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A kind of preparation method and its application of high safety hydroquinone composition

一种氢醌、对苯醌的技术，应用在氢醌组合物的制备领域，能够解决影响人们生命安全、损害血红蛋白等问题，达到药品质量可控、促进质量升级、降低副反应的效果

Active Publication Date: 2022-04-15
GUANGDONG RENRENKANG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aniline is a carcinogen, and it can also damage the hemoglobin that transports oxygen in the blood. Acute high exposure will cause dizziness, headache, irregular heartbeat, convulsions, coma and death, seriously affecting people's life safety

Method used

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  • A kind of preparation method and its application of high safety hydroquinone composition
  • A kind of preparation method and its application of high safety hydroquinone composition
  • A kind of preparation method and its application of high safety hydroquinone composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Example 1 The preparation of hydroquinone of the present invention

[0099] The preparation method of hydroquinone, comprises the steps:

[0100] 1) MnO 2 Add 280g, 430g of 98% sulfuric acid, and 2.0L of water into the reaction flask, slowly add 100g of aniline dropwise at 5-10°C, stir, and gradually raise the temperature to about 25°C until the reaction is complete. The reaction liquid is steam distilled at 60-90°C, and the collected p-benzoquinone condensate is introduced into another reaction flask;

[0101] 2) Under the condition of shading and nitrogen protection, add 42g of iron powder to the collected p-benzoquinone condensate, stir and react for 3-4 hours at 90-100°C, until the reaction is complete, filter, and depressurize the collected filtrate Concentrating to a hydroquinone content of 35% in the concentrated solution;

[0102] 3) Add 550mg of sodium metabisulfite, 2.2g of activated carbon, and 330mg of zinc powder to the concentrated solution, heat to ...

Embodiment 2

[0103] Example 2 The preparation of hydroquinone of the present invention

[0104] The preparation method of hydroquinone, comprises the steps:

[0105] 1) MnO 2 Add 350g, 500g of 98% sulfuric acid, and 2.0L of water into the reaction flask, slowly add 100g of aniline dropwise at 5°C-8°C, stir, and gradually raise the temperature to about 25°C until the reaction is complete. The reaction liquid is steam distilled at 60-90°C, and the collected p-benzoquinone condensate is introduced into another reaction flask;

[0106] 2) Under the conditions of shading and nitrogen protection, add 60g of iron powder to the collected p-benzoquinone condensate, stir and react for 2-3 hours at 90-100°C, until the reaction is complete, filter, collect the filtrate and concentrate under reduced pressure To the hydroquinone content in the concentrated solution is 25%;

[0107] 3) Add 750 mg of sodium pyrosulfite, 3.1 g of activated carbon, and 500 mg of iron powder to the concentrated solution,...

Embodiment 3

[0108] Example 3 The preparation of hydroquinone of the present invention

[0109] The preparation method of hydroquinone, comprises the steps:

[0110] 1) MnO 2 Add 250g, 370g of 98% sulfuric acid, and 2.5L of water into the reaction flask, slowly add 100g of aniline dropwise at 6-10°C, stir, and gradually raise the temperature to about 25°C until the reaction is complete. The reaction liquid is steam distilled at 70-95°C, and the collected p-benzoquinone condensate is introduced into another reaction flask;

[0111] 2) Under the conditions of shading and nitrogen protection, add 31g of iron powder to the collected p-benzoquinone condensate, stir and react at 90-100°C for 2-3 hours, until the reaction is complete, filter, collect the filtrate and concentrate it under reduced pressure to The content of hydroquinone in the concentrated solution is 30%;

[0112] 3) Add 550 mg of sodium pyrosulfite, 2.20 g of activated carbon, and 350 mg of zinc powder to the concentrated s...

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Abstract

The present invention also provides a method for preparing a high-safety hydroquinone composition, comprising the steps of: 1) aniline, MnO2, and sulfuric acid are mixed according to the molar ratio of aniline: MnO2: sulfuric acid is 1:1-5:2- 6 Add the reaction device and stir until the reaction is complete to obtain p-benzoquinone, wherein the feeding temperature is 0-15°C and the reaction temperature is 0-30°C; 2) the prepared p-benzoquinone reaction solution is steam distilled and Add iron powder to the collected distillation condensate according to the p-benzoquinone:iron powder molar ratio of 1:0.5-1.0, and stir at 70-100°C until the reaction is complete to obtain hydroquinone. The method has the advantages of simple operation, high yield, high purity, low cost, suitable for industrial production and the like.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and in particular relates to a preparation method and application of a high-safety hydroquinone composition. Background technique [0002] As a tyrosinase inhibitor, hydroquinone (also known as hydroquinone) mainly inhibits tyrosinase activity through complexation, regulates the metabolic process of melanocytes, and significantly reduces the number of dopa-positive melanocytes in the epidermis, resulting in reversible Sexual skin discoloration. Oettel first proposed in 1936 that hydroquinone has the effect of whitening the skin. Since the 1960s, many countries have used hydroquinone as a whitening agent in cosmetics and in dermatology for the treatment of pigmentation, freckles and other external preparations. But the amount of hydroquinone must be strictly controlled. [0003] [0004] Hydroquinone is unstable and is susceptible to oxidative degradation reactions under the influence...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C37/00C07C39/08A61K8/34A61Q19/02A61K31/05A61P17/00
CPCC07C46/04C07C37/07C07C46/10G01N30/06G01N30/74C07C2601/16C07C50/04C07C39/08
Inventor 苏冠荣尹贝立
Owner GUANGDONG RENRENKANG PHARM CO LTD
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