- ANTIMICROBIAL QUINOLONES, THEIR COMPOSITIONS AND USES
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Compounds of the following formula (I) are effective antimicrobial agents.
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Page column 83; 84
(2010/02/06)
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- A practical synthesis of (S)-(-)-nadifloxacin: Novel acid-catalyzed racemization of tetrahydroquinaldine derivative
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(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.
- Hashimoto, Koji,Okaichi, Yoshihiko,Nomi, Daisuke,Miyamoto, Hisashi,Bando, Masahiko,Kido, Masaru,Fujimura, Tsutomu,Furuta, Takuya,Minamikawa, Jun-Ichi
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p. 642 - 645
(2007/10/03)
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