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A technology of dexrazoxane and propylenediaminetetraacetic acid, which is applied in the field of medicine, can solve the problems of large batch operation fluctuation, limited industrial application, and uncontrollable product quality, and achieves easy control of process conditions and simple and easy operation of post-processing , The effect of strong process operability
Active Publication Date: 2022-07-01
SICHUAN HUIYU PHARMA +1
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CN104177301A, CN101563329A etc. also disclose can be in methanol or dioxane, use sodium methoxide or sodium hydride to catalyze the reaction, but the yield is lower
[0011] Wherein, chloroacetic acid or its derivatives are used as substrates to react with the resolved (S)-1,2-propanediamine to form (S)-1,2-propanediaminetetraacetic acid or its corresponding derivatives, Finally, in the process of ring-closing reaction to prepare dexrazoxane, it is necessary to carry out a decompression reaction at about 150°C. At high temperature, dexrazoxane is very easy to react to form impurities, so the yield and purity of the reaction are poor, and the operation fluctuates between batches. High reliability and uncontrollable product quality limit the industrial application of this route
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Embodiment 1
[0058] Synthesis of Dexrazoxane
[0059] 15ml of N,N-dimethylformamide, 3.91g of urea, 5.03g of (S)-1,2-propanediaminetetraacetic acid were added to the reaction flask, the temperature was raised to 140°C under stirring, reacted for 5h, and 45ml of ethanol was added at room temperature Stir for 1 h, filter with suction, and dry to obtain 2.89 g of an off-white solid with a yield of 65% and a purity of 96.45% detected by HPLC.
Embodiment 2
[0061] Synthesis of Dexrazoxane
[0062] 15ml of dimethyl sulfoxide, 2.98g of urea, 5.07g of (S)-1,2-propanediaminetetraacetic acid were added to the reaction flask, the temperature was raised to 180°C under stirring, reacted for 3h, 30ml of ethanol was added, stirred at room temperature for 1h, and suction filtered , dried to obtain 3.09g off-white solid, yield 69%, HPLC detection purity 97.11%.
Embodiment 3
[0064] Synthesis of Dexrazoxane
[0065] 15ml of N,N-dimethylacetamide, 2.98g of urea, 5.01g of (S)-1,2-propanediaminetetraacetic acid were added to the reaction flask, the temperature was raised to 160°C under stirring, reacted for 6h, and 105ml of ethanol was added at room temperature Stir for 1 h, filter with suction, and dry to obtain 3.28 g of an off-white solid with a yield of 75% and a purity of 95.46% detected by HPLC.
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Abstract
The invention provides a preparation method of dexrazolone, which comprises the following step: carrying out ring closing reaction on (S)-1, 2-propylene diamine tetraacetic acid and urea to obtain the dexrazolone. The preparation method has the following beneficial effects: 1, urea is adopted as an amination nitrogen source, high-purity dexrazoxane can be obtained through conventional reaction operation, harsh reaction conditions are avoided, the process operability is high, and process production is facilitated; 2, the reaction is fast, the generation of partial process impurities is avoided, the purification pressure of the final product is reduced, the purity and yield of the prepared dexrazoxane are high, the production cost is greatly reduced, and the method is economical and environment-friendly; 3, post-treatment is simple, convenient and easy to operate, and stable production of a high-quality dexrazoxane raw material medicine is facilitated; and 4, the operation is simple, the process conditions are easy to control, the cost is lower, the yield of products among batches is stable, the refined dexrazoxane is white powder, the purity reaches 99.9% or above, and the maximum individual impurity is 0.05% or below.
Description
technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of dexrazoxane. Background technique [0002] Dexrazoxane is an anti-tumor adjuvant drug, clinically used to alleviate or reduce the cardiotoxicity caused by anthracycline (such as doxorubicin) chemotherapy. The mechanism by which dexrazoxane exerts its cytoprotective activity is not fully understood. Dexrazoxane is a lipophilic derivative of the chelating agent ethylenediaminetetraacetic acid (EDTA), which can rapidly penetrate the cell membrane to reduce the cardiotoxicity of anthracycline antitumor antibiotics such as doxorubicin. Dexrazoxane is hydrolyzed to TCRE in cells -198, and then chelate with intracellular iron, reduce the complex of ferric ions and anthracycline antitumor drugs such as doxorubicin, and prevent the formation of free radicals. [0003] Dexrazoxane for injection was developed by Chiron Corporation of the United States. It was firs...
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