- Synthesis method of ozenoxacin
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A synthesis method of ozenoxacin belongs to the technical field of medicinal chemistry and synthetic chemistry. The method comprises the following steps: (1) taking N-(5-bromo-3-methyl-2-pyridyl) methylamine as a raw material, and carrying out amino protection reaction to obtain an intermediate II; (2) with the intermediate II as a raw material, carrying out a boronation reaction to obtain an intermediate III; (3) carrying out Suzuki coupling reaction on the intermediate III and 7-chloro-1-cyclopropyl-8-methyl-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid ethyl ester to obtain a condensation compound intermediate IV; and (4) removing a protecting group from the condensation compound intermediate IV under an acidic condition, and hydrolyzing the condensation compound intermediate IV under an alkaline condition to obtain ozenoxacin. The method has the advantages that the generation of genotoxic impurities is effectively avoided, the yield and quality of the final product are improved, the reaction conditions are milder, the monitoring cost of the production process is reduced, and the method has a good industrial prospect.
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Paragraph 0018; 0020; 0026; 0027; 0033; 0034; 0040-0041
(2020/09/30)
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- CRYSTALLINE FORM OF OZENOXACIN AND PROCESSES FOR PREPARATION THEREOF
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The present invention relates to a crystalline form of 1-cyclopropyl-8-methyl-7- (5-methyl-6-(methylamino)pyridin-3-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid the compound of formula-1, which is represented by the following structural formula-1. The
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- Preparation method of Ozenoxacin and intermediates thereof
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The invention provides compounds represented by the formula (IIIb) and a preparation method thereof. The invention also provides an application of the compound represented by the formula (IIIb) as a key intermediate in Ozenoxacin preparation.
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- Quinolonecarboxylic acid derivatives or salts thereof
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Novel quinolonecarboxylic acid derivatives of general formula (1) or salts thereof which have potent antibacterial effects on gram-positive bacteria in particular Propionibacterium acnes (wherein R1represents a hydrogen atom or a carboxyl-protective group; R2represents an optionally substituted cycloalkyl group; R3represents a hydrogen atom, a halogen atom, an optionally substituted alkyl, alkoxy or alkylthio group, an optionally protected hydroxyl or amino group, or a nitro group; R4represents an optionally substituted alkyl or alkoxy group; and Z represents a pyridin-4-yl or pyridin-3-yl group which is optionally substituted with at least one group selected from a halogen atom, an optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio or amino group and an optionally protected hydroxyl or amino group).
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Page column 43
(2010/01/30)
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