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;.
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.
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.