Method for producing aztreonam amino acid salt

Abstract

The invention discloses a synthesis method for aztreonam salt. The method comprises the steps as follow: aztreonam is dissolved into organic solvent; the water solution of amino acid is dropped in the mixture; and the aztreonam salt is obtained by cooling and filtering the solution after full reaction. The invention is characterized in that the organic solvent is used as reaction solution, thereby ensuring the salt making reaction of aztreonam to be more completely with the high reaction yield; the used solvent can be recycled, thereby enabling the aztreonam amino acid salt to have better water-solubility and to be more easily to be made into preparations; and the salt is no longer mixed with the amino acid, thereby being more convenient for medicine use. The invention has the advantages of easy operation, high purity, low cost, and being suitable for mass production.

Description

technical field [0001] The invention relates to a preparation method of antibacterial drugs, in particular to a preparation method of aztreonam amino acid salt. Background technique [0002] Aztreonam is a new monocyclic β-lactam antibiotic first developed by Bristol-Myers Squibb in the United States. It was first launched in Italy in 1984, and then in many European and American countries. It is the first monocyclic β-lactam antibiotic used clinically. It is currently used clinically well, and its curative effect is very affirmed at home and abroad. [0003] The chemical name of aztreonam is: [2s-[2α, 3β(Z)]]-2-[[[1-(2-amino-4-thiazolyl)-2-[(2-methyl-4- Oxo-1-sulfo-3-azetidinyl)amino]-2-oxoethylene]amino]oxo]-2-methylpropionic acid, and has the following chemical structure: [0004] [0005] Its pharmacological action is as follows: aztreonam inhibits the fusion of the cell wall through a high affinity with penicillin-binding protein 3 (PBP3) on the cell membrane of sen...

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Problems solved by technology

[0009] In order to solve the problem of low water solubility of aztreonam, Chinese patent CN1030238 discloses a mixture of preparing aztreonam L-arginine, which is to mix L-arginine and aztreonam, then dissolve it in water and The mixture of L-arginine and aztreonam is obtained by freeze-drying, but there are high investment and operating costs for freeze-drying equipment, long freeze-drying process, high product cost, and problems such as uneven moisture content

[0010] Document WO2005 / 005424 reports a method for preparing aztreonam lysine salt, which is prepared by dissolving aztreonam in water, and then adding an aqueous solution of lysine dropwise. The preparation process of this method is simple and no special equipment is required. Because aztreonam lysine salt has poor stability in aqueous solution, it is partially decomposed into aztreonam and lysine, so that the reaction yield is not high, less than 70%.

[0011] The more common problem of the above methods is that aztreonam salt is not made, but it is directly mixed for medicinal purposes, or it is mixed and then freeze-dried to obtain its mixture, or its lysine salt is obtained in water. The yield is not high

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