- Preparation method of sitafloxacin hydrate
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The invention provides a preparation method of a sitafloxacin hydrate. The preparation method takes a compound II as a raw material, debenzylation, substitution, chlorination and removal of t-butyloxycarboryl are sequentially carried out, and finally the sitafloxacin hydrate is obtained. The preparation method provided by the invention has the advantages that use of hydrogen and an autoclave is avoided, technological operation is greatly simplified, and hidden danger is also eliminated; and reaction in each technological step is rapid, no side reaction is generated, and separation and purification are simple and rapid, so that the preparation method provided by the invention not only has high yield, more importantly, the preparation method also has the advantages of environment friendliness, simple technology and low cost, and industrial large-scale mass production requirement can be met.
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Paragraph 0031; 0043; 0047; 0049; 0055
(2018/03/24)
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- (Fluorocyclopropyl)quinolones. 2. Synthesis and stereochemical structure- activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1- (2-fluorocyclopropyl)quinolone antibacterial agents
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A series of novel chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro- 1-(2-fluorocyclopropyl)-quinolones were synthesized as a continuation of a research project of 1-(2-fluorocyclopropyl)-quinolones by considering stereochemical and physicochemical properties of the molecule. Absolute configurations of the 1-(cis-2-fluorocyclopropyl) moiety and the 7-(7-amino- 5-azaspiro-[2.4]heptan-5-yl) moiety were determined by X-ray crystallographic analysis. Stereochemical structure-activity relationship studies indicated that 1-[(1R,2S)-2-fluorocyclopropyl] and 7-[(7S)-amino-5-azaspiro[2.4]heptan- 5-yl] derivatives are more potent against Gram-positive and Gram-negative bacteria than the other stereoisomers and 7-[(7S)-7-amino-5-azaspiro[2.4]- heptan-5-yl]-8-chloro-1-[(1R,2S)-2-fluorocyclopropyl]quinolone (33) is the most potent of all stereoisomers. Pharmacokinetic profiles and physicochemical properties of the selected compounds were also examined, and it was found that 33 (DU-6859a) possesses moderate lipophilicity and good pharmacokinetic profiles.
- Kimura,Atarashi,Kawakami,Sato,Hayakawa
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p. 3344 - 3352
(2007/10/02)
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