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A kind of method that piperazine is applied mechanically to produce piperaquine phosphate intermediate quinoline piperazine hydrochloride

A technology of quinoline piperazine and piperaquine phosphate, which is applied in the field of drug synthesis, can solve the problems of serious environmental pollution, high production cost, and long production cycle, and achieve the effects of small environmental pollution, low production cost, and increased yield

Active Publication Date: 2022-03-18
珠海润都制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0016] The main shortcomings of the above-mentioned method for preparing quinoline piperazine are the low purity of the prepared product, low yield, complicated operation, long production cycle, serious environmental pollution, and high production costs. Therefore, it is necessary to develop a new preparation method for the above-mentioned shortcomings. , and it is also important to recycle or apply mechanically the excessive reaction raw material piperazine

Method used

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  • A kind of method that piperazine is applied mechanically to produce piperaquine phosphate intermediate quinoline piperazine hydrochloride
  • A kind of method that piperazine is applied mechanically to produce piperaquine phosphate intermediate quinoline piperazine hydrochloride
  • A kind of method that piperazine is applied mechanically to produce piperaquine phosphate intermediate quinoline piperazine hydrochloride

Examples

Experimental program
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Effect test

Embodiment 1

[0051] Preparation of quinoline piperazine hydrochloride (first preparation)

[0052] Add 40g of water and 36g of anhydrous piperazine into a three-necked flask, stir, adjust the pH of the system to 6.0 with concentrated hydrochloric acid, heat to 65°C and stir for 1 hour; continue to heat up to 90°C, and slowly add 4,7-dichloroquine 20g of morphine, after the addition, continue to heat up to 95°C and stir the reaction for 5 hours; after the reaction, cool down to 45°C, stir for 1 hour, and filter while it is hot (collect the mother liquor as a solvent), and dry the filter cake to obtain quinoline Oxyzine hydrochloride 26.1g, yield 91.0%, purity 99.7%.

Embodiment 2

[0054] Preparation of quinoline piperazine hydrochloride (first preparation)

[0055] Add 60g of water and 52g of anhydrous piperazine into the three-necked flask, stir, adjust the pH of the system to 7.0 with 30% hydrochloric acid, raise the temperature to 80°C and stir for 30 minutes, slowly add 20g of 4,7-dichloroquinoline, after the addition is complete Continue to stir and react for 5 hours; after the reaction, cool down to 60°C, stir for 30 minutes, and filter while hot (collect the mother liquor as a solvent for application), and dry the filter cake to obtain 25.9 g of quinoline piperazine hydrochloride, with a yield of 90.3 %, 99.6% purity.

Embodiment 3

[0057] Preparation of quinoline piperazine hydrochloride (first preparation)

[0058] Add 80kg of water and 150kg of piperazine to a 1000L reaction tank, stir, adjust the pH of the system to 7.5 with concentrated hydrochloric acid, heat to 75±10°C and stir for 1 hour; continue to heat up to 95±5°C, slowly add 4,7-Di Chloroquinoline 100kg, after the addition, control the temperature at 95±5°C and stir the reaction for 4~5 hours; after the reaction, cool down to 60±5°C, stir for 1 hour, centrifuge while it is hot (collect the mother liquor as a solvent for application), filter cake After drying, 131 kg of quinoline piperazine hydrochloride was obtained, with a yield of 91.3% and a purity of 99.6%.

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Abstract

The invention discloses a method for preparing high-purity quinoline piperazine hydrochloride. The process is simple, the product is easy to purify, the purity is more than 99.5%, and toxic reagents are avoided, the environmental pollution is small, the production cost is low, and it is suitable for industrial production. The invention also discloses a method for producing quinoline piperazine hydrochloride by mechanical application of piperazine, without separating piperazine from the mother liquor, and directly applying the mother liquor to the production of the next batch of quinoline piperazine hydrochloride, The method has little environmental pollution and low production cost, improves the yield of the intermediate quinoline piperazine hydrochloride, and reduces production cost.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and relates to a synthesis method of an antimalarial drug piperaquine phosphate intermediate 7-chloro-4-(1-piperazinyl)quinoline (hereinafter referred to as quinoline piperazine) and the production of phosphoric acid by applying piperazine mechanically. The method of piperaquine intermediate quinoline piperazine hydrochloride. 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 resistanc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/42
CPCC07D215/42
Inventor 覃志俊庞振坤胡双龙周爱新焦慎超祁红林黄肖艳
Owner 珠海润都制药股份有限公司
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