Preparation method of chloroquinaldol

A technology for chloroquinadol and chloroquinadol hydrochloride, applied in the field of medicine, can solve the problems of lack of chloroquinadol product quality research, affecting product stability, efficacy and metabolism, etc., and achieves the effects of easy operation and high stability

Active Publication Date: 2020-05-08
BEIJING JINCHENG TAIER PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Although this method does not adjust the pH value, N-chlorosuccinimide can chlorinate on the methyl group of 8-hydroxyl-2-methylquinoline, generate new impurities, affect the stability of the product and Drug efficacy a

Method used

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  • Preparation method of chloroquinaldol
  • Preparation method of chloroquinaldol
  • Preparation method of chloroquinaldol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Under the condition of avoiding light and nitrogen protection, add 200ml of 20wt.% hydrochloric acid, 10 grams of 8-hydroxy-2-methylquinoline into a 500ml four-necked bottle, and feed 9.8 grams of chlorine gas until the chlorination reaction is completed, filter, and the filter cake dissolves. Add 10ml of 0.05M citric acid-sodium dihydrogen phosphate solution in water under the condition of dark and nitrogen protection, adjust the pH to 4.5 with sodium isooctanoate, filter, and refine with ethanol to obtain 14.14 g of chloroquinaldol with a yield of 98.6% , HPLC purity 99.99%.

Embodiment 2

[0037] Under the condition of avoiding light and nitrogen protection, add 200ml of 20wt.% hydrochloric acid, 10 grams of 8-hydroxy-2-methylquinoline to a 500ml four-necked bottle, add dropwise 103 grams of 10wt.% sodium hypochlorite solution, and keep warm until the chlorination reaction Finish, filter, dissolve the filter cake in water, under the condition of dark and nitrogen protection, add 20ml of 0.05 citric acid-sodium dihydrogen phosphate solution, adjust the pH to 4.5 with sodium isooctanoate, filter, and refine with ethanol to obtain 14.18 grams of chloroquinaldol , the yield was 98.9%, and the HPLC purity was 99.99%.

Embodiment 3

[0039] Under the condition of avoiding light and nitrogen protection, add 200ml of formic acid and 10 grams of 8-hydroxy-2-methylquinoline into a 500ml four-necked bottle, feed 9.8 grams of chlorine gas until the chlorination reaction is completed, filter, and the filter cake is dissolved in water. Under the condition of avoiding light and nitrogen protection, add 15ml of 0.05M citric acid-sodium dihydrogen phosphate solution, adjust the pH to 4.5 with sodium isooctanoate, filter, and refine with ethanol to obtain 14.15 grams of chloroquinaldol, with a yield of 98.7%, HPLC purity is 99.99%.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of chloroquinaldol. The preparation method comprises the following steps: adding water intochloroquinaldol hydrochloride for dissolving, adding a buffer solution under the conditions of light shielding and nitrogen protection, regulating the pH value by using alkali, filtering and refiningthe solution to obtain chloroquinaldol. The method is easy and convenient to operate and suitable for industrial production, the purity of the prepared chloroquinaldol is high and can reach 99.99% orabove, and the stability of the product is high.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of chloroquinaldol. Background technique [0002] Chlorquinaldol is a broad-spectrum bacteriostatic agent, and its structural formula is as follows: [0003] [0004] The relative molecular weight of chloroquinaldol is 228.07, and it has a slightly pungent smell, and it is a yellow needle-like crystal. As early as the 1950s, many European pharmaceutical companies conducted extensive research on it and found that it has anti-microbial pathogen activity such as anti-fungal, trichomonas, bacteria (G+ and G-), chlamydia and mycoplasma. [0005] Chloroquinaldol was first developed and produced by Theramex Pharmaceutical Factory in Monaco. The disclosed synthetic method is to use 8-hydroxy-2-methylquinoline as a raw material, use 20% hydrochloric acid as a solvent, and undergo one-step chlorination under the condition of chlorine gas. Synthesize b...

Claims

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Application Information

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IPC IPC(8): C07D215/28
CPCC07D215/28
Inventor 王琨张忠政刘文杰张国斌张治中张彤寇世超李景坤
Owner BEIJING JINCHENG TAIER PHARMA CO LTD
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