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A kind of method of synthesizing theophylline

A technology of theophylline and mixed acid solution, which is applied in the direction of organic chemistry, can solve the problems of complicated process, low purity of theophylline, and low yield, and achieve the effect of simple operation process, simple reaction conditions, and high purity

Active Publication Date: 2016-04-13
HEFEI PINGGUANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the biological extraction method mainly uses tea leaves as raw materials, and theophylline is obtained through extraction, resin adsorption, purification and other steps, but the purity of theophylline is not high.
However, the chemical synthesis method often has complex processes, and the yield of each step reaction is low.

Method used

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  • A kind of method of synthesizing theophylline
  • A kind of method of synthesizing theophylline

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Experimental program
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Effect test

Embodiment 1

[0028] A kind of method of synthesizing theophylline that the present invention proposes, comprises the steps:

[0029] S1. Add 10 parts of dimethyl sulfate, 3.5 parts of 6-aminouracil, 32 wt% sodium hydroxide solution and water into the first reaction vessel in parts by weight, stir in an ice-salt bath for 4.2 hours, filter and wash with water , drying to obtain material A, wherein the mass volume ratio (g / ml) of 6-aminouracil and sodium hydroxide solution is 9:12, and the volume ratio of sodium hydroxide solution and water is 6.5:24;

[0030] S2. Add 11 parts of material A to 610 parts of formic acid in parts by weight, heat to 100° C. and reflux for 13 hours, then continue to add saturated sodium bicarbonate solution until no crystals continue to precipitate, and obtain solid material B by filtration;

[0031] S3. Put the solid material B in a reaction container, add the mixed acid solution, heat to 100°C, reflux for 0.8h, add ice water until no crystals continue to precipi...

Embodiment 2

[0034] A kind of method of synthesizing theophylline that the present invention proposes, comprises the steps:

[0035] S1. Add 9.3 parts of dimethyl sulfate, 3.6 parts of 6-aminouracil, 31.5 wt% sodium hydroxide solution and water into the first reaction vessel in parts by weight, stir in an ice-salt bath for 4.2 hours, filter, Washing and drying to obtain material A, wherein the mass volume ratio (g / ml) of 6-aminouracil to sodium hydroxide solution is 8.1:12.2, and the volume ratio of sodium hydroxide solution to water is 21:82;

[0036] S2. Add 10 parts of material A to 614 parts of formic acid in parts by weight, heat to 100.5°C and reflux for 12 hours, then continue to add saturated sodium bicarbonate solution until no crystals continue to precipitate, and filter to obtain solid material B;

[0037]S3. Put the solid material B in a reaction vessel, add the mixed acid solution, heat to 99°C, reflux for 1 hour, then add ice water until no crystals continue to precipitate, t...

Embodiment 3

[0040] A kind of method of synthesizing theophylline that the present invention proposes, comprises the steps:

[0041] S1. Add 8.5 parts of dimethyl sulfate, 4 parts of 6-aminouracil, 31 wt% sodium hydroxide solution and water into the first reaction vessel in parts by weight, stir in an ice-salt bath for 4.5 hours, filter and wash with water , dry to obtain material A, wherein the mass volume ratio (g / ml) of 6-aminouracil and sodium hydroxide solution is 7.3:12.6, and the volume ratio of sodium hydroxide solution and water is 31:127;

[0042] S2. Add 8 parts of material A to 620 parts of formic acid in parts by weight, heat to 102°C and reflux for 10 hours, then continue to add saturated sodium bicarbonate solution until no crystals continue to precipitate, and obtain solid material B by filtration;

[0043] S3. Put the solid material B in a reaction vessel, add the mixed acid solution, heat to 98°C, reflux for 1.1h, then add ice water until no crystals continue to precipita...

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Abstract

The invention discloses a method for synthesizing theophylline. The method comprises the following steps: performing a methylation reaction on dimethyl sulfate, 6-aminouracil and a sodium hydroxide solution; adding formic acid for a carboxylation reaction; adding a mixed acid solution formed by mixing fuming nitric acid and concentrated sulfuric acid at a volume ratio of (0.8-1.1):(0.9-1.2), and performing heating reflux for a nitrosylation reaction; and finally, adding iron powder and anhydrous acetic acid for a cyclization reaction to obtain theophylline. According to the method disclosed by the invention, the yield is greatly higher than that of the prior art, the operation process is simple, and the reaction conditions are simple.

Description

technical field [0001] The invention relates to the technical field of synthesizing theophylline, in particular to a method for synthesizing theophylline. Background technique [0002] Theophylline is a methylpurine drug, the chemical name is 1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione, which has the functions of strengthening the heart, diuresis, dilating coronary arteries, and stimulating the central nervous system. Through systemic effects, it can be used to treat bronchial asthma, emphysema, bronchitis, and cardiac dyspnea. Its structural formula is: [0003] [0004] At present, the preparation methods of theophylline mainly include biological extraction and chemical synthesis. Among them, the biological extraction method mainly uses tea leaves as raw materials, and theophylline is obtained through steps such as extraction, resin adsorption, and purification, but the purity of theophylline is not high. However, the chemical synthesis method is often complicated i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D473/08
CPCC07D473/08
Inventor 王康林张成栋马婕
Owner HEFEI PINGGUANG PHARMA
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