Levo ofloxacin derivative, its production and use

Abstract

A laevo-ofloxacin derivative, its production and use are disclosed. Its chemical molecular formula is (s)-(-)-9-fluorine-2, 3-dihydro-3-methyl-10-(4-methyl-1-piperazine)-7-oxygen7H-pyrido (1,2,3-de)(1,4)-benzoqin-6-carboxylic maleate. It can be used to treat gram-positive bacterium and gram-negative infection. It has better solubility and stability and higher crystallizing rate.

Description

technical field [0001] The invention relates to the technical field of levofloxacin derivatives of broad-spectrum antibiotics, specifically levofloxacin maleate ((s)-(-)-9-fluoro-2,3-dihydro -3-Methyl-10-(4-methyl-1-piperazinyl)-7-oxo 7H-pyrido[1,2,3-de][1,4]-benzoxazine-6-carboxy Acid maleate) and preparation method and application thereof, and the application of the substance (preparation) in the treatment of Gram-positive bacteria and Gram-negative bacteria infection diseases. [0002] The molecular formula is: [0003] Background technique [0004] Qunolones antibacterial drugs refer to a class of antibacterial drugs that contain a 4-quinolone core, among which fluoroquinolones have gradually become the mainstream of this class of drugs. Since the discovery of the first quinolone antibacterial drug by the Sterling-Winthrop Institute in the United States in 1962, many such drugs have appeared one after another. The antibacterial effect can be compared with the third...

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Problems solved by technology

[0009] Levofloxacin mesylate has strong stomach discomfort, can cause adverse reactions in the central nervous system and skin, and occasionally can cause seizures, mental disorders and intermittent nephritis, due to the adverse reactions caused by it And safety has not been determined, especially not suitable for the application of teenagers and infants under the age of 18

[0010] The clinical use of levofloxacin lactate can increase serum alanine aminotransferase, and its lactate ion can produce local irritation when injected locally, and excessive dripping speed during intravenous injection can cause venous irritation symptoms or central nervous system reactions , although most patients can tolerate it, and it can disappear on its own after the course of treatment, but after all, it causes the patient's pain during use, and clinically requires appropriate improvement.

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