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Synthesis method of pentoxifylline

A technology of pentoxifylline and a synthetic method, applied in the direction of organic chemistry and the like, can solve problems such as unreasonable medication, change of indications, etc., and achieve the effects of simple synthesis process, improved reaction yield and simple process

Active Publication Date: 2021-08-06
HAINAN GENERAL & KANGLI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In this patent, two functional raw materials, taurine and vitamin B6, are added to the pentoxifylline pharmaceutical composition, which will change its indications and cause unreasonable drug use.

Method used

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  • Synthesis method of pentoxifylline
  • Synthesis method of pentoxifylline
  • Synthesis method of pentoxifylline

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1 A kind of synthetic method of pentoxifylline S1

[0027] The present embodiment provides a synthetic method of pentoxifylline S1, the synthetic method is:

[0028] Measure 70ml of THF into the reaction vessel, start stirring and cool down to -15°C, then weigh 11.5g of amino-5-hexanone into the cooled THF, add 27ml of TEA, mix well, keep warm at -15°C, gradually Add dropwise 23.5g of 4-(nitromethylacyl chloride)-1-methylimidazolium-5-acyl chloride solution dissolved in 20mlTHF, react for 45min, take a small amount of reaction solution as a sample, and inject it into a liquid chromatograph for detection. Amino-5- The absorption peak of hexanone disappears, and the reaction can be terminated, and its reaction formula is:

[0029]

[0030] At -15°C, add 100ml of purified water to the reaction solution and stir for 10min, add 300ml of ethyl acetate and continue to stir for 5min, then let stand to separate layers, remove the water phase, keep the organic phas...

Embodiment 2-4

[0031] The synthetic method of embodiment 2-4 pentoxifylline S2-S4

[0032] The synthesis methods of pentoxifylline S2-S4 provided in Examples 2-4 are basically the same as those in Example 1, the only difference being that some process parameters are different, and the specific process parameters are shown in Table 1.

[0033] Table 1: Process parameter table of pentoxifylline S2-S4

[0034]

[0035]

[0036] Other parameters are all the same as in Example 1.

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Abstract

The invention belongs to the field of medicine synthesis, and discloses a synthesis method of pentoxifylline, which is characterized in that 4-(nitrogen methyl acyl chloride)-1-methylimidazole-5-acyl chloride and amino-5-hexanone are subjected to condensation ring closing, and the target product pentoxifylline is synthesized by only one-step reaction. The pentoxifylline synthesis method provided by the invention is simple in synthesis process, and byproducts obtained in the reaction process can be recycled to synthesize pentoxifylline again. The method is suitable for synthesizing pentoxifylline, and the synthesized pentoxifylline is used for preparing pentoxifylline for injection.

Description

technical field [0001] The invention belongs to the field of medicine synthesis, and relates to a synthesis method of a cerebrovascular medicine raw material, in particular to a synthesis method and application of pentoxifylline. Background technique [0002] Pentoxifylline (Pentoxifylline) chemical name is 3,7-dihydro-3,7-dimethyl-1-(5-oxohexyl)-1H-purine-2,6-dione, white needle crystal . Molecular formula is C 13 h 18 N 4 o 3 , the molecular weight is 278.3, and the structural formula is: [0003] [0004] Pentoxifylline is an agent for improving cerebral circulation and peripheral vascular circulation disorders, which has the effect of expanding cerebral blood vessels and peripheral blood vessels, and improving blood circulation in the brain and extremities. In addition, it can improve the oxidation capacity of hypoxic tissues. It is mainly used for the improvement of cerebral circulation after ischemic stroke, and it can also be used for the treatment of periph...

Claims

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Application Information

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IPC IPC(8): C07D473/10
CPCC07D473/10
Inventor 唐雄肇符永红林方育肖汉文林小雪
Owner HAINAN GENERAL & KANGLI PHARMA
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