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Method for synthesizing L-2-amino propanol

A synthesis method and aminopropanol technology are applied in the preparation of aminohydroxy compounds, chemical instruments and methods, preparation of organic compounds, etc., can solve the problems of difficulty in separation and purification, unsuitable for industrial production, etc., and achieve cost reduction and unit consumption reduction. Effect

Inactive Publication Date: 2008-06-18
HEFEI UNIV OF TECH
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Problems solved by technology

In addition to the above methods, there are also asymmetric synthesis methods and racemate resolution methods. The separation and purification in this method are relatively difficult and are not suitable for industrial production.

Method used

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  • Method for synthesizing L-2-amino propanol

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Embodiment Construction

[0011] 1. Preparation of reducing agent tetramethylammonium borohydride

[0012] Mix and stir 55.5g of tetramethylammonium chloride, 40g of sodium hydroxide, 0.5g of sodium chloride, and 100ml of water, slowly add 27.8g of potassium borohydride in 100ml of aqueous solution at room temperature for 30 minutes, and control the temperature at 35°C. Reaction 2h. After the reaction, 20-30ml of water was distilled off under reduced pressure, left to cool, and a large amount of tetramethylammonium borohydride crystals were formed, and filtered by suction to obtain 44.6g of tetramethylammonium borohydride, with a yield of 98.6%.

[0013] 2. Preparation of intermediate L-2-aminopropanol

[0014] (1) Esterification:

[0015] Mix and stir 18g of L-alanine and 300ml of ethanol, then cool down to below 4°C, add 26.5g of thionyl chloride dropwise within 30min, control the temperature not to exceed 5°C, remove the cooling, and react at 40°C for 4h. Evaporate about 250ml of ethanol from the...

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Abstract

The invention discloses a method for the synthesis of L-2-aminopropanol. L-alanine is taken as starting material, and L-alanine is esterified, and then is reduced for 0.5-2h in organic solvent with tetramethylammonium borohydride as reducing agent; subsequently, is separated after reduction for 2-6h under 35-55 DEG C. The tetramethylammonium borohydride is prepared by the reaction of potassium borohydride with tetramethylammonium chloride, sodium chloride is added during reaction, the reacted product is separated by removing part of water crystallization. The yield of one crystallization separation is greater than or equal to 98 percent, and purification is not required and the product can be used to reduction directly. Since the method adopts the novel reducing agent, the original 2 tons of potassium borohydride required by each ton of L-2- aminopropanol is reduced to 1.25 tons, and as a result, the cost of levofloxacin is largely reduced.

Description

1. Technical field [0001] The invention relates to a preparation method of fine chemicals, in particular to a preparation method of a pharmaceutical intermediate, in particular to a synthesis method of L-2-aminopropanol. 2. Background technology [0002] L-2-aminopropanol is an important chiral intermediate for the synthesis of levofloxacin. Levofloxcain (levofloxcain, DR-3355) is the S-shaped levorotatory optical isomer of ofloxacin ofloxacin, with twice the antibacterial activity of the latter, less toxic side effects, and greater water solubility. In addition to oral dosage forms, it can also be made into injection dosage forms. It is one of the excellent broad-spectrum antibacterial drugs in quinolones. The antibacterial activity of levofloxacin is 8 to 128 times that of the enantiomer. It is 100% effective for intestinal infection and gonococcal infection. It is one of the bulk drugs currently used clinically. At present, the main method of producing L-2-aminopropa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C215/08C07C213/00
Inventor 曾庆梅胡斌徐迪韩抒张冬冬
Owner HEFEI UNIV OF TECH
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