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A kind of preparation technology of ethacridine lactate

A technology for preparing ethacridine lactate and its preparation technology, which is applied in the field of preparation technology of ethacridine lactate and can solve problems such as difficulty in adapting to large-scale industrial production

Inactive Publication Date: 2021-06-08
成都巴赛泰德生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is: in the synthesis of 2-ethoxy-6,9-diaminoacridine in the prior art, there is a problem that it is difficult to adapt to large-scale industrial production, and the purpose is to provide a kind of ethacridine lactate The preparation process, through the optimization of the process, can effectively simplify the separation operation of the reaction route and post-treatment, reduce the amount of solvent, reduce the production cost, and realize the purpose of large-scale industrial production of ethacridine lactate

Method used

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  • A kind of preparation technology of ethacridine lactate

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Embodiment 1

[0028] A preparation process of ethacridine lactate, comprising:

[0029] First add 10g of 2-ethoxy-6-nitro-9-aminoacridine, 8g of zinc powder, and 3.9g of 90% lactic acid into the 500mL reaction bottle;

[0030] Then add 150mL of ethanol, heat to 80°C for 5 hours under the protection of nitrogen, and then filter while it is hot. The filtrate is naturally cooled to room temperature to precipitate a bright yellow solid. The bright yellow solid is ethacridine lactate solid, with a weight of 8.5g, the total yield is 70%, and the purity is 99.52%.

Embodiment 2

[0032] A preparation process of ethacridine lactate, comprising:

[0033] First add 200g of 2-ethoxy-6-nitro-9-aminoacridine, 160g of zinc powder, and 78g of 90% lactic acid into the 5L reaction flask;

[0034] Then add 3L of ethanol, heat to 80°C for 6 hours under the protection of nitrogen, and then filter while it is hot. The filtrate is naturally cooled to room temperature to precipitate a bright yellow solid. The bright yellow solid is ethacridine lactate solid, with a weight of 174g, the total yield is 71.6%, and the purity is 99.36%.

Embodiment 3

[0036] A preparation process of ethacridine lactate, comprising:

[0037] First add 2kg of 2-ethoxy-6-nitro-9-aminoacridine, 1.6kg of zinc powder, and 0.78kg of 90% lactic acid into the 50L reactor;

[0038] Then add 30L of ethanol, heat to 80°C for 7 hours under the protection of nitrogen, and then filter while it is hot. The filtrate is naturally cooled to room temperature to precipitate a bright yellow solid. The bright yellow solid is the ethacridine lactate solid, with a weight of 1.738g, the total yield is 71.4%, and the purity is 99.34%.

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Abstract

The invention discloses a preparation process and a preparation method of ethacridine lactate, which solves the problem that the synthesis of 2-ethoxy-6,9-diaminoacridine in the prior art is difficult to adapt to large-scale industrial production . The present invention comprises: step 1, using 2-ethoxy-6-nitro-9-aminoacridine as raw material, after adding organic solvent, reducing agent and lactic acid, heating to 40-90 DEG C under the protection of nitrogen to react; step 2. After the reaction is completed, filter, and the filtrate is naturally cooled to room temperature to precipitate bright yellow crystals. The invention can effectively realize the purpose of large-scale industrial production of 2-ethoxy-6,9-diaminoacridine, and can effectively improve production efficiency; it has the advantages of shortening the reaction route, avoiding environmental pollution, simplifying the process, and reducing production costs, Improve the reaction yield and other advantages.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a preparation process of ethacridine lactate. Background technique [0002] Ethacridine Lactate (Ethacridine Lactate) is an acridine-type bactericidal antiseptic drug, the trade name is Rivanol or Ravenol, and it has a strong killing effect on a very small number of Gram-negative bacteria. It has a good antibacterial effect on cocci, especially streptococcus, and is mainly used for the treatment of various wounds and infectious skin diseases, wound washing and external disinfection. In addition, due to the special effect of this product on the amniotic membrane of the uterus, it can be used as a drug for inducing labor in mid-trimester pregnancy. Its structural formula is as follows: [0003] [0004] The synthetic route of ethacridine was first disclosed in German Patent DE364033C. In this synthetic route, 2-ethoxy-6,9-diaminoacridine is separated first, and then undergoes a s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D219/10C07C59/08C07C51/41
CPCC07D219/10
Inventor 易磊邢桂燕
Owner 成都巴赛泰德生物科技有限公司
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