131190-82-4Relevant articles and documents
Synthesis process of S-(-)-nadifloxacin chiral intermediate
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Paragraph 0014; 0058-0060; 0063-0065; 0068-0070; 0073-0077, (2021/10/27)
The invention discloses a synthesis process of an S-(-)-nadifloxacin chiral intermediate, and belongs to the technical field of chemical pharmacy. The synthesis process comprises the following steps: 1, synthesizing an intermediate 1; and 2, synthesizing the S-(-)-chiral intermediate. R binaphthylenediamine is used as a matrix of a chiral ligand, epoxy polysilsesquioxane is grafted on a molecule of N-Boc-L-histidine to form the chiral ligand, on one hand, the ee value is increased by utilizing the chiral characteristic of N-Boc-L-histidine, and on the other hand, the ee value is increased by utilizing the characteristics of nanoscale size and solubility of the epoxy polysilsesquioxane, so that the solubility of the catalyst is increased, and the catalyst can be mixed with the reactant in the nanometer size so as to improve the catalytic performance of the chiral catalyst and improve the reaction yield, such that the chiral ligand and the metal ruthenium are subjected to coordination to form the chiral catalyst so as to provide the good chiral amplification effect;.
Synthesis, antibacterial activities, mode of action and acute toxicity studies of new oxazolidinone-fluoroquinolone hybrids
Liu, Lili,Shao, Liping,Li, Jing,Cui, Haifeng,Li, Bing,Zhou, Xuzheng,Lv, Pengyue,Zhang, Jiyu
, (2019/05/01)
To combat bacterial resistance, a series of new oxazolidinone-fluoroquinolone hybrids have been synthesized and characterized. All synthetic hybrids were preliminarily evaluated for their in vitro antibacterial activities against 6 standard strains and 3 clinical isolates. The majority of hybrids displayed excellent activities against Gram-positive bacteria, but limited activities against Gram-negative bacteria. Hybrids OBP-4 and OBP-5 were found to be the most promising compounds. Further, in vitro antibacterial activities, mode of action and acute toxicity in mice of hybrids OBP-4 and OBP-5 were investigated. Hybrids OBP-4 and OBP-5 exhibited potent activities against Gram-positive bacteria, including drug-resistant strains. Correspondingly, studies on the mode of action of hybrids OBP-4 and OBP-5 indicated a strong inhibitory activity on protein synthesis by binding the active site of 50S subunit, but a weak inhibitory action on DNA synthesis. In addition, LD50 values of hybrids OBP-4 and OBP-5 in the acute oral toxicity were larger than 2000 mg/kg, suggesting a good safety profile.
DIPHENYLMETHANE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS
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Page/Page column 44, (2008/06/13)
The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.
DIPHENYL SUBSTITUTED CYCLOALKANES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE
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Page/Page column 55, (2008/06/13)
The instant invention provides compounds of Formula (I) which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
A practical synthesis of (S)-(-)-nadifloxacin: Novel acid-catalyzed racemization of tetrahydroquinaldine derivative
Hashimoto, Koji,Okaichi, Yoshihiko,Nomi, Daisuke,Miyamoto, Hisashi,Bando, Masahiko,Kido, Masaru,Fujimura, Tsutomu,Furuta, Takuya,Minamikawa, Jun-Ichi
, p. 642 - 645 (2007/10/03)
(S)-(-)-Nadifloxacin [(S)-(-)-9-fluro-6,7-dihydro-8-(4-hyroxy-1- piperidyl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, (S)- (-)-OPC-7251], an antibacterial agent, was synthesized from (S)-(-)-5,6- difluoro-2-methyl-1,2,3,4-tetrahydroquinoline (DFTQ), which was prepared by the optical resolution of racemic DFTQ with 2,3-di-O-benzoyl-L-tartaric acid. Racemization of the undesired enantiomer [(R)-(+)-DFTQ] was studied in the presence of various acids and the best result was obtained in the case of methanesulfonic acid. The absolute configuraton of (-)-nadifloxacin was determined as S by X-ray crystallographic analysis.