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Prepn. of L-2-amino propanol

A kind of technology of aminopropanol and production process, which is applied in the field of production process for preparing L-2-aminopropanol, can solve the problems of low yield and increased cost of levofloxacin, etc., and achieve improved product yield and good economy Benefits, the effect of reducing the cost of raw materials

Inactive Publication Date: 2004-03-10
昆山虹祺药业有限责任公司
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AI Technical Summary

Problems solved by technology

[0003] The present invention is in order to solve the problem that the cost of levofloxacin is increased due to the low yield of L-2-alanine due to the reduction of the first esterification of the current industrial production method, the adopted technical scheme is: -2-aminopropionic acid as raw material, ①, potassium borohydride and anhydrous zinc chloride first react in ethylene glycol dimethyl ether solvent, L-2-aminopropionic acid is then added to the reaction solution to undergo a reduction reaction, the reduction After the reaction, hydrolyze under alkaline conditions, ②, separate the organic layer, after the water layer is extracted by the extractant, combine the organic layer, dry with a desiccant, and distill to obtain the product L-2-aminopropanol

Method used

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Embodiment Construction

[0006] The present invention is described in further detail in conjunction with embodiment:

[0007] Add ethylene glycol dimethyl ether (500 ml), anhydrous zinc chloride (60 g, 0.441 mol) and potassium borohydride (30 g, 0.566 mol) in sequence, and after reacting at room temperature for 1 hour, add L-2-aminopropyl Acid (25 g, 0.278 mol) was refluxed for 5 hours, cooled to room temperature, the reaction solution was poured into industrial liquid caustic soda (150 ml, content 40%), reacted at 40 degrees Celsius for 1 hour, cooled to room temperature, and the organic layer, the water layer was extracted with n-butanol, the organic layers were combined, dried overnight with anhydrous sodium sulfate, most of the solvent was evaporated under reduced pressure, and the fraction at 72-73 degrees Celsius / 1.47KPa was collected by rectification to obtain a viscous colorless liquid That is, the product L-2-aminopropanol (9.5 g, 45%), the content is greater than or equal to 99.0% (gas chrom...

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Abstract

The present invention is the preparation process of L-2-amino propanol, as one important intermediate for preparing L-Ofloxacin, by using L-2-aminopropionic acid as main raw material. The technological process includes the reaction of potassium borohybride and anhydrous zinc chloride in aldehyde acetal solvent, the reduction reaction of L-2-aminopropionic acid added into the reaction solution and the hydrolysis in alkali condition; separating organic layers, extracting water layer, merging the organic layers, drying and distillation to obtain product L-2-amino propanol. The present invention has simplified process, high product yield and low material cost of L-Ofloxacin.

Description

(1) Technical field [0001] The invention relates to a production process for preparing L-2-aminopropanol by using L-2-aminopropionic acid as a raw material, which is a method for producing L-2- A new process for the production of aminopropanol. (2) Background technology [0002] L-2-aminopropanol is an important intermediate for the preparation of levofloxacin, which is a synthetic broad-spectrum antibacterial drug. The antibacterial activity of this product is 8 to 128 times greater than that of the corresponding dextrorotary form, and the effective rate against intestinal infection and gonorrhea infection is 100%, and its water solubility is 10 times that of ofloxacin. Because the drug has definite curative effect and low toxic and side effects, it is currently a bulk drug in clinical use. In China, the industrial production method of first esterifying L-2-alanine and then reducing it is mostly used. Due to the high price of raw materials and low yield, the cost of levof...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C213/08C07C215/06C07C215/08
Inventor 王斌王皆胜
Owner 昆山虹祺药业有限责任公司