in the field of preparation of lobaplatin trihydrate, can solve the problems of incomplete reaction, low lobaplatin yield, unstable properties, etc. Conducive to the effect of synthesis and complete reaction
CN102020679AActive Publication Date: 2011-04-20GUIZHOU YIBAI PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
GUIZHOU YIBAI PHARMA CO LTD
Publication Date
2011-04-20

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Abstract

The invention relates to a method for preparing a lobaplatin trihydrate by using oxalate, diaminomethyl cyclobutane oxalate, potassium chloroplatinite and potassium iodide are taken as raw materials, and the method comprises the following steps: firstly replacing the potassium chloroplatinite to potassium iodoplatinite, neutralizing the oxalic acid in diaminomethyl cyclobutane under alkaline condition, enabling the diaminomethyl cyclobutane to be freed, and then reacting the diaminomethyl cyclobutane with K2PtI4 (potassium iodoplatinate) for synthesizing a diiodide; enabling the diiodide to carry out replacement reaction with silver nitrate to generate silver iodide precipitate, enabling reactants after filtering out the precipitate to carry out ion exchange with anion exchange resin, then synthesizing a lobaplatin anhydride with lactic acid, re-crystallizing the anhydride in water / acetone mixed solution, and finally obtaining a lobaplatin trihydrate product. The raw materials used in the method have stable performances, the reaction is fuller and more complete, and the yield of the lobaplatin trihydrate is high.
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Description

technical field

[0001] The invention relates to a preparation method of lobaplatin trihydrate, in particular to a method for preparing lobaplatin trihydrate with oxalate. Background technique

[0002] Lobaplatin (D19466), also known as Lobaplatin, is the third-generation platinum-based antineoplastic drug developed by ASTA Medica AG after cisplatin and carboplatin. Its chemical name is: 1,2-diaminomethyl-cyclobutane-lactate platinum. Molecular formula is C 9 h 18 N 2 o 3 Pt, the molecular weight is 397.34, the chemical structure formula is as follows:

[0003]

[0004] Lobaplatin has an alkylating effect and is an alkylating agent (broad sense). Studies have shown that it has definite cytotoxic effects on a variety of animal and human tumor cell lines, which is equivalent to or better than cisplatin and carboplatin in tumor inhibition, and has the same toxic effect as carboplatin, and has no cross-resistance to cisplatin . It has strong anticancer activity, low to...

Claims

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