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Preparation method of piperaquine derivative

A technology of derivatives and piperaquine, which is applied in the preparation of 1,4-dipiperazine and the field of piperaquine derivatives Ⅲ, which can solve the problems that the synthesis and purification methods of piperaquine derivatives Ⅲ have not been reported.

Inactive Publication Date: 2016-02-17
CHONGQING KANGLE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] The synthesis and purification methods of piperaquine derivative Ⅲ have not been reported

Method used

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  • Preparation method of piperaquine derivative
  • Preparation method of piperaquine derivative
  • Preparation method of piperaquine derivative

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Embodiment 1

[0033] The preparation of embodiment 1 piperaquine derivative III

[0034] Add 100ml of ethanol, 39.6g of 4,7-dichloroquinoline, and 4.3g of anhydrous piperazine into the reaction flask, start stirring, and raise the temperature to reflux for 8 hours. After the reaction, distill out ethanol, add 200ml of 5% dilute hydrochloric acid solution, Stir for 30 minutes, cool to 20-25°C, and separate the solid by filtration. Transfer the filter cake into a reaction flask, add 100ml of 5% sodium hydroxide solution, stir at 20-25°C for 1 hour, filter and separate the solid; transfer the filter cake into a reaction flask, add 100ml of 5% dilute hydrochloric acid solution, Stir for 1 hour, filter and separate the solid; then use 5% sodium hydroxide solution and 5% dilute hydrochloric acid solution to beat for 3 times; transfer the separated solid into a reaction flask, add 200ml of purified water, and stir for 1 hour at 20-25°C , the solid was separated by filtration, and dried under redu...

Embodiment 2

[0035] The preparation of embodiment 2 piperaquine derivative III

[0036] Add 100ml of methanol, 59.6g of 4,7-dichloroquinoline, and 4.3g of anhydrous piperazine into the reaction flask, start stirring, and raise the temperature to reflux for 8 hours. After the reaction, distill off methanol, add 200ml of 5% dilute hydrochloric acid solution, Stir for 30 minutes, cool to 20-25°C, and separate the solid by filtration. Transfer the filter cake into a reaction flask, add 100ml of 5% sodium hydroxide solution, stir at 20-25°C for 1 hour, filter and separate the solid; transfer the filter cake into a reaction flask, add 100ml of 5% dilute hydrochloric acid solution, Stir for 1 hour, filter and separate the solid; then use 5% sodium hydroxide solution and 5% dilute hydrochloric acid solution to beat for 3 times; transfer the separated solid into a reaction flask, add 200ml of purified water, and stir for 1 hour at 20-25°C , the solid was separated by filtration, and dried under re...

Embodiment 3

[0037] The preparation of embodiment 3 piperaquine derivative III

[0038] Add 100ml of methanol, 39.6g of 4,7-dichloroquinoline, and 4.3g of anhydrous piperazine into the reaction flask, start stirring, and raise the temperature to reflux for 8 hours. After the reaction, distill off methanol, add 200ml of 5% dilute hydrochloric acid solution, Stir for 30 minutes, cool to 20-25°C, and separate the solid by filtration. Transfer the filter cake into a reaction flask, add 100ml of 5% sodium hydroxide solution, stir at 20-25°C for 1 hour, filter and separate the solid; transfer the filter cake into a reaction flask, add 100ml of 5% dilute hydrochloric acid solution, Stir for 1 hour, filter and separate the solid; then use 5% sodium hydroxide solution and 5% dilute hydrochloric acid solution to beat for 3 times; transfer the separated solid into a reaction flask, add 200ml of purified water, and stir for 1 hour at 20-25°C , the solid was separated by filtration, and dried under re...

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Abstract

The invention discloses a preparation method of a piperaquine derivative III, namely, 1,4-bi(7-chloroquinolin-4-yl)piperazine. The piperaquine derivative III is a piperaquine dimmer impurity and is one of main impurities of crude drugs or preparations of piperaquine and piperaquine salt. The piperaquine derivative III can be used for analyzing and detecting the purity of chemicals piperaquine and piperaquine salt, thereby controlling the quality of piperaquine and piperaquine salt.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical industry, and specifically relates to the preparation method and application of piperaquine derivative III, namely 1,4-bis(7-chloroquinolin-4-yl)piperazine. Background technique [0002] Pipequine is a bisquinoline antimalarial drug, and among the three major deadly diseases in Africa, malaria ranks first. According to the statistics of the World Bank, malaria causes economic losses of 12 billion U.S. dollars to sub-Saharan African countries every year, seriously hindering the economic development of Africa. Most of the malaria-infected people in Africa are children, who face the threat of death due to lack of effective treatment. Malaria is prevalent in more than a dozen provinces, municipalities, and autonomous regions in China, with about 40,000 people suffering from it every year. The World Health Organization pointed out that the existing cheap drugs have been used for many ye...

Claims

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Application Information

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IPC IPC(8): C07D215/46
CPCC07D215/46
Inventor 唐明沈文晖马小平郑雪陈林杨继斌蔡中文王亚川
Owner CHONGQING KANGLE PHARMA
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