- Preparation method of quinolone carboxylic acid derivative or phthalazinone carboxylic acid derivative
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The invention belongs to the field of pharmaceutical chemicals, relates to a preparation method of a quinolone carboxylic acid derivative or a phthalazinone carboxylic acid derivative, and particularly relates to a preparation method of a 7-substituted-3-quinolone carboxylic acid derivative or a 7-substituted-1,5-phthalazinone carboxylic acid derivative. The preparation method comprises the following steps: (1) in an organic solvent, carrying out coupling reaction on a boron chelate II and organic amine III in the presence of an organosilicon compound to obtain a compound IV; and (2) mixing the compound IV with hydrochloric acid, and then filtering and separating the precipitated compound I. Compared with conventional methods, the preparation method provided by the invention has the advantages that the conditions are milder, the hydrolysis of the substrate quinoline carboxylic acid boric acid ester can be reduced, and meanwhile, the influence of a byproduct HF on the product purity is avoided. The method is high in yield and high in purity; compared with the traditional alkali, the organic silicon is more suitable for industrial preparation of the 7-substituted-3-quinolone carboxylic acid derivative or the 7-substituted-1,5-phthalazinone carboxylic acid derivative.
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Paragraph 0098-0100; 0179
(2021/10/27)
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- Cyclopropanation–ring expansion of 3-chloroindoles with α-halodiazoacetates: Novel synthesis of 4-quinolone-3-carboxylic acid and norfloxacin
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We present a short and efficient way of synthesizing two synthetically versatile 4-quinolone-3-carboxylate building blocks by cyclopropanation-ring expansion of 3-chloroindoles with α-halodiazoacetates as the key step. This novel transformation was applied towards the synthesis of the antibiotic drug norfloxacin.
- Peeters, Sara,Berntsen, Linn Neerbye,Rongved, P?l,Bonge-Hansen, Tore
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p. 2156 - 2160
(2019/09/30)
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- Developing ciprofloxacin analogues against plant DNA gyrase: A novel herbicide mode of action
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Ciprofloxacin has been shown to exhibit potent herbicidal activity through action against plant DNA gyrase, presenting a novel mode of action. Analogues of ciprofloxacin have been prepared with increased herbicidal activity and diminished antibacterial activity, compared to ciprofloxacin, as demonstrated using model systems.
- Wallace, Michael D.,Waraich, Nidda F.,Debowski, Aleksandra W.,Corral, Maxime G.,Maxwell, Anthony,Mylne, Joshua S.,Stubbs, Keith A.
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supporting information
p. 1869 - 1872
(2018/02/23)
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- ANTIBIOTIC RESISTANCE BREAKERS
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The invention relates to antibiotic compounds of formula (A1) and pharmaceutically acceptable salts, solvates, tautomers and combinations thereof, wherein X and L are optional linkers and one of RA or R1 comprises Ar1, wherein Ar1 is an antibiotic resistance breaker moiety which comprises an optionally substituted C6-10 aryl, C7-13 aralkyl, C5-10 heteroaryl, C6-13 heteroaralkyl, C5-10 heterocyclyl, C6-13 heterocyclalkyl, C3-10 carbocyclyl, C4-13 carbocyclalkyl, -C(=NR')-NR'R'' or –CH2- CH=CH2 group; wherein after administration of the compound to a bacterial infection this moiety reduces or prevents efflux. The invention also discloses pharmaceutical compositions comprising compounds of formula (A1) and the use of such compounds as medicaments, in particular, to treat bacterial infections, such as drug-resistant bacterial infections.
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Page/Page column 100; 101
(2019/01/05)
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- An expeditious synthesis of quinolone antibacterials
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A facile and rapid synthesis of ciprofloxacin under microwave irradiation is described. The product ciprofloxacin was isolated and the impurity was characterized as the product of substitution of fluorine instead of chlorine in acid 1. Similarly norfloxacin was synthesized.
- Heravi, Majid M.,Oskooie, Hossein A.,Motamedi, Radineh,Ghassemzadeh, Mitra
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p. 423 - 426
(2007/10/03)
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- Substituted quinoline carboxylic acid derivatives
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This invention relates to new compounds of value as antibacterial agents. More particularly, it relates to quinoline carboxylic acid derivatives, the hydrates and the acid or alkali addition salts thereof.
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- Piperazinyl derivatives of quinoline carboxylic acids
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This invention relates to new compounds of value as antibacterial agent. More particularly, it relates to piperazinyl derivatives of quinoline carboxylic acids, the hydrates, and the acid addition salts thereof.
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