74351-59-0Relevant academic research and scientific papers
Hydroxy piperaquini and its phosphate preparation method
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Paragraph 0063; 0068; 0069; 0080; 0091; 0102; 0113; 0124, (2018/01/20)
The invention provides a preparation method of hydroxypiperaquine and phosphate thereof. The preparation method of hydroxypiperaquine comprises the following steps: by using piperazine, 1,3-dihalopropanol and 4,7-dichloroquinoline as raw materials, reacting the piperazine and 1,3-dihalopropanol by using an acid-binding agent as a catalyst to obtain 1,3-dipiperazinylpropanol, carrying out condensation reaction on the 1,3-dipiperazinylpropanol and 4,7-dichloroquinoline under the catalytic action of an alkali to obtain the hydroxypiperaquine. The obtained hydroxypiperaquine reacts with phosphoric acid to obtain the hydroxypiperaquine phosphate. The method has the advantages of mild reaction conditions, simple preparation technique and low cost, and is suitable for industrial production. The total reaction yield of the hydroxypiperaquine is up to 90-91.5%, and the total reaction yield of the hydroxypiperaquine phosphate is up to 82.7-87.5%.
