Preparation of piperaquini phosphatis

A technology of piperaquine phosphate and quinoline, which is applied in the field of preparation of raw materials, can solve the problems of large environmental pollution, high production cost, and low product yield, and achieve low environmental pollution, low production cost, and high product yield. Effect
CN101440063BActive Publication Date: 2011-07-13CHONGQING KANGLE PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CHONGQING KANGLE PHARMA
Publication Date
2011-07-13

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Abstract

The invention discloses a method for preparing piperaquine phosphate. 4,7-dichloroquinoline is taken as an initial raw material and is subjected to condensation reaction with anhydrous piperazidine first to obtain 7-chloro-4-(1-piperazinyl)quinoline, then the 7-chloro-4-(1-piperazinyl)quinoline is subjected to condensation reaction with 1, 3-bromochloropropane to obtain piperaquine, and finally the piperaquine is salified with phosphorous acid to obtain the piperaquine phosphate. The method has a simple process, is easy to purify intermediate products and a final product, has high product yield and good quality, avoids the use of toxic reagents, has small pollution to the environment and low production cost, and is suitable for industrialized production.
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Description

technical field

[0001] The present invention relates to a kind of preparation method of crude drug, particularly a kind of preparation method of piperaquine phosphate. Background technique

[0002] Today, malaria is still listed as the world's three major catastrophic diseases together with AIDS and tuberculosis, and more than 90 countries and regions are still in the middle and high prevalence levels of malaria. According to the statistics of the World Health Organization (WHO), there are 300-500 million malaria-infected people in the world every year, and the death toll exceeds 1 million, and most of them are children under the age of five. In order to enhance the therapeutic effect and slow down the occurrence of drug resistance, since 2001, WHO has recommended the use of "Artemesinin-based Combination Therapy (ACT)" for the treatment of malaria. Piperaquine phosphate is a synthetic antimalarial drug, mainly used in the treatment of malaria resistant to chloroquine. In ...

Claims

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