Optical active compound of anti-infective prulifloxacin and preparation method thereof

Abstract

An optical active compound of anti-infective prulifloxacin and a preparation method thereof relate to an antimicrobial agent of optical active sulfur-nitrogen oxetane and quinoline carboxylic acid, and a preparation method. The compound of the invention takes the following formula 1 to show the compound and salt thereof, the stereo configuration is in S configuration, and the compound has the optical activity of levorotary deviated light; the compound and the salt for medical purpose can be added with pharmaceutical adjuvant to make into preparations for oral use; the method comprises: taking levorotary ulifloxacin as raw material, putting into an organic solvent, and reacting under the condition of the existence of alkali substance, with the reaction temperature of 20 DEG C below zero to 60 DEG C, and the reaction time of 15min to 24h. The levorotary prulifloxacin and physically allowed salt thereof can substitute for the existing antibacterial prulifloxacin and physically allowed salt thereof, not only antibacterial action is obviously improved, but also the toxicity is little.

Description

Technical field

[0001] The invention relates to an optically active antibacterial agent of thiazetidine quinoline carboxylic acid and a preparation method. Specifically, it relates to an optically active compound of prulifloxacin, its oral preparation and a preparation method thereof. Background technique

[0002] Quinolones are a class of anti-infectives synthesized in recent years. They are widely used clinically in the treatment of respiratory system, gastrointestinal tract, urinary system, dermatology, gynecology, surgery and other fields, with good results. Prulifloxacin, chemical name (±)6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxol-4-yl) )Methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazetidine[3,2-α]quinoline-3-carboxylic acid, a joint venture with Japan New Drug A quinolone drug jointly developed by Meiji Confectionery. Pralifloxacin is a third-generation fluoroquinolone broad-spectrum antibacterial drug, which has a broad-spectrum antibacterial effect on gram-positive an...

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