- Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections
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Delafloxacin, a fourth-generation anionic fluoroquinolone (FQ) was approved in 2019 for community acquired bacterial pneumonia (CARP). It has broad spectrum activity and an improved class-related toxicity profile. However, it has recently failed a Phase 3
- Betson, Mark,Bingham, Matilda,Doyle, Paul,Hallworth, Sebastian,Harvey, Rebecca,Huxley, Anthony,Kirk, Ralph,Moat, John,Nelson, Gary,Pesnot, Thomas,Tait, Michael
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- Preparation method of 3-chloro-2,4,5-trifluorobenzoic acid
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The invention discloses a preparation method of 3-chloro-2,4,5-trifluorobenzoic acid. The reaction equation of the method is shown in the description. The preparation method concretely comprises the following steps: preparing a compound of formula (1) fro
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- A 2, 4, 5 - trifluoro -3 - chlorobenzoic acid preparation method
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The invention discloses a 2, 4, 5 - trifluoro - 3 - chlorobenzoic acid preparation method, which belongs to the chemical pharmaceutical intermediates preparation method technical field, the use of 1, 2, 4, - trifluorobenzene as raw materials, by nitration, chloro, re-nitration, reduction, diazotization, cyanide Sandmeyer reaction and hydrolysis reaction for preparing 2, 4, 5 - trifluoro - 3 - chlorobenzoic acid. The method of the invention, the raw materials using relatively inexpensive and easy to obtain, the process route is mature, the operation is simple, high yield, and has high industrial value.
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- Spiro compound
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The present invention relates to spiro compounds of general formula I: STR1 wherein the substituents are herein below defined. The present invention relates to antibacterial spiro compounds which are of value as drugs for humans, veterinary drugs or drugs for use in fish culture or as preservatives, and to antibacterial compositions containing one or more of the same compounds as active ingredients.
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- 2,3,4,5-tetrahalogenobenzene derivatives
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2,3,4,5-trihalogenobenzene derivatives of the formula STR1 in which R is --COOH, --COCl, --COF, --CN, --CONH2, --CH2 OH, --CH2 Cl, --CHCl2, --CCl3 or --CHO, R1 is H, Cl or F, and R2 is Cl or F, it only being possible for R1 or R2 to be F, and processes for their preparation starting from benzonitriles reacted with potassium fluoride. The novel compounds are intermediates for antibacterials such as quinolone carboxylic acids.
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- Process for the synthesis of 3-chloro-2,4,5-trifluorobenzoic acid
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An improved process for the preparation of 3-chloro-2,4,5-trifluorobenzoic acid is described which involves reaction of a diester of 3,4,5,6-tetrafluoro-1,2-benzenedicarboxylic acid with a substituted amine to afford 3-amino-2,4,5-trifluorobenzoic acid followed by subsequent conversion of the amio intermediate into 3-chloro-2,4,5-trifluorobenzoic acid.
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- Antibacterial agents
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Novel quinoline-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
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