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Method for preparing butafosfan

A technology of butafosfos and n-butylamine, which is applied in the field of preparation of butafosfos, can solve the problems of short steps, no literature report on the preparation method, and no mention of the preparation method of butafosfos, and achieve short reaction steps and suitable The effect of large-scale industrial production and low cost

Active Publication Date: 2010-12-15
HANGZHOU FST PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The method has short steps and is easy to operate, but the article does not mention the preparation method of butafosfos
In recent years, with the widespread application of butafosfos as an organophosphorus supplement, more and more scientists and scientific research institutions have done a lot of theoretical research on its structural characteristics and functional efficacy, but its preparation method has not been seen in the literature so far. to report

Method used

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  • Method for preparing butafosfan
  • Method for preparing butafosfan

Examples

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Effect test

Embodiment 1

[0021] Put 14.6kg of n-butylamine, 100kg of acetone, and 20kg of molecular sieve into a three-necked flask, heat up to 40°C-45°C and stir, keep warm for 3 hours, after the reaction is complete, cool slightly, control the temperature at 20°C-25°C, and slowly add hypophosphorous acid dropwise 13.5kg, the dropwise addition was completed, and the reaction was kept for 2 hours, a large amount of white solid was precipitated, and the crude product was obtained by centrifugation. Add 3 times the amount of ethanol and 5% activated carbon and raise the temperature to 70°C for reflux. After holding the heat for 1 hour, suction filter it into a crystallization kettle and cool it to 10°C.

Embodiment 2

[0023] Put 14.6kg of n-butylamine, 100kg of acetone, and 20kg of molecular sieve into a three-necked flask, heat up to 40°C-45°C and stir, keep warm for 3 hours, after the reaction is complete, cool slightly, control the temperature at 20°C-25°C, and slowly add hypophosphorous acid dropwise 20kg, the dropwise addition was completed, and the reaction was kept for 2 hours, a large amount of white solid was precipitated, and the crude product was obtained by centrifugation. Add 3 times the amount of ethanol and 5% activated carbon and raise the temperature to 70°C for reflux. After holding the heat for 1 hour, suction filter it into a crystallization kettle and cool it to 10°C.

Embodiment 3

[0025] Put 14.6kg of n-butylamine, 100kg of acetone, and 20kg of molecular sieve into a three-necked flask, heat up to 40°C-45°C and stir, keep warm for 3 hours, after the reaction is complete, cool slightly, control the temperature at 20°C-25°C, and slowly add hypophosphorous acid dropwise 25kg, the dropwise addition was completed, and the reaction was incubated for 2 hours, a large amount of white solid was precipitated, and the crude product was obtained by centrifugation. Add 3 times the amount of ethanol and 5% activated carbon and raise the temperature to 70°C for reflux. After holding the heat for 1 hour, suction filter and cool to 10°C in a crystallization kettle.

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Abstract

The invention discloses the fields of organic chemistry and pharmaceutical chemistry, and in particular relates to a method for preparing butafosfan. The method comprises the following steps of: putting n-butylamine, acetone and a molecular sieve into a reaction kettle, raising the temperature and stirring for reaction, cooling, controlling the temperature to be between 20 and 25 DEG C, adding hypophosphorous acid and reacting for certain time, and centrifuging to obtain a crude product; and adding ethanol and activated carbon, raising the temperature to 70 DEG C, filtering until a crystallizing kettle is cooled to 10 DEG C, precipitating and centrifuging to obtain a fine product, and drying in a fine product drying room to obtain a finished product. The method has the advantages of abundant source and low price of raw materials, short reaction steps, simple operation, ideal yield (over 90 percent) by optimizing reaction conditions, low cost and environmental friendliness; and the product prepared by the method can be used for preparing veterinary medicaments and the like.

Description

technical field [0001] The invention belongs to the field of organic chemistry and medicinal chemistry, in particular to a preparation method of butafosfos. technical background [0002] Butafosfos is an important veterinary pharmaceutical raw material and an effective organophosphate supplement. It can promote liver function, help the muscle motor system to recover from fatigue, reduce stress response, stimulate appetite, and promote non-specific immune function; it is a physical stimulation mode with no residue in the body and no toxic side effects. [0003] The chemical name of butafosfos is 1-(butylamino)-1-methylethyl]-phosphonic acid. English name: Butafostan; alias: Butaphosphan; 1-(Butylamino)-1-methylethyl]-phosphonic acid; its chemical structure is: [0004] [0005] Molecular formula is C 7 h 18 NO 2 P, molecular weight 179.20, CAS accession number: 17316-67-5. [0006] In 1967, German scientist Kreutzkamp reported a general preparation method for α-subst...

Claims

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Application Information

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IPC IPC(8): C07F9/30
Inventor 吴永龙徐竹清陈长荣徐伟
Owner HANGZHOU FST PHARMA