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Synthetic method for trimethoprim medicine midbody parahydroxybenzaldehyde

A technology of p-hydroxybenzaldehyde and trimethoprim, which is applied in the field of synthesis of trimethoprim pharmaceutical intermediate p-hydroxybenzaldehyde, can solve the problems that bacteria are prone to drug resistance and are rarely used alone, so as to reduce the reaction Effect of temperature and reaction time, reduction of intermediate links, and improvement of reaction yield

Inactive Publication Date: 2017-02-22
厦门莱恩斯特信息科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] Trimethoprim is a broad-spectrum antibacterial drug, the antibacterial spectrum is similar to that of sulfa drugs, and it can inhibit dihydrofolate reductase, but bacteria are prone to drug resistance, so it is rarely used alone

Method used

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  • Synthetic method for trimethoprim medicine midbody parahydroxybenzaldehyde

Examples

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Effect test

example 1

[0014] (i) Add 0.17mol of p-aminobenzaldehyde (2) and 150ml of water into a reaction vessel with a volume of 800mL, slowly add 50mL of concentrated phosphoric acid with a mass fraction of 50%, control the temperature of the solution to rise to 80°C, and generate phosphate to obtain Suspension, cool the solution to 15°C, slowly add 0.25mol of sodium bisulfite dissolved in 100ml of aqueous solution dropwise, control the stirring speed at 100rpm during the dropwise addition, and test the end point with potassium iodide test paper;

[0015] (ii) Control the temperature of the solution at 30°C, let it stand for 20min, add 5g of urea, control the temperature of the solution to rise gradually, after a large amount of gas escapes, heat the solution to 90°C, keep it for 10min, decolorize with molecular sieve, filter while hot, filter The cake was washed with ether solvent, the filtrate and the washing liquid were combined, and the solid was precipitated after the temperature was lowered...

example 2

[0017] (i) Add 0.17mol of p-aminobenzaldehyde (2) and 180ml of water into a reaction vessel with a volume of 900mL, slowly add 50mL of concentrated phosphoric acid with a mass fraction of 60%, control the temperature of the solution to rise to 90°C, and generate phosphate, and obtain Suspension, cool the solution to 17°C, slowly add 0.25mol of sodium bisulfite dissolved in 100ml of aqueous solution dropwise, control the stirring speed at 200rpm during the dropwise addition, and test the end point with potassium iodide test paper;

[0018] (ii) Control the temperature of the solution at 30°C, let it stand for 20min, add 5g of urea, control the temperature of the solution to rise gradually, after a large amount of gas escapes, heat the solution to 92°C, keep it for 10min, decolorize with molecular sieve, filter while hot, filter The cake was washed with acetone solvent, the filtrate and the washing liquid were combined, and the solid was precipitated after the temperature was low...

example 3

[0020] (i) Add 0.17mol of p-aminobenzaldehyde (2) and 200ml of water into a reaction vessel with a volume of 1000mL, slowly add 50mL of concentrated phosphoric acid, control the temperature of the solution to rise to 95°C, and generate phosphate to obtain a suspension, and cool the solution To 20°C, slowly add 0.25mol of sodium bisulfite dissolved in 100ml of aqueous solution dropwise, control the stirring speed at 300rpm during the dropwise addition, and test the end point with potassium iodide test paper;

[0021] (ii) Control the temperature of the solution at 30°C, let it stand for 20min, add 5g of urea, control the temperature of the solution to rise gradually, after a large amount of gas escapes, heat the solution to 95°C, keep it for 10min, decolorize with molecular sieve, filter while hot, filter The cake was washed with ethyl acetate solvent, the filtrate and the washing liquid were combined, and a solid was precipitated after the temperature was lowered, and the solid...

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Abstract

The invention discloses a synthetic method for a trimethoprim medicine midbody parahydroxybenzaldehyde. The synthetic method comprises the steps of i, adding 0.17 mol of para aminotenzaldehyde (2) and 150-200 ml of water into a reaction container with a volume of 800-1000 mL, slowly adding 50 mL of strong phosphoric acid, controlling the solution temperature to rise to 80-95 DEG C, generating phosphate, obtaining the suspension liquid, cooling the solution to 15-20 DEG C, slowly adding dropwisely 0.25 mol pf sodium hydrogen sulfite into 100 ml water solution, controlling stirring speed at 100-300 rpm in the dropwise adding process, and testing the terminal point with potassium iodide starch paper; (ii), controlling solution temperature at 30 DEG C, still standing for 20 min, adding 5 g of urea, controlling the solution temperature to rise gradually, after a large amount of gas escapes, heating the solution to 90-95 DEG C, keeping 10 min, decoloring with a molecular sieve, filtering as the solution is hot, washing a filter cake with a solvent, mixing filter liquor and a washed liquid, precipitating a solid after the temperature falls, adding the solid into a sodium chloride solution for recrystallization, filtering, and drying to obtain the parahydroxybenzaldehyde.

Description

technical field [0001] The invention relates to a method for synthesizing trimethoprim drug intermediate p-hydroxybenzaldehyde. Background technique [0002] Trimethoprim is a broad-spectrum antibacterial drug with a similar antibacterial spectrum to sulfonamides. It has the effect of inhibiting dihydrofolate reductase, but bacteria are prone to drug resistance and are rarely used alone. Sulfonamides inhibit dihydrofolate synthase. The combination of the two can double block the folic acid metabolism of bacteria, thus greatly improving the antibacterial effect (several times to dozens of times), so it is called a sulfonamide synergist, and can reduce the emergence of drug-resistant strains . p-Hydroxybenzaldehyde is an intermediate of trimethoprim medicine, the advantages and disadvantages of its synthesis method are of great economic significance for improving the quality of medicine synthesis products and reducing the content of by-products. Contents of the invention ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C45/64C07C47/565C07C245/20
CPCC07C45/64C07C245/20
Inventor 彭响亮
Owner 厦门莱恩斯特信息科技有限公司
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